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    Daniel Santi, MD, PhD

    TitleProfessor
    SchoolUCSF School of Pharmacy
    DepartmentPharmaceutical Chemistry
    Address600 16th St
    San Francisco CA 94158
    Phone415-215-5586
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      Collapse Biography 
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      University of California, San FranciscoM.D. Medicine1980

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      Collapse Overview
      Dr. Santi received a Ph.D. in Medicinal Chemistry from SUNY in 1967 and a M.D. from UCSF in 1981. He was Assistant Professor of Chemistry at UCSB from 1968 to 1974. He joined the UCSF faculty in 1974 and was Professor of Biochemistry and Biophysics, and of Pharmaceutical Chemistry at UCSF until 2000 when he became CEO of Kosan Biosciences. He returned to UCSF in 2007 where he served as interim Director of the UCSF CTSI and then Director of Translational Research at QB3. He became an Associate Dean of External Relationships in the School of Pharmacy in 2009, and manages an Industry Outreach Program. Dr. Santi has published over 300 scientific papers and is co-inventor on over 40 US patents.

      Santi was a member of the original Scientific Advisory Board of Chiron Corp. and has co-founded five biotechnology companies. In 1988, he founded and was Chairman of the peptide-combinatorial chemistry company Protos Corp., which merged with Chiron in 1992. He was also a co-founder of Parnassus Pharmaceuticals, and of Prospect Genomics which merged with Structural Genomix in 2001. In 1996, he co-founded Kosan Biosciences where he served as CEO and Chairman until 2006 when Kosan was acquired by Bristol Myers Squibb. He co-founded the platform technology company ProLynx LLC in 2010, where he currently serves as President.


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      Publications listed below are automatically derived from MEDLINE/PubMed and other sources, which might result in incorrect or missing publications. Researchers can login to make corrections and additions, or contact us for help.
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      1. Schneider EL, Hearn BR, Pfaff SJ, Fontaine SD, Reid R, Ashley GW, Grabulovski S, Strassberger V, Vogt L, Jung T, Santi DV. Approach for Half-Life Extension of Small Antibody Fragments That Does Not Affect Tissue Uptake. Bioconjug Chem. 2016 Oct 7. PMID: 27657443.
        View in: PubMed
      2. Schneider EL, Henise J, Reid R, Ashley GW, Santi DV. Subcutaneously Administered Self-Cleaving Hydrogel-Octreotide Conjugates Provide Very Long-Acting Octreotide. Bioconjug Chem. 2016 Jul 20; 27(7):1638-44. PMID: 27253622.
        View in: PubMed
      3. Simoni M, Santi D, Negri L, Hoffmann I, Muratori M, Baldi E, Cambi M, Marcou M, Greither T, Baraldi E, Tagliavini S, Carra D, Lombardo F, Gandini L, Pallotti F, Krausz C, Rastrelli G, Ferlin A, Menegazzo M, Pignatti E, Linari F, Marino M, Benaglia R, Levi-Setti PE, Behre HM. Treatment with human, recombinant FSH improves sperm DNA fragmentation in idiopathic infertile men depending on the FSH receptor polymorphism p.N680S: a pharmacogenetic study. Hum Reprod. 2016 Sep; 31(9):1960-9. PMID: 27329968.
        View in: PubMed
      4. Santi D, Vezzani S, Granata AR, Roli L, De Santis MC, Ongaro C, Donati F, Baraldi E, Trenti T, Setti M, Simoni M. Sperm quality and environment: A retrospective, cohort study in a Northern province of Italy. Environ Res. 2016 Oct; 150:144-53. PMID: 27288912.
        View in: PubMed
      5. Schneider EL, Henise J, Reid R, Ashley GW, Santi DV. Hydrogel Drug Delivery System Using Self-Cleaving Covalent Linkers for Once-a-Week Administration of Exenatide. Bioconjug Chem. 2016 May 18; 27(5):1210-5. PMID: 26930186.
        View in: PubMed
      6. Santi D, Granata AR, Guidi A, Pignatti E, Trenti T, Roli L, Bozic R, Zaza S, Pacchioni C, Romano S, Nofer JR, Rochira V, Carani C, Simoni M. Six months of daily treatment with vardenafil improves parameters of endothelial inflammation and of hypogonadism in male patients with type 2 diabetes and erectile dysfunction: a randomized, double-blind, prospective trial. Eur J Endocrinol. 2016 Apr; 174(4):513-22. PMID: 26792933.
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      7. Casarini L, Santi D, Marino M. Impact of gene polymorphisms of gonadotropins and their receptors on human reproductive success. Reproduction. 2015 Dec; 150(6):R175-84. PMID: 26370242.
        View in: PubMed
      8. Marino M, Monzani ML, Brigante G, Cioni K, Madeo B, Santi D, Maiorana A, Bettelli S, Moriondo V, Pignatti E, Bonacini L, Carani C, Rochira V, Simoni M. High-Resolution Melting Is a Sensitive, Cost-Effective, Time-Saving Technique for BRAF V600E Detection in Thyroid FNAB Washing Liquid: A Prospective Cohort Study. Eur Thyroid J. 2015 Jun; 4(2):73-81. PMID: 26279992; PMCID: PMC4521072 [Available on 12/01/15].
      9. Schneider EL, Ashley GW, Dillen L, Stoops B, Austin NE, Malcolm BA, Santi DV. Half-life extension of the HIV-fusion inhibitor peptide TRI-1144 using a novel linker technology. Eur J Pharm Biopharm. 2015 Jun; 93:254-9. PMID: 25900863.
        View in: PubMed
      10. Lotti F, Rochira V, Pivonello R, Santi D, Galdiero M, Maseroli E, Balestrieri A, Faustini-Fustini M, Peri A, Sforza A, Colao A, Maggi M, Corona G. Erectile Dysfunction is Common among Men with Acromegaly and is Associated with Morbidities Related to the Disease. J Sex Med. 2015 May; 12(5):1184-93. PMID: 25736192.
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      11. Henise J, Hearn BR, Ashley GW, Santi DV. Biodegradable tetra-PEG hydrogels as carriers for a releasable drug delivery system. Bioconjug Chem. 2015 Feb 18; 26(2):270-8. PMID: 25584814.
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      12. Fontaine SD, Reid R, Robinson L, Ashley GW, Santi DV. Long-term stabilization of maleimide-thiol conjugates. Bioconjug Chem. 2015 Jan 21; 26(1):145-52. PMID: 25494821.
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      13. Santi D, Giannetta E, Isidori AM, Vitale C, Aversa A, Simoni M. Therapy of endocrine disease. Effects of chronic use of phosphodiesterase inhibitors on endothelial markers in type 2 diabetes mellitus: a meta-analysis. Eur J Endocrinol. 2015 Mar; 172(3):R103-14. PMID: 25277671.
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      14. Brigante G, Spaggiari G, Santi D, Cioni K, Gnarini V, Diazzi C, Pignatti E, Casarini L, Marino M, Tüttelmann F, Carani C, Simoni M. The TRHR Gene Is Associated with Hypothalamo-Pituitary Sensitivity to Levothyroxine. Eur Thyroid J. 2014 Jun; 3(2):101-8. PMID: 25114873; PMCID: PMC4109513.
      15. Santi D, Simoni M. Biosimilar recombinant follicle stimulating hormones in infertility treatment. Expert Opin Biol Ther. 2014 Oct; 14(10):1399-409. PMID: 24889801.
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      16. Santi DV, Schneider EL, Ashley GW. Macromolecular prodrug that provides the irinotecan (CPT-11) active-metabolite SN-38 with ultralong half-life, low C(max), and low glucuronide formation. J Med Chem. 2014 Mar 27; 57(6):2303-14. PMID: 24494988.
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      17. Santi D, Brigante G, Zona S, Guaraldi G, Rochira V. Male sexual dysfunction and HIV--a clinical perspective. Nat Rev Urol. 2014 Feb; 11(2):99-109. PMID: 24394405.
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      18. Schneider EL, Robinson L, Reid R, Ashley GW, Santi DV. ß-Eliminative releasable linkers adapted for bioconjugation of macromolecules to phenols. Bioconjug Chem. 2013 Dec 18; 24(12):1990-7. PMID: 24171387.
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      19. Czudnochowski N, Ashley GW, Santi DV, Alian A, Finer-Moore J, Stroud RM. The mechanism of pseudouridine synthases from a covalent complex with RNA, and alternate specificity for U2605 versus U2604 between close homologs. Nucleic Acids Res. 2014 Feb; 42(3):2037-48. PMID: 24214967; PMCID: PMC3919597.
      20. Ashley GW, Henise J, Reid R, Santi DV. Hydrogel drug delivery system with predictable and tunable drug release and degradation rates. Proc Natl Acad Sci U S A. 2013 Feb 5; 110(6):2318-23. PMID: 23345437; PMCID: PMC3568318.
      21. Zona S, Guaraldi G, Luzi K, Beggi M, Santi D, Stentarelli C, Madeo B, Rochira V. Erectile dysfunction is more common in young to middle-aged HIV-infected men than in HIV-uninfected men. J Sex Med. 2012 Jul; 9(7):1923-30. PMID: 22548701.
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      22. Santi DV, Schneider EL, Reid R, Robinson L, Ashley GW. Predictable and tunable half-life extension of therapeutic agents by controlled chemical release from macromolecular conjugates. Proc Natl Acad Sci U S A. 2012 Apr 17; 109(16):6211-6. PMID: 22474378; PMCID: PMC3341049.
      23. Rochira V, Zirilli L, Orlando G, Santi D, Brigante G, Diazzi C, Carli F, Carani C, Guaraldi G. Premature decline of serum total testosterone in HIV-infected men in the HAART-era. PLoS One. 2011; 6(12):e28512. PMID: 22174826; PMCID: PMC3235128.
      24. Menzella HG, Carney JR, Li Y, Santi DV. Using chemobiosynthesis and synthetic mini-polyketide synthases to produce pharmaceutical intermediates in Escherichia coli. Appl Environ Microbiol. 2010 Aug; 76(15):5221-7. PMID: 20543042; PMCID: PMC2916480.
      25. Bayer TS, Widmaier DM, Temme K, Mirsky EA, Santi DV, Voigt CA. Synthesis of methyl halides from biomass using engineered microbes. J Am Chem Soc. 2009 May 13; 131(18):6508-15. PMID: 19378995.
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      26. Rastelli G, Rosenfeld R, Reid R, Santi DV. Molecular modeling and crystal structure of ERK2-hypothemycin complexes. J Struct Biol. 2008 Oct; 164(1):18-23. PMID: 18571434.
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      27. Hearn BR, Sundermann K, Cannoy J, Santi DV. Semisynthesis and cytotoxicity of hypothemycin analogues. ChemMedChem. 2007 Nov; 2(11):1598-600. PMID: 17691074.
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      28. Menzella HG, Carney JR, Santi DV. Rational design and assembly of synthetic trimodular polyketide synthases. Chem Biol. 2007 Feb; 14(2):143-51. PMID: 17317568.
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      29. Newby Z, Lee TT, Morse RJ, Liu Y, Liu L, Venkatraman P, Santi DV, Finer-Moore JS, Stroud RM. The role of protein dynamics in thymidylate synthase catalysis: variants of conserved 2'-deoxyuridine 5'-monophosphate (dUMP)-binding Tyr-261. Biochemistry. 2006 Jun 20; 45(24):7415-28. PMID: 16768437; PMCID: PMC2556892.
      30. Chandran SS, Menzella HG, Carney JR, Santi DV. Activating hybrid modular interfaces in synthetic polyketide synthases by cassette replacement of ketosynthase domains. Chem Biol. 2006 May; 13(5):469-74. PMID: 16720267.
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      31. Schirmer A, Kennedy J, Murli S, Reid R, Santi DV. Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides. Proc Natl Acad Sci U S A. 2006 Mar 14; 103(11):4234-9. PMID: 16537514; PMCID: PMC1449676.
      32. Reisinger SJ, Patel KG, Santi DV. Total synthesis of multi-kilobase DNA sequences from oligonucleotides. Nat Protoc. 2006; 1(6):2596-603. PMID: 17406514.
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      33. Menzella HG, Reisinger SJ, Welch M, Kealey JT, Kennedy J, Reid R, Tran CQ, Santi DV. Redesign, synthesis and functional expression of the 6-deoxyerythronolide B polyketide synthase gene cluster. J Ind Microbiol Biotechnol. 2006 Jan; 33(1):22-8. PMID: 16187094.
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      34. Menzella HG, Reid R, Carney JR, Chandran SS, Reisinger SJ, Patel KG, Hopwood DA, Santi DV. Combinatorial polyketide biosynthesis by de novo design and rearrangement of modular polyketide synthase genes. Nat Biotechnol. 2005 Sep; 23(9):1171-6. PMID: 16116420.
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      35. Jayaraj S, Reid R, Santi DV. GeMS: an advanced software package for designing synthetic genes. Nucleic Acids Res. 2005; 33(9):3011-6. PMID: 15911632; PMCID: PMC1137029.
      36. Kodumal SJ, Patel KG, Reid R, Menzella HG, Welch M, Santi DV. Total synthesis of long DNA sequences: synthesis of a contiguous 32-kb polyketide synthase gene cluster. Proc Natl Acad Sci U S A. 2004 Nov 2; 101(44):15573-8. PMID: 15496466; PMCID: PMC524854.
      37. Tian ZQ, Liu Y, Zhang D, Wang Z, Dong SD, Carreras CW, Zhou Y, Rastelli G, Santi DV, Myles DC. Synthesis and biological activities of novel 17-aminogeldanamycin derivatives. Bioorg Med Chem. 2004 Oct 15; 12(20):5317-29. PMID: 15388159.
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      38. Kodumal SJ, Santi DV. DNA ligation by selection. Biotechniques. 2004 Jul; 37(1):34, 36, 38 passim. PMID: 15283197.
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      39. Shimazu M, Vetcher L, Galazzo JL, Licari P, Santi DV. A sensitive and robust method for quantification of intracellular short-chain coenzyme A esters. Anal Biochem. 2004 May 1; 328(1):51-9. PMID: 15081907.
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      40. Gonzalez-Pacanowska D, Ruiz-Perez LM, Carreras-Gómez MA, Costi MP, Stroud RM, Finer-Moore J, Santi DV. The structural roles of conserved Pro196, Pro197 and His199 in the mechanism of thymidylate synthase. Protein Eng. 2003 Aug; 16(8):607-14. PMID: 12968078.
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      41. Carreras CW, Schirmer A, Zhong Z, Santi DV. Filter binding assay for the geldanamycin-heat shock protein 90 interaction. Anal Biochem. 2003 Jun 1; 317(1):40-6. PMID: 12729599.
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      42. Jez JM, Chen JC, Rastelli G, Stroud RM, Santi DV. Crystal structure and molecular modeling of 17-DMAG in complex with human Hsp90. Chem Biol. 2003 Apr; 10(4):361-8. PMID: 12725864.
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      43. Hu Z, Desai RP, Volchegursky Y, Leaf T, Woo E, Licari P, Santi DV, Hutchinson CR, McDaniel R. Approaches to stabilization of inter-domain recombination in polyketide synthase gene expression plasmids. J Ind Microbiol Biotechnol. 2003 Mar; 30(3):161-7. PMID: 12715253.
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      44. Finer-Moore JS, Santi DV, Stroud RM. Lessons and conclusions from dissecting the mechanism of a bisubstrate enzyme: thymidylate synthase mutagenesis, function, and structure. Biochemistry. 2003 Jan 21; 42(2):248-56. PMID: 12525151.
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      45. Reid R, Piagentini M, Rodriguez E, Ashley G, Viswanathan N, Carney J, Santi DV, Hutchinson CR, McDaniel R. A model of structure and catalysis for ketoreductase domains in modular polyketide synthases. Biochemistry. 2003 Jan 14; 42(1):72-9. PMID: 12515540.
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      46. Dayem LC, Carney JR, Santi DV, Pfeifer BA, Khosla C, Kealey JT. Metabolic engineering of a methylmalonyl-CoA mutase-epimerase pathway for complex polyketide biosynthesis in Escherichia coli. Biochemistry. 2002 Apr 23; 41(16):5193-201. PMID: 11955068.
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      47. Carreras CW, Siani MA, Santi DV, Dillon SB. Stable expression of a synthetic gene for the human motilin receptor: use in an aequorin-based receptor activation assay. Anal Biochem. 2002 Jan 15; 300(2):146-51. PMID: 11779105.
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      48. Agarwalla S, Kealey JT, Santi DV, Stroud RM. Characterization of the 23 S ribosomal RNA m5U1939 methyltransferase from Escherichia coli. J Biol Chem. 2002 Mar 15; 277(11):8835-40. PMID: 11779873.
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      49. Carreras CW, Fu H, Santi DV. An FKBP12 binding assay based upon biotinylated FKBP12. Anal Biochem. 2001 Nov 1; 298(1):57-61. PMID: 11673895.
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      50. Kawase S, Cho SW, Rozelle J, Stroud RM, Finer-Moore J, Santi DV. Replacement set mutagenesis of the four phosphate-binding arginine residues of thymidylate synthase. Protein Eng. 2000 Aug; 13(8):557-63. PMID: 10964985.
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      51. Siani MA, Skillman AG, Carreras CW, Ashley G, Kuntz ID, Santi DV. Development and screening of a polyketide virtual library for drug leads against a motilide pharmacophore. J Mol Graph Model. 2000 Aug-Oct; 18(4-5):497-511, 539-40. PMID: 11143565.
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      52. Liu Y, Santi DV. m5C RNA and m5C DNA methyl transferases use different cysteine residues as catalysts. Proc Natl Acad Sci U S A. 2000 Jul 18; 97(15):8263-5. PMID: 10899996; PMCID: PMC26935.
      53. Santi DV, Siani MA, Julien B, Kupfer D, Roe B. An approach for obtaining perfect hybridization probes for unknown polyketide synthase genes: a search for the epothilone gene cluster. Gene. 2000 Apr 18; 247(1-2):97-102. PMID: 10773448.
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      54. Variath P, Liu Y, Lee TT, Stroud RM, Santi DV. Effects of subunit occupancy on partitioning of an intermediate in thymidylate synthase mutants. Biochemistry. 2000 Mar 14; 39(10):2429-35. PMID: 10704192.
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      55. Morse RJ, Kawase S, Santi DV, Finer-Moore J, Stroud RM. Energetic contributions of four arginines to phosphate-binding in thymidylate synthase are more than additive and depend on optimization of "effective charge balance". Biochemistry. 2000 Feb 8; 39(5):1011-20. PMID: 10653645.
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      56. Foster PG, Huang L, Santi DV, Stroud RM. The structural basis for tRNA recognition and pseudouridine formation by pseudouridine synthase I. Nat Struct Biol. 2000 Jan; 7(1):23-7. PMID: 10625422.
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      57. Santi DV. Mechanistic studies of RNA modifying enzymes. RNA pseudouridine synthase and m5cytosine methyl transferase. Nucleic Acids Symp Ser. 2000; (44):147-8. PMID: 12903311.
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      58. Gu X, Liu Y, Santi DV. The mechanism of pseudouridine synthase I as deduced from its interaction with 5-fluorouracil-tRNA. Proc Natl Acad Sci U S A. 1999 Dec 7; 96(25):14270-5. PMID: 10588695; PMCID: PMC24426.
      59. Nopponpunth V, Sirawaraporn W, Greene PJ, Santi DV. Cloning and expression of Mycobacterium tuberculosis and Mycobacterium leprae dihydropteroate synthase in Escherichia coli. J Bacteriol. 1999 Nov; 181(21):6814-21. PMID: 10542185; PMCID: PMC94148.
      60. Xue Q, Ashley G, Hutchinson CR, Santi DV. A multiplasmid approach to preparing large libraries of polyketides. Proc Natl Acad Sci U S A. 1999 Oct 12; 96(21):11740-5. PMID: 10518520; PMCID: PMC18356.
      61. Reid R, Greene PJ, Santi DV. Exposition of a family of RNA m(5)C methyltransferases from searching genomic and proteomic sequences. Nucleic Acids Res. 1999 Aug 1; 27(15):3138-45. PMID: 10454610; PMCID: PMC148540.
      62. Costi PM, Rinaldi M, Tondi D, Pecorari P, Barlocco D, Ghelli S, Stroud RM, Santi DV, Stout TJ, Musiu C, Marangiu EM, Pani A, Congiu D, Loi GA, La Colla P. Phthalein derivatives as a new tool for selectivity in thymidylate synthase inhibition. J Med Chem. 1999 Jun 17; 42(12):2112-24. PMID: 10377217.
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      63. Velanker SS, Gokhale RS, Ray SS, Gopal B, Parthasarathy S, Santi DV, Balaram P, Murthy MR. Disulfide engineering at the dimer interface of Lactobacillus casei thymidylate synthase: crystal structure of the T155C/E188C/C244T mutant. Protein Sci. 1999 Apr; 8(4):930-3. PMID: 10211840; PMCID: PMC2144305.
      64. Gu XR, Gustafsson C, Ku J, Yu M, Santi DV. Identification of the 16S rRNA m5C967 methyltransferase from Escherichia coli. Biochemistry. 1999 Mar 30; 38(13):4053-7. PMID: 10194318.
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      65. Prasanna V, Gopal B, Murthy MR, Santi DV, Balaram P. Effect of amino acid substitutions at the subunit interface on the stability and aggregation properties of a dimeric protein: role of Arg 178 and Arg 218 at the Dimer interface of thymidylate synthase. Proteins. 1999 Feb 15; 34(3):356-68. PMID: 10024022.
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      66. Stout TJ, Tondi D, Rinaldi M, Barlocco D, Pecorari P, Santi DV, Kuntz ID, Stroud RM, Shoichet BK, Costi MP. Structure-based design of inhibitors specific for bacterial thymidylate synthase. Biochemistry. 1999 Feb 2; 38(5):1607-17. PMID: 9931028.
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      67. Liu Y, Barrett JE, Schultz PG, Santi DV. Tyrosine 146 of thymidylate synthase assists proton abstraction from the 5-position of 2'-deoxyuridine 5'-monophosphate. Biochemistry. 1999 Jan 12; 38(2):848-52. PMID: 9888826.
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      68. Liu Y, Santi DV. A continuous spectrophotometric assay for thymidine and deoxycytidine kinases. Anal Biochem. 1998 Nov 15; 264(2):259-62. PMID: 9866691.
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      69. Huang L, Ku J, Pookanjanatavip M, Gu X, Wang D, Greene PJ, Santi DV. Identification of two Escherichia coli pseudouridine synthases that show multisite specificity for 23S RNA. Biochemistry. 1998 Nov 10; 37(45):15951-7. PMID: 9843401.
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      70. Stout TJ, Schellenberger U, Santi DV, Stroud RM. Crystal structures of a unique thermal-stable thymidylate synthase from Bacillus subtilis. Biochemistry. 1998 Oct 20; 37(42):14736-47. PMID: 9778348.
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      71. Chiericatti G, Santi DV. Aspartate 221 of thymidylate synthase is involved in folate cofactor binding and in catalysis. Biochemistry. 1998 Jun 23; 37(25):9038-42. PMID: 9636048.
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      72. Birdsall DL, Huang W, Santi DV, Stroud RM, Finer-Moore J. The separate effects of E60Q in Lactobacillus casei thymidylate synthase delineate between mechanisms for formation of intermediates in catalysis. Protein Eng. 1998 Mar; 11(3):171-83. PMID: 9613841.
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      73. Finer-Moore JS, Liu L, Birdsall DL, Brem R, Apfeld J, Santi DV, Stroud RM. Contributions of orientation and hydrogen bonding to catalysis in Asn229 mutants of thymidylate synthase. J Mol Biol. 1998 Feb 13; 276(1):113-29. PMID: 9514716.
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      74. Kealey JT, Liu L, Santi DV, Betlach MC, Barr PJ. Production of a polyketide natural product in nonpolyketide-producing prokaryotic and eukaryotic hosts. Proc Natl Acad Sci U S A. 1998 Jan 20; 95(2):505-9. PMID: 9435221; PMCID: PMC18449.
      75. Huang L, Pookanjanatavip M, Gu X, Santi DV. A conserved aspartate of tRNA pseudouridine synthase is essential for activity and a probable nucleophilic catalyst. Biochemistry. 1998 Jan 6; 37(1):344-51. PMID: 9425056.
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      76. Gu X, Yu M, Ivanetich KM, Santi DV. Molecular recognition of tRNA by tRNA pseudouridine 55 synthase. Biochemistry. 1998 Jan 6; 37(1):339-43. PMID: 9425055.
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      77. Agarwalla S, LaPorte S, Liu L, Finer-Moore J, Stroud RM, Santi DV. A novel dCMP methylase by engineering thymidylate synthase. Biochemistry. 1997 Dec 16; 36(50):15909-17. PMID: 9398324.
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      78. Sirawaraporn W, Yongkiettrakul S, Sirawaraporn R, Yuthavong Y, Santi DV. Plasmodium falciparum: asparagine mutant at residue 108 of dihydrofolate reductase is an optimal antifolate-resistant single mutant. Exp Parasitol. 1997 Nov; 87(3):245-52. PMID: 9371090.
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      79. Gschwend DA, Sirawaraporn W, Santi DV, Kuntz ID. Specificity in structure-based drug design: identification of a novel, selective inhibitor of Pneumocystis carinii dihydrofolate reductase. Proteins. 1997 Sep; 29(1):59-67. PMID: 9294866.
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      80. Trujillo M, Duncan R, Santi DV. Construction of a homodimeric dihydrofolate reductase-thymidylate synthase bifunctional enzyme. Protein Eng. 1997 May; 10(5):567-73. PMID: 9215575.
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      81. Yao LJ, James TL, Kealey JT, Santi DV, Schmitz U. The dynamic NMR structure of the T psi C-loop: implications for the specificity of tRNA methylation. J Biomol NMR. 1997 Apr; 9(3):229-44. PMID: 9204554.
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      82. Ku J, Mirmira RG, Liu L, Santi DV. Expression of a functional non-ribosomal peptide synthetase module in Escherichia coli by coexpression with a phosphopantetheinyl transferase. Chem Biol. 1997 Mar; 4(3):203-7. PMID: 9115412.
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      83. Huang W, Santi DV. Active site general catalysts are not necessary for some proton transfer reactions of thymidylate synthase. Biochemistry. 1997 Feb 18; 36(7):1869-73. PMID: 9048572.
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      84. Sirawaraporn W, Sathitkul T, Sirawaraporn R, Yuthavong Y, Santi DV. Antifolate-resistant mutants of Plasmodium falciparum dihydrofolate reductase. Proc Natl Acad Sci U S A. 1997 Feb 18; 94(4):1124-9. PMID: 9037017; PMCID: PMC19755.
      85. Prapunwattana P, Sirawaraporn W, Yuthavong Y, Santi DV. Chemical synthesis of the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene. Mol Biochem Parasitol. 1996 Dec 2; 83(1):93-106. PMID: 9010845.
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      86. Gustafsson C, Reid R, Greene PJ, Santi DV. Identification of new RNA modifying enzymes by iterative genome search using known modifying enzymes as probes. Nucleic Acids Res. 1996 Oct 1; 24(19):3756-62. PMID: 8871555; PMCID: PMC146159.
      87. Gu X, Ivanetich KM, Santi DV. Recognition of the T-arm of tRNA by tRNA (m5U54)-methyltransferase is not sequence specific. Biochemistry. 1996 Sep 10; 35(36):11652-9. PMID: 8794745.
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      88. Yu PL, Zhao J, Yu M, Reid R, Santi DV. Functional expression of the dihydrofolate reductase domain of Leishmania major dihydrofolate reductase-thymidylate synthase bifunctional protein. Protein Expr Purif. 1996 Aug; 8(1):23-7. PMID: 8812831.
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      89. Gokhale RS, Agarwalla S, Santi DV, Balaram P. Covalent reinforcement of a fragile region in the dimeric enzyme thymidylate synthase stabilizes the protein against chaotrope-induced unfolding. Biochemistry. 1996 Jun 4; 35(22):7150-8. PMID: 8679542.
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      90. Trujillo M, Donald RG, Roos DS, Greene PJ, Santi DV. Heterologous expression and characterization of the bifunctional dihydrofolate reductase-thymidylate synthase enzyme of Toxoplasma gondii. Biochemistry. 1996 May 21; 35(20):6366-74. PMID: 8639582.
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      91. Finer-Moore JS, Liu L, Schafmeister CE, Birdsall DL, Mau T, Santi DV, Stroud RM. Partitioning roles of side chains in affinity, orientation, and catalysis with structures for mutant complexes: asparagine-229 in thymidylate synthase. Biochemistry. 1996 Apr 23; 35(16):5125-36. PMID: 8611496.
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      92. Costi PM, Liu L, Finer-Moore JS, Stroud RM, Santi DV. Asparagine 229 mutants of thymidylate synthase catalyze the methylation of 3-methyl-2'-deoxyuridine 5'-monophosphate. Biochemistry. 1996 Apr 2; 35(13):3944-9. PMID: 8672425.
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      93. Gu X, Matsuda A, Ivanetich KM, Santi DV. Interaction of tRNA (uracil-5-)-methyltransferase with NO2Ura-tRNA. Nucleic Acids Res. 1996 Mar 15; 24(6):1059-64. PMID: 8604339; PMCID: PMC145746.
      94. Reche P, Arrebola R, Santi DV, Gonzalez-Pacanowska D, Ruiz-Perez LM. Expression and characterization of the Trypanosoma cruzi dihydrofolate reductase domain. Mol Biochem Parasitol. 1996 Feb-Mar; 76(1-2):175-85. PMID: 8920005.
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      95. Agarwalla S, Gokhale RS, Santi DV, Balaram P. Covalent tethering of the dimer interface annuls aggregation in thymidylate synthase. Protein Sci. 1996 Feb; 5(2):270-7. PMID: 8745405; PMCID: PMC2143334.
      96. Ivanetich KM, Santi DV. Preparation of equimolar mixtures of peptides by adjustment of activated amino acid concentrations. Methods Enzymol. 1996; 267:247-60. PMID: 8743321.
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      97. Finer-Moore JS, Fauman EB, Morse RJ, Santi DV, Stroud RM. Contribution of a salt bridge to binding affinity and dUMP orientation to catalytic rate: mutation of a substrate-binding arginine in thymidylate synthase. Protein Eng. 1996 Jan; 9(1):69-75. PMID: 9053905.
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      98. Schiffer CA, Clifton IJ, Davisson VJ, Santi DV, Stroud RM. Crystal structure of human thymidylate synthase: a structural mechanism for guiding substrates into the active site. Biochemistry. 1995 Dec 19; 34(50):16279-87. PMID: 8845352.
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      99. Gamarro F, Yu PL, Zhao J, Edman U, Greene PJ, Santi D. Addendum to "Trypanosoma brucei dihydrofolate reductase-thymidylate synthase: gene isolation and expression and characterization of the enzyme" [Mol. Biochem. Parasitol. 72 (1995) 11-22]. Mol Biochem Parasitol. 1995 Dec; 75(1):127. PMID: 8720183.
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      100. Ono A, Matsuda A, Zhao J, Santi DV. The synthesis of blocked triplet-phosphoramidites and their use in mutagenesis. Nucleic Acids Res. 1995 Nov 25; 23(22):4677-82. PMID: 8524660; PMCID: PMC307443.
      101. Kealey JT, Eckstein J, Santi DV. Role of the conserved tryptophan 82 of Lactobacillus casei thymidylate synthase. Chem Biol. 1995 Sep; 2(9):609-14. PMID: 9383465.
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      102. García-Fuentes L, Reche P, López-Mayorga O, Santi DV, González-Pacanowska D, Barón C. Thermodynamic analysis of the binding of 5-fluoro-2'-deoxyuridine 5'-monophosphate to thymidylate synthase over a range of temperatures. Eur J Biochem. 1995 Sep 1; 232(2):641-5. PMID: 7556218.
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      103. Schellenberger U, Livi LL, Santi DV. Cloning, expression, purification, and characterization of 2'-deoxyuridylate hydroxymethylase from phage SPO1. Protein Expr Purif. 1995 Aug; 6(4):423-30. PMID: 8527927.
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      104. Malcolm BA, Lowe C, Shechosky S, McKay RT, Yang CC, Shah VJ, Simon RJ, Vederas JC, Santi DV. Peptide aldehyde inhibitors of hepatitis A virus 3C proteinase. Biochemistry. 1995 Jun 27; 34(25):8172-9. PMID: 7794931.
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      105. Gamarro F, Yu PL, Zhao J, Edman U, Greene PJ, Santi D. Trypanosoma brucei dihydrofolate reductase-thymidylate synthase: gene isolation and expression and characterization of the enzyme. Mol Biochem Parasitol. 1995 Jun; 72(1-2):11-22. PMID: 8538681.
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      106. Marlowe CK, Selassie CD, Santi DV. Quantitative structure-activity relationships of the inhibition of Pneumocystis carinii dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(X-phenyl)-s-triazines. J Med Chem. 1995 Mar 17; 38(6):967-72. PMID: 7699713.
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      107. Kealey JT, Santi DV. Stereochemistry of tRNA(m5U54)-methyltransferase catalysis: 19F NMR spectroscopy of an enzyme-FUraRNA covalent complex. Biochemistry. 1995 Feb 28; 34(8):2441-6. PMID: 7532997.
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      108. Carreras CW, Santi DV. The catalytic mechanism and structure of thymidylate synthase. Annu Rev Biochem. 1995; 64:721-62. PMID: 7574499.
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      109. Eckstein JW, Foster PG, Finer-Moore J, Wataya Y, Santi DV. Mechanism-based inhibition of thymidylate synthase by 5-(trifluoromethyl)-2'-deoxyuridine 5'-monophosphate. Biochemistry. 1994 Dec 20; 33(50):15086-94. PMID: 7999767.
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      110. Huang W, Santi DV. Isolation of a covalent steady-state intermediate in glutamate 60 mutants of thymidylate synthase. J Biol Chem. 1994 Dec 16; 269(50):31327-9. PMID: 7989294.
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      111. Livi LL, Edman U, Schneider GP, Greene PJ, Santi DV. Cloning, expression and characterization of thymidylate synthase from Cryptococcus neoformans. Gene. 1994 Dec 15; 150(2):221-6. PMID: 7821787.
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      112. Davisson VJ, Sirawaraporn W, Santi DV. Expression of human thymidylate synthase in Escherichia coli. J Biol Chem. 1994 Dec 2; 269(48):30740. PMID: 7982996.
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      113. Liu L, Santi DV. 5-Fluoro-2'-deoxycytidine 5'-monophosphate is a mechanism-based inhibitor of thymidylate synthase. Biochim Biophys Acta. 1994 Nov 16; 1209(1):89-94. PMID: 7947987.
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      114. Greene PJ, Yu PL, Zhao J, Schiffer CA, Santi D. Expression, purification, and characterization of thymidylate synthase from Lactococcus lactis. Protein Sci. 1994 Jul; 3(7):1114-6. PMID: 7920258; PMCID: PMC2142890.
      115. Reche P, Arrebola R, Olmo A, Santi DV, Gonzalez-Pacanowska D, Ruiz-Perez LM. Cloning and expression of the dihydrofolate reductase-thymidylate synthase gene from Trypanosoma cruzi. Mol Biochem Parasitol. 1994 Jun; 65(2):247-58. PMID: 7969266.
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      116. Schellenberger U, Balaram P, Francis VS, Shoichet BK, Santi DV. Partial restoration of activity to Lactobacillus casei thymidylate synthase following inactivation by domain deletion. Biochemistry. 1994 May 10; 33(18):5623-9. PMID: 8180187.
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      117. Huang W, Santi DV. Identification of biologically active mutants by combinatorial cassette mutagenesis: exclusion of wild-type codon from degenerate codons. Anal Biochem. 1994 May 1; 218(2):454-7. PMID: 8074306.
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      118. Carreras CW, Costi PM, Santi DV. Heterodimeric thymidylate synthases with C-terminal deletion on one subunit. J Biol Chem. 1994 Apr 29; 269(17):12444-6. PMID: 8175650.
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      119. Arrebola R, Olmo A, Reche P, Garvey EP, Santi DV, Ruiz-Perez LM, Gonzalez-Pacanowska D. Isolation and characterization of a mutant dihydrofolate reductase-thymidylate synthase from methotrexate-resistant Leishmania cells. J Biol Chem. 1994 Apr 8; 269(14):10590-6. PMID: 8144647.
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      120. Kealey JT, Santi DV. High-level expression and rapid purification of tRNA (m5U54)-methyltransferase. Protein Expr Purif. 1994 Apr; 5(2):149-52. PMID: 8054847.
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      121. Carreras CW, Naber N, Cooke R, Santi DV. A C-terminal conformational equilibrium in thymidylate synthase observed by electron paramagnetic resonance spectroscopy. Biochemistry. 1994 Mar 1; 33(8):2071-7. PMID: 8117663.
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      122. Gu X, Ofengand J, Santi DV. In vitro methylation of Escherichia coli 16S rRNA by tRNA (m5U54)-methyltransferase. Biochemistry. 1994 Mar 1; 33(8):2255-61. PMID: 8117682.
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      123. Gokhale RS, Agarwalla S, Francis VS, Santi DV, Balaram P. Thermal stabilization of thymidylate synthase by engineering two disulfide bridges across the dimer interface. J Mol Biol. 1994 Jan 7; 235(1):89-94. PMID: 7904654.
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      124. Kealey JT, Gu X, Santi DV. Enzymatic mechanism of tRNA (m5U54)methyltransferase. Biochimie. 1994; 76(12):1133-42. PMID: 7748948.
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      125. Santi DV, Ouyang TM, Tan AK, Gregory DH, Scanlan T, Carreras CW. Interaction of thymidylate synthase with pyridoxal 5'-phosphate as studied by UV/visible difference spectroscopy and molecular modeling. Biochemistry. 1993 Nov 9; 32(44):11819-24. PMID: 8218253.
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      126. Sirawaraporn W, Prapunwattana P, Sirawaraporn R, Yuthavong Y, Santi DV. The dihydrofolate reductase domain of Plasmodium falciparum thymidylate synthase-dihydrofolate reductase. Gene synthesis, expression, and anti-folate-resistant mutants. J Biol Chem. 1993 Oct 15; 268(29):21637-44. PMID: 8408015.
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      127. Greene PJ, Maley F, Pedersen-Lane J, Santi DV. Catalytically active cross-species heterodimers of thymidylate synthase. Biochemistry. 1993 Oct 5; 32(39):10283-8. PMID: 8399170.
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      128. Liu L, Santi DV. Asparagine 229 in thymidylate synthase contributes to, but is not essential for, catalysis. Proc Natl Acad Sci U S A. 1993 Sep 15; 90(18):8604-8. PMID: 8378336; PMCID: PMC47406.
      129. Liu L, Santi DV. Exclusion of 2'-deoxycytidine 5'-monophosphate by asparagine 229 of thymidylate synthase. Biochemistry. 1993 Sep 14; 32(36):9263-7. PMID: 8369294.
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      130. Margosiak SA, Appleman JR, Santi DV, Blakley RL. Dihydrofolate reductase from the pathogenic fungus Pneumocystis carinii: catalytic properties and interaction with antifolates. Arch Biochem Biophys. 1993 Sep; 305(2):499-508. PMID: 8373187.
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      131. Finer-Moore J, Fauman EB, Foster PG, Perry KM, Santi DV, Stroud RM. Refined structures of substrate-bound and phosphate-bound thymidylate synthase from Lactobacillus casei. J Mol Biol. 1993 Aug 20; 232(4):1101-16. PMID: 8371269.
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      132. Perry KM, Carreras CW, Chang LC, Santi DV, Stroud RM. Structures of thymidylate synthase with a C-terminal deletion: role of the C-terminus in alignment of 2'-deoxyuridine 5'-monophosphate and 5,10-methylenetetrahydrofolate. Biochemistry. 1993 Jul 20; 32(28):7116-25. PMID: 8343503.
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      133. Sirawaraporn W, Cao M, Santi DV, Edman JC. Cloning, expression, and characterization of Cryptococcus neoformans dihydrofolate reductase. J Biol Chem. 1993 Apr 25; 268(12):8888-92. PMID: 8473332.
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      134. Shoichet BK, Stroud RM, Santi DV, Kuntz ID, Perry KM. Structure-based discovery of inhibitors of thymidylate synthase. Science. 1993 Mar 5; 259(5100):1445-50. PMID: 8451640.
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      135. Santi DV. Mutagenesis, structure and function studies of thymidylate synthase. Nucleic Acids Symp Ser. 1993; (29):103-5. PMID: 8247725.
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      136. Pookanjanatavip M, Yuthavong Y, Greene PJ, Santi DV. Subunit complementation of thymidylate synthase. Biochemistry. 1992 Oct 27; 31(42):10303-9. PMID: 1420149.
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      137. Gu X, Santi DV. Covalent adducts between tRNA (m5U54)-methyltransferase and RNA substrates. Biochemistry. 1992 Oct 27; 31(42):10295-302. PMID: 1420148.
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      138. Kealey JT, Santi DV. Purification methods for recombinant Lactobacillus casei thymidylate synthase and mutants: a general, automated procedure. Protein Expr Purif. 1992 Oct; 3(5):380-5. PMID: 1333860.
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      139. Climie SC, Carreras CW, Santi DV. Complete replacement set of amino acids at the C-terminus of thymidylate synthase: quantitative structure-activity relationship of mutants of an enzyme. Biochemistry. 1992 Jul 7; 31(26):6032-8. PMID: 1627545.
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      140. Carreras CW, Climie SC, Santi DV. Thymidylate synthase with a C-terminal deletion catalyzes partial reactions but is unable to catalyze thymidylate formation. Biochemistry. 1992 Jul 7; 31(26):6038-44. PMID: 1627546.
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      141. Liu L, Santi DV. Mutation of asparagine 229 to aspartate in thymidylate synthase converts the enzyme to a deoxycytidylate methylase. Biochemistry. 1992 Jun 9; 31(22):5100-4. PMID: 1606134.
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      142. Perry KM, Pookanjanatavip M, Zhao J, Santi DV, Stroud RM. Reversible dissociation and unfolding of the dimeric protein thymidylate synthase. Protein Sci. 1992 Jun; 1(6):796-800. PMID: 1304920; PMCID: PMC2142238.
      143. Zuckermann RN, Kerr JM, Siani MA, Banville SC, Santi DV. Identification of highest-affinity ligands by affinity selection from equimolar peptide mixtures generated by robotic synthesis. Proc Natl Acad Sci U S A. 1992 May 15; 89(10):4505-9. PMID: 1584783; PMCID: PMC49111.
      144. Ivanetich KM, Santi DV. 5,6-dihydropyrimidine adducts in the reactions and interactions of pyrimidines with proteins. Prog Nucleic Acid Res Mol Biol. 1992; 42:127-56. PMID: 1574586.
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      145. Petithory JR, Masiarz FR, Kirsch JF, Santi DV, Malcolm BA. A rapid method for determination of endoproteinase substrate specificity: specificity of the 3C proteinase from hepatitis A virus. Proc Natl Acad Sci U S A. 1991 Dec 15; 88(24):11510-4. PMID: 1662396; PMCID: PMC53165.
      146. Kealey JT, Lee S, Floss HG, Santi DV. Stereochemistry of methyl transfer catalyzed by tRNA (m5U54)-methyltransferase--evidence for a single displacement mechanism. Nucleic Acids Res. 1991 Dec 11; 19(23):6465-8. PMID: 1754383; PMCID: PMC329199.
      147. Kealey JT, Santi DV. Identification of the catalytic nucleophile of tRNA (m5U54)methyltransferase. Biochemistry. 1991 Oct 8; 30(40):9724-8. PMID: 1911760.
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      148. Santi DV, Edman U, Minkin S, Greene PJ. Purification and characterization of recombinant Pneumocystis carinii thymidylate synthase. Protein Expr Purif. 1991 Oct-Dec; 2(5-6):350-4. PMID: 1821808.
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      149. Sirawaraporn W, Edman JC, Santi DV. Purification and properties of recombinant Pneumocystis carinii dihydrofolate reductase. Protein Expr Purif. 1991 Oct-Dec; 2(5-6):313-6. PMID: 1821803.
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      150. Ivanetich KM, Akiyama J, Santi DV, Reschenberg M. Automated purification of synthetic oligonucleotides. Biotechniques. 1991 Jun; 10(6):704-8. PMID: 1878202.
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      151. Schiffer CA, Davisson VJ, Santi DV, Stroud RM. Crystallization of human thymidylate synthase. J Mol Biol. 1991 May 20; 219(2):161-3. PMID: 2038053.
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      152. Gu XR, Santi DV. The T-arm of tRNA is a substrate for tRNA (m5U54)-methyltransferase. Biochemistry. 1991 Mar 26; 30(12):2999-3002. PMID: 2007136.
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      153. Gu X, Santi DV. Affinity chromatography of Escherichia coli (m5U54)-methyltransferase on tRNA-agarose. Protein Expr Purif. 1991 Feb; 2(1):66-8. PMID: 1821774.
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      154. Sirawaraporn W, Sirawaraporn R, Chanpongsri A, Jacobs WR, Santi DV. Purification and characterization of dihydrofolate reductase from wild-type and trimethoprim-resistant Mycobacterium smegmatis. Exp Parasitol. 1991 Feb; 72(2):184-90. PMID: 2009922.
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      155. Ho DK, Wu JC, Santi DV, Floss HG. Stereochemical studies of the C-methylation of deoxycytidine catalyzed by HhaI methylase and the N-methylation of deoxyadenosine catalyzed by EcoRI methylase. Arch Biochem Biophys. 1991 Feb 1; 284(2):264-9. PMID: 1989510.
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      156. Sirawaraporn W, Sirawaraporn R, Cowman AF, Yuthavong Y, Santi DV. Heterologous expression of active thymidylate synthase-dihydrofolate reductase from Plasmodium falciparum. Biochemistry. 1990 Dec 4; 29(48):10779-85. PMID: 2176883.
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      157. Climie S, Ruiz-Perez L, Gonzalez-Pacanowska D, Prapunwattana P, Cho SW, Stroud R, Santi DV. Saturation site-directed mutagenesis of thymidylate synthase. J Biol Chem. 1990 Nov 5; 265(31):18776-9. PMID: 2229040.
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      158. Bathurst IC, Moen LK, Lujan MA, Gibson HL, Feucht PH, Pichuantes S, Craik CS, Santi DV, Barr PJ. Characterization of the human immunodeficiency virus type-1 reverse transcriptase enzyme produced in yeast. Biochem Biophys Res Commun. 1990 Sep 14; 171(2):589-95. PMID: 1698361.
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      159. Gu XR, Santi DV. High-level expression of Escherichia coli tRNA (m5U54)-methyltransferase. DNA Cell Biol. 1990 May; 9(4):273-8. PMID: 2190591.
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      160. Santi DV, Pinter K, Kealey J, Davisson VJ. Site-directed mutagenesis of arginine 179 of thymidylate synthase. A nonessential substrate-binding residue. J Biol Chem. 1990 Apr 25; 265(12):6770-5. PMID: 2182628.
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      161. Ivanetich KM, Santi DV. Bifunctional thymidylate synthase-dihydrofolate reductase in protozoa. FASEB J. 1990 Apr 1; 4(6):1591-7. PMID: 2180768.
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      162. Ivanetich KM, Santi DV. Thymidylate synthase-dihydrofolate reductase in protozoa. Exp Parasitol. 1990 Apr; 70(3):367-71. PMID: 2178951.
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      163. Climie S, Santi DV. Chemical synthesis of the thymidylate synthase gene. Proc Natl Acad Sci U S A. 1990 Jan; 87(2):633-7. PMID: 2153960; PMCID: PMC53319.
      164. Subramaniam R, Wang Y, Mathews CK, Santi DV. On the inhibition of deoxycytidylate hydroxymethylase by 5-fluoro-2'-deoxycytidine 5'-monophosphate. Arch Biochem Biophys. 1989 Nov 15; 275(1):11-5. PMID: 2684015.
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      165. Edman JC, Edman U, Cao M, Lundgren B, Kovacs JA, Santi DV. Isolation and expression of the Pneumocystis carinii dihydrofolate reductase gene. Proc Natl Acad Sci U S A. 1989 Nov; 86(22):8625-9. PMID: 2682653; PMCID: PMC298340.
      166. Sowdhamini R, Srinivasan N, Shoichet B, Santi DV, Ramakrishnan C, Balaram P. Stereochemical modeling of disulfide bridges. Criteria for introduction into proteins by site-directed mutagenesis. Protein Eng. 1989 Nov; 3(2):95-103. PMID: 2594728.
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      167. Edman U, Edman JC, Lundgren B, Santi DV. Isolation and expression of the Pneumocystis carinii thymidylate synthase gene. Proc Natl Acad Sci U S A. 1989 Sep; 86(17):6503-7. PMID: 2671992; PMCID: PMC297872.
      168. Davisson VJ, Sirawaraporn W, Santi DV. Expression of human thymidylate synthase in Escherichia coli. J Biol Chem. 1989 Jun 5; 264(16):9145-8. PMID: 2656695.
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      169. Hightower RC, Santi DV. Migration properties of circular DNAs using orthogonal-field-alternation gel electrophoresis. Electrophoresis. 1989 May-Jun; 10(5-6):283-90. PMID: 2670543.
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      170. Hightower RC, Bliska JB, Cozzarelli NR, Santi DV. Analysis of amplified DNAs from drug-resistant Leishmania by orthogonal-field-alternation gel electrophoresis. The effect of size and topology on mobility. J Biol Chem. 1989 Feb 15; 264(5):2979-84. PMID: 2536730.
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      171. Ivanetich KM, Santi DV. Biomedical science and the third world. Under the volcano. Recent studies on thymidylate synthase. Ann N Y Acad Sci. 1989; 569:201-10. PMID: 2698088.
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      172. Edman JC, Kovacs JA, Masur H, Santi DV, Elwood HJ, Sogin ML. Ribosomal RNA genes of Pneumocystis carinii. J Protozool. 1989 Jan-Feb; 36(1):18S-20S. PMID: 2540326.
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      173. Hochhaus G, Patthy A, Schwietert R, Santi DV, Sadée W. [Biocytin13]dynorphin A 1-13 amide: a potential probe for the kappa-opioid receptor. Pharm Res. 1988 Dec; 5(12):790-4. PMID: 2907785.
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      174. Hightower RC, Ruiz-Perez LM, Wong ML, Santi DV. Extrachromosomal elements in the lower eukaryote Leishmania. J Biol Chem. 1988 Nov 15; 263(32):16970-6. PMID: 3182826.
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      175. Sirawaraporn W, Sertsrivanich R, Booth RG, Hansch C, Neal RA, Santi DV. Selective inhibition of Leishmania dihydrofolate reductase and Leishmania growth by 5-benzyl-2,4-diaminopyrimidines. Mol Biochem Parasitol. 1988 Oct; 31(1):79-85. PMID: 3185614.
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      176. Edman JC, Kovacs JA, Masur H, Santi DV, Elwood HJ, Sogin ML. Ribosomal RNA sequence shows Pneumocystis carinii to be a member of the fungi. Nature. 1988 Aug 11; 334(6182):519-22. PMID: 2970013.
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      177. Osterman DG, DePillis GD, Wu JC, Matsuda A, Santi DV. 5-Fluorocytosine in DNA is a mechanism-based inhibitor of HhaI methylase. Biochemistry. 1988 Jul 12; 27(14):5204-10. PMID: 3167042.
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      178. Pogolotti AL, Ono A, Subramaniam R, Santi DV. On the mechanism of DNA-adenine methylase. J Biol Chem. 1988 Jun 5; 263(16):7461-4. PMID: 3259576.
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      179. Grumont R, Sirawaraporn W, Santi DV. Heterologous expression of the bifunctional thymidylate synthase-dihydrofolate reductase from Leishmania major. Biochemistry. 1988 May 17; 27(10):3776-84. PMID: 2841973.
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      180. Pinter K, Davisson VJ, Santi DV. Cloning, sequencing, and expression of the Lactobacillus casei thymidylate synthase gene. DNA. 1988 May; 7(4):235-41. PMID: 2840247.
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      181. Wu JC, Santi DV. High level expression and purification of HhaI methyltransferase. Nucleic Acids Res. 1988 Jan 25; 16(2):703-17. PMID: 3340551; PMCID: PMC334686.
      182. Ivanetich KM, Santi DV. Thymidylate synthase and fluorouracil. Adv Exp Med Biol. 1988; 244:113-24. PMID: 3150251.
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      183. Santi DV, Hardy LW. Catalytic mechanism and inhibition of tRNA (uracil-5-)methyltransferase: evidence for covalent catalysis. Biochemistry. 1987 Dec 29; 26(26):8599-606. PMID: 3327525.
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      184. Santi DV, McHenry CS, Raines RT, Ivanetich KM. Kinetics and thermodynamics of the interaction of 5-fluoro-2'-deoxyuridylate with thymidylate synthase. Biochemistry. 1987 Dec 29; 26(26):8606-13. PMID: 3126806.
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      185. Hightower RC, Metge DW, Santi DV. Plasmid migration using orthogonal-field-alternation gel electrophoresis. Nucleic Acids Res. 1987 Oct 26; 15(20):8387-98. PMID: 2823228; PMCID: PMC306366.
      186. Hightower RC, Wong ML, Ruiz-Perez L, Santi DV. Electron microscopy of amplified DNA forms in antifolate-resistant Leishmania. J Biol Chem. 1987 Oct 25; 262(30):14618-24. PMID: 2822697.
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      187. Santi DV, Nolan P, Shane B. Folylpolyglutamates in Leishmania major. Biochem Biophys Res Commun. 1987 Aug 14; 146(3):1089-92. PMID: 3619916.
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      188. Garvey EP, Santi DV. A stable binary complex between Leishmania major thymidylate synthase and the substrate deoxyuridylate. A slow-binding interaction. J Biol Chem. 1987 Jul 5; 262(19):9068-74. PMID: 3597407.
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      189. Booth RG, Selassie CD, Hansch C, Santi DV. Quantitative structure-activity relationship of triazine-antifolate inhibition of Leishmania dihydrofolate reductase and cell growth. J Med Chem. 1987 Jul; 30(7):1218-24. PMID: 3599028.
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      190. Wu JC, Santi DV. Kinetic and catalytic mechanism of HhaI methyltransferase. J Biol Chem. 1987 Apr 5; 262(10):4778-86. PMID: 3558369.
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      191. Hardy LW, Finer-Moore JS, Montfort WR, Jones MO, Santi DV, Stroud RM. Atomic structure of thymidylate synthase: target for rational drug design. Science. 1987 Jan 23; 235(4787):448-55. PMID: 3099389.
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      192. Garvey EP, Santi DV. Stable amplified DNA in drug-resistant Leishmania exists as extrachromosomal circles. Science. 1986 Aug 1; 233(4763):535-40. PMID: 3726545.
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      193. Grumont R, Washtien WL, Caput D, Santi DV. Bifunctional thymidylate synthase-dihydrofolate reductase from Leishmania tropica: sequence homology with the corresponding monofunctional proteins. Proc Natl Acad Sci U S A. 1986 Aug; 83(15):5387-91. PMID: 3461439; PMCID: PMC386291.
      194. Pogolotti AL, Danenberg PV, Santi DV. Kinetics and mechanism of interaction of 10-propargyl-5,8-dideazafolate with thymidylate synthase. J Med Chem. 1986 Apr; 29(4):478-82. PMID: 3754285.
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      195. Santi DV. The mechanism and structure of thymidylate synthetase. Nucleic Acids Symp Ser. 1986; (17):125-6. PMID: 3562257.
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      196. Garvey EP, Santi DV. Limited proteolysis of the bifunctional thymidylate synthase-dihydrofolate reductase from Leishmania tropica. Proc Natl Acad Sci U S A. 1985 Nov; 82(21):7188-92. PMID: 3903747; PMCID: PMC390814.
      197. Garvey EP, Coderre JA, Santi DV. Selection and properties of Leishmania tropica resistant to 10-propargyl-5,8-dideazafolate, an inhibitor of thymidylate synthetase. Mol Biochem Parasitol. 1985 Oct; 17(1):79-91. PMID: 4058489.
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      198. Rainey P, Nolan PA, Townsend LB, Robins RK, Fox JJ, Secrist Iii JA, Santi DV. Inosine analogs as anti-leishmanial agents. Pharm Res. 1985 Sep; 2(5):217-20. PMID: 24272839.
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      199. Washtien WL, Grumont R, Santi DV. DNA amplification in antifolate-resistant Leishmania. The thymidylate synthase-dihydrofolate reductase gene and abundant mRNAs. J Biol Chem. 1985 Jul 5; 260(13):7809-12. PMID: 2409075.
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      200. Meek TD, Garvey EP, Santi DV. Purification and characterization of the bifunctional thymidylate synthetase-dihydrofolate reductase from methotrexate-resistant Leishmania tropica. Biochemistry. 1985 Jan 29; 24(3):678-86. PMID: 3922404.
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      201. Wu JC, Santi DV. On the mechanism and inhibition of DNA cytosine methyltransferases. Prog Clin Biol Res. 1985; 198:119-29. PMID: 4070306.
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      202. Golden JA, Sjoerdsma A, Santi DV. Pneumocystis carinii pneumonia treated with alpha-difluoromethylornithine. A prospective study among patients with the acquired immunodeficiency syndrome. West J Med. 1984 Nov; 141(5):613-23. PMID: 6440364; PMCID: PMC1011166.
      203. Santi DV, Norment A, Garrett CE. Covalent bond formation between a DNA-cytosine methyltransferase and DNA containing 5-azacytosine. Proc Natl Acad Sci U S A. 1984 Nov; 81(22):6993-7. PMID: 6209710; PMCID: PMC392062.
      204. Goldstein S, Pogolotti AL, Garvey EP, Santi DV. Interaction of N4-hydroxy-2'-deoxycytidylic acid with thymidylate synthetase. J Med Chem. 1984 Oct; 27(10):1259-62. PMID: 6434741.
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      205. Beverley SM, Coderre JA, Santi DV, Schimke RT. Unstable DNA amplifications in methotrexate-resistant Leishmania consist of extrachromosomal circles which relocalize during stabilization. Cell. 1984 Sep; 38(2):431-9. PMID: 6467372.
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      206. Kobayashi S, Hoshino T, Santi DV. Experimental combination chemotherapy with thymidylate synthetase and ribonucleotide reductase inhibitors. Pharm Res. 1984 Jul; 1(4):181-3. PMID: 24277289.
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      207. Rainey P, Santi DV. Formycin B resistance in Leishmania. Biochem Pharmacol. 1984 Apr 15; 33(8):1374-7. PMID: 6712743.
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      208. Garrett CE, Coderre JA, Meek TD, Garvey EP, Claman DM, Beverley SM, Santi DV. A bifunctional thymidylate synthetase-dihydrofolate reductase in protozoa. Mol Biochem Parasitol. 1984 Apr; 11:257-65. PMID: 6749182.
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      209. Prior JJ, Santi DV. On the mechanism of the acid-catalyzed hydrolysis of uridine to uracil. Evidence for 6-hydroxy-5,6-dihydrouridine intermediates. J Biol Chem. 1984 Feb 25; 259(4):2429-34. PMID: 6546573.
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      210. Prior JJ, Maley J, Santi DV. Adducts across the 5,6-double bond of pyrimidines. The mechanism of dehydration of 1-substituted uracil photohydrates. J Biol Chem. 1984 Feb 25; 259(4):2422-8. PMID: 6698974.
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      211. Barr PJ, Oppenheimer NJ, Santi DV. Thymidylate synthetase-catalyzed conversions of E-5-(2-bromovinyl)-2'-deoxyuridylate. J Biol Chem. 1983 Nov 25; 258(22):13627-31. PMID: 6417131.
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      212. Coderre JA, Santi DV, Matsuda A, Watanabe KA, Fox JJ. Mechanism of action of 2',5-difluoro-1-arabinosyluracil. J Med Chem. 1983 Aug; 26(8):1149-52. PMID: 6876083.
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      213. Berman JD, Rainey P, Santi DV. Metabolism of formycin B by Leishmania amastigotes in vitro. Comparative metabolism in infected and uninfected human macrophages. J Exp Med. 1983 Jul 1; 158(1):252-7. PMID: 6190980; PMCID: PMC2187072.
      214. Santi DV, Garrett CE, Barr PJ. On the mechanism of inhibition of DNA-cytosine methyltransferases by cytosine analogs. Cell. 1983 May; 33(1):9-10. PMID: 6205762.
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      215. Coderre JA, Beverley SM, Schimke RT, Santi DV. Overproduction of a bifunctional thymidylate synthetase-dihydrofolate reductase and DNA amplification in methotrexate-resistant Leishmania tropica. Proc Natl Acad Sci U S A. 1983 Apr; 80(8):2132-6. PMID: 6572966; PMCID: PMC393771.
      216. Barr PJ, Robins MJ, Santi DV. Reaction of 5-ethynyl-2'-deoxyuridylate with thiols and thymidylate synthetase. Biochemistry. 1983 Mar 29; 22(7):1696-703. PMID: 6405782.
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      217. Rainey P, Garrett CE, Santi DV. The metabolism and cytotoxic effects of Formycin B in Trypanosoma cruzi. Biochem Pharmacol. 1983 Feb 15; 32(4):749-52. PMID: 6338883.
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      218. Rainey P, Santi DV. Metabolism and mechanism of action of formycin B in Leishmania. Proc Natl Acad Sci U S A. 1983 Jan; 80(1):288-92. PMID: 6572004; PMCID: PMC393358.
      219. Bruice TW, Santi DV. Secondary alpha-hydrogen isotope effects on the interaction of 5-fluoro-2'-deoxyuridylate and 5,10-methylenetetrahydrofolate with thymidylate synthetase. Biochemistry. 1982 Dec 21; 21(26):6703-9. PMID: 7159556.
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      220. Newman EM, Santi DV. Metabolism and mechanism of action of 5-fluorodeoxycytidine. Proc Natl Acad Sci U S A. 1982 Nov; 79(21):6419-23. PMID: 6959127; PMCID: PMC347137.
      221. Pogolotti AL, Santi DV. High-pressure liquid chromatography--ultraviolet analysis of intracellular nucleotides. Anal Biochem. 1982 Nov 1; 126(2):335-45. PMID: 7158770.
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      222. Washtien WL, Santi DV. Mechanism of action of 5-nitro-2'-deoxyuridine. J Med Chem. 1982 Oct; 25(10):1252-5. PMID: 6183429.
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      223. Barr PJ, Nolan PA, Santi DV, Robins MJ. Inhibition of thymidylate synthetase by 5-alkynyl-2'-deoxyuridylates. J Med Chem. 1981 Dec; 24(12):1385-8. PMID: 6796687.
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      224. Nakayama C, Wataya Y, Santi DV, Saneyoshi M, Ueda T. Interaction of 1-(5-phospho-beta-D-arabinofuranosyl)-5-substituted-uracils with thymidylate synthetase: mechanism-based inhibition by 1-(5-phospho-beta-D-arabinosyl)-5-fluorouracil. J Med Chem. 1981 Oct; 24(10):1161-5. PMID: 7328576.
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      225. Pogolotti AL, Nolan PA, Santi DV. Methods for the complete analysis of 5-fluorouracil metabolites in cell extracts. Anal Biochem. 1981 Oct; 117(1):178-86. PMID: 6459042.
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      226. Nakayama C, Wataya Y, Meyer RB, Santi DV, Saneyoshi M, Ueda T. Thymidine phosphorylase. Substrate specificity for 5-substituted 2'-deoxyuridines. J Med Chem. 1980 Aug; 23(8):962-4. PMID: 7401121.
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      227. Wataya Y, Matsuda A, Santi DV. Interaction of thymidylate synthetase with 5-nitro-2'-deoxyuridylate. J Biol Chem. 1980 Jun 25; 255(12):5538-44. PMID: 6769917.
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      228. Kunitani MG, Santi DV. On the mechanism of 2'-deoxyuridylate hydroxymethylase. Biochemistry. 1980 Apr 1; 19(7):1271-5. PMID: 6770896.
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      229. Santi DV. Perspective on the design and biochemical pharmacology of inhibitors of thymidylate synthetase. J Med Chem. 1980 Feb; 23(2):103-11. PMID: 6987403.
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      230. Wataya Y, Kawada R, Itadani A, Hayatsu H, Bruice TW, Garrett C, Matsuda A, Santi DV. Use of alpha-secondary isotope effects in nucleophile-promoted reactions of pyrimidine derivatives; evidence for transient 5,6-dihydropyrimidine intermediates. Nucleic Acids Symp Ser. 1980; (8):s55-8. PMID: 7255197.
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      231. Bruice TW, Garrett C, Wataya Y, Santi DV. Use of secondary alpha-hydrogen isotope effects in reactions of pyrimidine nucleoside/nucleotide metabolism: thymidylate synthetase. Methods Enzymol. 1980; 64:125-35. PMID: 6768958.
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      232. Smith RA, Santi DV. Simultaneous measurement of charging levels of multiple aminoacyl-tRNAs. Anal Biochem. 1979 Nov 1; 99(2):372-8. PMID: 391096.
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      233. Garrett C, Santi DV. A rapid and sensitive high pressure liquid chromatography assay for deoxyribonucleoside triphosphates in cell extracts. Anal Biochem. 1979 Nov 1; 99(2):268-73. PMID: 517739.
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      234. Santi DV, Cunnion SO, Anderson RT, Webster RW. In vivo inhibitors of Escherichia coli phenylalanyl-tRNA synthetase. J Med Chem. 1979 Oct; 22(10):1260-3. PMID: 390149.
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      235. Washtien WL, Santi DV. Assay of intracellular free and macromolecular-bound metabolites of 5-fluorodeoxyuridine and 5-fluorouracil. Cancer Res. 1979 Sep; 39(9):3397-404. PMID: 157805.
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      236. Garrett C, Wataya Y, Santi DV. Thymidylate synthetase. Catalysis of dehalogenation of 5-bromo- and 5-iodo-2'-deoxyuridylate. Biochemistry. 1979 Jun 26; 18(13):2798-804. PMID: 476052.
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      237. Pogolotti AL, Weill C, Santi DV. Thymidylate synthetase catalyzed exchange of tritiumfrom [5-3H]-2'-deoxyuridylate for protons of water. Biochemistry. 1979 Jun 26; 18(13):2794-8. PMID: 113030.
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      238. Wataya Y, Matsuda A, Santi DV, Bergstrom DE, Ruth JL. trans-5-(3,3,3-Trifluoro-1-propenyl-)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase. J Med Chem. 1979 Apr; 22(4):339-40. PMID: 430474.
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      239. Santi DV, Washtien W, Pogolotti AL. Approaches for purification of the glucocorticoid receptor. Monogr Endocrinol. 1979; 12:109-22. PMID: 492170.
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      240. Matsuda A, Wataya Y, Santi DV. 5-Nitro-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase. Biochem Biophys Res Commun. 1978 Oct 16; 84(3):654-9. PMID: 102324.
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      241. Ullman B, Lee M, Martin DW, Santi DV. Cytotoxicity of 5-fluoro-2'-deoxyuridine: requirement for reduced folate cofactors and antagonism by methotrexate. Proc Natl Acad Sci U S A. 1978 Feb; 75(2):980-3. PMID: 147465; PMCID: PMC411383.
      242. Washtien W, Matsuda A, Wataya Y, Santi DV. Cytotoxicity of 5-nitro-2'-deoxyuridine by in vivo inhibition of thymidylate synthetase. Biochem Pharmacol. 1978; 27(22):2663-6. PMID: 215163.
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      243. Wataya Y, Santi DV, Hansch C. Inhibition of Lactobacillus casei thymidylate synthetase by 5-substituted 2'-deoxyuridylates. Preliminary quantitative structure-activity relationship. J Med Chem. 1977 Nov; 20(11):1469-73. PMID: 410930.
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      244. Wataya Y, Santi DV. A secondary isotope effect in the cysteine-Promoted dehalogenation of 5-bromo-2'-deoxyuridine. evidence for transient 5,6-dihydropyrimidine intermediates. J Am Chem Soc. 1977 Jun 22; 99(13):4534-6. PMID: 864127.
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      245. Garrett C, Pogolotti AL, Santi DV. Separation of 5-substituted 2'-deoxyuridines and deoxyuridylates by high-pressure anion-exchange liquid chromatography. Anal Biochem. 1977 May 1; 79(1-2):602-4. PMID: 869199.
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      246. Wataya Y, Santi DV. Active-site labeling of thymidylate synthetase with 5-fluoro-2'-deoxyuridylate. Methods Enzymol. 1977; 46:307-12. PMID: 909420.
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      247. Anderson RT, Santi DV. Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli B. Potent inhibition by analogues of N-benzyl-2-phenylethylamine. J Med Chem. 1976 Nov; 19(11):1270-5. PMID: 794470.
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      248. Santi DV, Webster RW. Phenylalanyl transfer ribonucleic acid synthetase from rat liver. Analysis of phenylalanine and adenosine 5'-triphosphate binding sites and comparison to the enzyme from Escherichia coli. J Med Chem. 1976 Nov; 19(11):1276-9. PMID: 794471.
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      249. James TL, Pogolotti AL, Ivanetich KM, Wataya Y, Lam SS, Santi DV. Thymidylate synthetase: fluorine-19 nmr characterization of the active site peptide covalently bound to 5-fluoro-2'-deoxyuridylate and 5,10-methylenetetrahydrofolate. Biochem Biophys Res Commun. 1976 Sep 20; 72(2):404-10. PMID: 825116.
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      250. Pogolotti AL, Ivanetich KM, Sommer H, Santi DV. Thymidylate synthetase: studies on peptide containing covalently bound 5-fluoro-2'-deoxyuridylate and 5,10-methylenetetrahydrofolate. Biochem Biophys Res Commun. 1976 Jun 7; 70(3):972-8. PMID: 820346.
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      251. Santi DV, Penã VA, Lam SS. On the structure of the cofactor in the complex formed with thymidylate synthetase, 5,10-methylenetetrahy-drofolate and 5-fluoro-2'-deoxyuridylate. Biochim Biophys Acta. 1976 Jun 7; 438(1):324-31. PMID: 938684.
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      252. Wataya Y, Santi DV. Thymidylate synthetase catalyzed dehalogenation of 5-bromo-and 5-iodo-2'-deoxyuridylate. Biochem Biophys Res Commun. 1975 Nov 17; 67(2):818-23. PMID: 812499.
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      253. Santi DV, Webster RW. The role of polyamines in the aminoacyl transfer ribonucleic acid synthetase reactions. Demonstration of the requirement for magnesium ion and a secondary stimulatory effect of spermine. J Biol Chem. 1975 May 25; 250(10):3874-7. PMID: 165187.
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      254. Danenberg PV, Santi DV. Inhibition of phenylalanyl-tRNA synthetase by aromatic guanidines and amidines. J Med Chem. 1975 May; 18(5):528-30. PMID: 1097688.
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      255. Baxter JD, Santi DV, Rousseau GG. A filter technique for measurement of steroid-receptor binding. Methods Enzymol. 1975; 36:234-9. PMID: 162980.
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      256. Sommer H, Santi DV. Purification and amino acid analysis of an active site peptide from thymidylate synthetase containing covalently bound 5-fluoro-2'-deoxyuridylate and methylenetetrahydrofolate. Biochem Biophys Res Commun. 1974 Apr 8; 57(3):689-95. PMID: 4275130.
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      257. McHenry CS, Santi DV. A sulfhydryl group is not the covalent catalyst in the thymidylate synthetase reaction. Biochem Biophys Res Commun. 1974 Mar 15; 57(1):204-8. PMID: 4275163.
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      258. Santi DV, Anderson RT. A deae-cellulose filter disk assay for aminoacyl-tRNA. Anal Biochem. 1974 Mar; 58(1):175-82. PMID: 4596570.
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      259. Santi DV, Cunnion SO. Macromolecular affinity labeling agents. Reaction of N-bromoacetylisoleucyl transfer ribonucleic acid with isoleucyl transfer ribonucleic acid synthetase. Biochemistry. 1974 Jan 29; 13(3):481-5. PMID: 4589311.
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      260. Santi DV, McHenry CS, Sommer H. Mechanism of interaction of thymidylate synthetase with 5-fluorodeoxyuridylate. Biochemistry. 1974 Jan 29; 13(3):471-81. PMID: 4203910.
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      261. Pogolotti AL, Santi DV. Model studies of the thymidylate synthetase reaction. Nucleophilic displacement of 5-p-nitrophenoxymethyluracils. Biochemistry. 1974 Jan 29; 13(3):456-66. PMID: 4810063.
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      262. Santi DV, McHenry CS, Perriard ER. A filter assay for thymidylate synthetase using 5-fluoro-2'-deoxyuridylate as an active site titrant. Biochemistry. 1974 Jan 29; 13(3):467-70. PMID: 4358948.
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      263. Santi DV, Webster RW, Cleland WW. Kinetics of aminoacyl-tRNA synthetases catalyzed ATP-PPi exchange. Methods Enzymol. 1974; 29:620-7. PMID: 4368856.
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      264. Santi DV, Cunnion SO. Peptidyl-tRNA analogs as affinity labeling agents. Methods Enzymol. 1974; 29:695-706. PMID: 4604890.
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      265. Sakai TT, Santi DV. Hydrolysis of hydroxybenzotrifluorides and fluorinated uracil derivatives. A general mechanism for carbon-fluorine bond labilization. J Med Chem. 1973 Oct; 16(10):1079-84. PMID: 4749467.
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      266. Santi DV, Brewer CF. Model studies of thymidylate synthetase. Intramolecular catalysis of 5-hydrogen exchange and 5-hydroxymethylation of 1-substituted uracils. Biochemistry. 1973 Jun 19; 12(13):2416-24. PMID: 4709938.
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      267. Santi DV, Sibley CH, Perriard ER, Tomkins GM, Baxter JD. A filter assay for steroid hormone receptors. Biochemistry. 1973 Jun 19; 12(13):2412-6. PMID: 4350952.
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      268. Failla D, Santi DV. A simple method for quantitating ligands covalently bound to agarose beads. Anal Biochem. 1973 Apr; 52(2):363-8. PMID: 4698834.
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      269. Santi DV, Marchant W, Yarus M. Affinity labeling of isoleucyl-tRNA synthetase with N-bromoacetylisoleucyl-tRNA. Biochem Biophys Res Commun. 1973 Mar 17; 51(2):370-5. PMID: 4571405.
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      270. Santi DV, Pena VA. Tyrosyl transfer ribonucleic acid synthetase from Escherichia coli B. Analysis of tyrosine and adenosine 5'-triphosphate binding sites. J Med Chem. 1973 Mar; 16(3):273-80. PMID: 4581950.
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      271. Santi DV, McHenry CS. 5-Fluoro-2'-deoxyuridylate: covalent complex with thymidylate synthetase. Proc Natl Acad Sci U S A. 1972 Jul; 69(7):1855-7. PMID: 4505665; PMCID: PMC426818.
      272. Santi DV, Sakai TT. Irreversible inhibition of thymidylate synthetase by 5-formyl-2'-deoxyuridylic acid. Biochem Biophys Res Commun. 1972 Feb 16; 46(3):1320-5. PMID: 4622223.
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      273. Santi DV, Danenberg PV, Satterly P. Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli. Reaction parameters and order of substrate addition. Biochemistry. 1971 Dec 7; 10(25):4804-12. PMID: 4334585.
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      274. Santi DV, Danenberg PV. Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli. Analysis of the phenylalanine binding site. Biochemistry. 1971 Dec 7; 10(25):4813-20. PMID: 4334586.
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      275. Santi DV, Danenberg PV, Montgomery KA. Phenylalanyl transfer ribonucleic acid synthetase from Escherichia coli. Analysis of the adenosine triphosphate binding site. Biochemistry. 1971 Dec 7; 10(25):4821-4. PMID: 4334587.
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      276. Santi DV, Sakai TT. Thymidylate synthetase. Model studies of inhibition by 5-trifluoromethyl-2'-deoxyuridylic acid. Biochemistry. 1971 Sep 14; 10(19):3598-607. PMID: 5146573.
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      277. Wilcox G, Clemetson KJ, Santi DV, Englesberg E. Purification of the araC protein. Proc Natl Acad Sci U S A. 1971 Sep; 68(9):2145-8. PMID: 4943786; PMCID: PMC389371.
      278. Santi DV, Sakai TT. Inhibition of thymidylate synthetase by 5-formyl- and 5-hydroxymethyl-2'-deoxyuridylate. Biochem Biophys Res Commun. 1971 Mar 5; 42(5):813-7. PMID: 4929928.
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      279. Santi DV, Brewer CF. Model studies of thymidylate synthetase. Neighboring-group facilitation of electrophilic substitution reactions of uracil furanosides. J Am Chem Soc. 1968 Oct 23; 90(22):6236-8. PMID: 5696276.
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      280. Baker BR, Kawazu M, Santi DV, Schwan TJ. Irreversible Enzyme Inhibitors. LXXVII.(1,2) Inhibitors of Thymidine Phosphorylase. III.(2) Hydrophobic Bonding by 1-Substituted Uracils Containing Additional Substituents at the 5 and 6 Positions. J Med Chem. 1967 May 1; 10(3):304-11. PMID: 22185119.
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      281. Baker BR, Santi DV. Irreversible enzyme inhibitors. LXXIV. Inhibitors of guanine deaminase. II. Studies on bulk tolerance within enzyme-inhibitor complexes. J Med Chem. 1967 Jan; 10(1):62-4. PMID: 6031704.
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      282. Baker BR, Schwan TJ, Santi DV. Nonclassical antimetabolites. XXV. Inhibitors of thymidine kinase. I. A new spectrophotometric assay. Inhibition by nucleoside derivatives. J Med Chem. 1966 Jan; 9(1):66-72. PMID: 4225176.
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      283. Baker BR, Beng-Thong Ho, Santi DV. Analogs of tetrahydrofolic acid. XXVII. Hydrophobic bonding to dihydrofolic reductase by 2-amino-4,6-disubstituted-5-alkylpyrimidines and 1-alkyl-4,6-diamino-1,2-dihydro-s-triazines. J Pharm Sci. 1965 Oct; 54(10):1415-24. PMID: 5883214.
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      284. Baker BR, Santi DV. Analogs of tetrahydrofolic acid XXIV. Further observations on the mode of pyrimidyl binding to dihydrofolic reductase and thymidylate synthetase by the 2-amino-5-(3-anilinopropyl)-6-methyl-4-pyrimidinol type of inhibitor. J Pharm Sci. 1965 Sep; 54(9):1252-7. PMID: 5881214.
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      285. BAKER BR, SANTI DV, SHAPIRO HS. ANALOGS OF TETRAHYDROFOLIC ACID. XIV. FACILE SYNTHETIC ROUTE TO THE 2-AMINO-5-(3-ANILINOPROPYL)-6-METHYL-4-PYRIMIDINOL TYPE OF FOLIC REDUCTASE AND THYMIDYLATE SYNTHETASE INHIBITOR. J Pharm Sci. 1964 Nov; 53:1317-25. PMID: 14253585.
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      286. BAKER BR, SANTI DV, ALMAULA PI, WERKEISER WC. ANALOGS OF TETRAHYDROFOLIC ACID. X. SYNTHETIC AND ENZYMIC STUDIES ON THE CONTRIBUTION OF THE P-AMINOBENZOYL-L-GLUTAMATE MOIETY OF PYRIMIDYL ANALOGS TO BINDING TO SOME FOLIC COFACTOR AREA ENZYMES. J Med Chem. 1964 Jan; 7:24-30. PMID: 14186020.
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