Daniel Santi, MD, PhD
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Title(s) | Professor, Pharmaceutical Chemistry |
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School | School of Pharmacy |
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Phone | 415-215-5586 |
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vCard | Download vCard |
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Biography University of California, San Francisco | M.D. | 1980 | Medicine |
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.
Research Bibliographic
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Santi D, De Vincentis S, Scaltriti S, Rochira V. Relative hyperestrogenism in Klinefelter Syndrome: results from a meta-analysis. Endocrine. 2019 Jan 30. PMID: 30701446.
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Pignatti E, Vighi E, Magnani E, Kara E, Roncati L, Maiorana A, Santi D, Madeo B, Cioni K, Carani C, Rochira V, Simoni M, Brigante G. Expression and clinicopathological role of miR146a in thyroid follicular carcinoma. Endocrine. 2019 Jan 30. PMID: 30701447.
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Casarini L, Santi D, Brigante G, Simoni M. Two Hormones for One Receptor: Evolution, Biochemistry, Actions, and Pathophysiology of LH and hCG. Endocr Rev. 2018 10 01; 39(5):549-592. PMID: 29905829.
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Alviggi C, Conforti A, Santi D, Esteves SC, Andersen CY, Humaidan P, Chiodini P, De Placido G, Simoni M. Clinical relevance of genetic variants of gonadotrophins and their receptors in controlled ovarian stimulation: a systematic review and meta-analysis. Hum Reprod Update. 2018 09 01; 24(5):599-614. PMID: 29924306.
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Machinaga N, Ashley GW, Reid R, Yamasaki A, Tanaka K, Nakamura K, Yabe Y, Yoshigae Y, Santi DV. A Controlled Release System for Long-Acting Intravitreal Delivery of Small Molecules. Transl Vis Sci Technol. 2018 Jul; 7(4):21. PMID: 30174998.
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Santi D, Spaggiari G, Simoni M. Sperm DNA fragmentation index as a promising predictive tool for male infertility diagnosis and treatment management - meta-analyses. Reprod Biomed Online. 2018 09; 37(3):315-326. PMID: 30314886.
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Santi D, Locaso M, Granata AR, Trenti T, Roli L, Pacchioni C, Rochira V, Carani C, Simoni M. Could chronic Vardenafil administration influence the cardiovascular risk in men with type 2 diabetes mellitus? PLoS One. 2018; 13(6):e0199299. PMID: 29953477.
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Vezzani S, Giannetta E, Altieri B, Barbonetti A, Bellastella G, Certo R, Cignarelli A, Cinti F, D'Andrea S, Di Dalmazi G, Frara S, Garelli S, Giuffrida G, Maiorino MI, Mele C, Mezza T, Pani MG, Samà MT, Satta C, Santi D. AN ITALIAN SURVEY OF COMPLIANCE WITH MAJOR GUIDELINES FOR L-THYROXINE OF PRIMARY HYPOTHYROIDISM. Endocr Pract. 2018 May; 24(5):419-428. PMID: 29847168.
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Santi D, Casarini L, Alviggi C, Simoni M. Response: Commentary: Efficacy of Follicle-Stimulating Hormone (FSH) Alone, FSH?+?Luteinizing Hormone, Human Menopausal Gonadotropin or FSH?+?Human Chorionic Gonadotropin on Assisted Reproductive Technology Outcomes in the "Personalized" Medicine Era: A Meta-analysis. Front Endocrinol (Lausanne). 2018; 9:113. PMID: 29628912.
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Hearn BR, Fontaine SD, Pfaff SJ, Schneider EL, Henise J, Ashley GW, Santi DV. Primary deuterium kinetic isotope effects prolong drug release and polymer biodegradation in a drug delivery system. J Control Release. 2018 May 28; 278:74-79. PMID: 29577950.
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Santi D, Magnani E, Michelangeli M, Grassi R, Vecchi B, Pedroni G, Roli L, De Santis MC, Baraldi E, Setti M, Trenti T, Simoni M. Seasonal variation of semen parameters correlates with environmental temperature and air pollution: A big data analysis over 6 years. Environ Pollut. 2018 Apr; 235:806-813. PMID: 29353799.
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Casarini L, Santi D, Simoni M, Potì F. 'Spare' Luteinizing Hormone Receptors: Facts and Fiction. Trends Endocrinol Metab. 2018 04; 29(4):208-217. PMID: 29429918.
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Santi D, Potì F, Simoni M, Casarini L. Pharmacogenetics of G-protein-coupled receptors variants: FSH receptor and infertility treatment. Best Pract Res Clin Endocrinol Metab. 2018 04; 32(2):189-200. PMID: 29678285.
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Spaggiari G, Brigante G, De Vincentis S, Cattini U, Roli L, De Santis MC, Baraldi E, Tagliavini S, Varani M, Trenti T, Rochira V, Simoni M, Santi D. Probiotics Ingestion Does Not Directly Affect Thyroid Hormonal Parameters in Hypothyroid Patients on Levothyroxine Treatment. Front Endocrinol (Lausanne). 2017; 8:316. PMID: 29184537.
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Madeo B, Kara E, Cioni K, Vezzani S, Trenti T, Santi D, Simoni M, Rochira V. Serum Calcium to Phosphorous (Ca/P) Ratio Is a Simple, Inexpensive, and Accurate Tool in the Diagnosis of Primary Hyperparathyroidism. JBMR Plus. 2018 Mar; 2(2):109-117. PMID: 30283895.
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Bosco L, Ruvolo G, Luparello C, Ferrari S, Valerio D, Santi D, Piomboni P, Sarcina E, Lispi M, Roccheri MC. Gene Expression and Apoptosis Levels in Cumulus Cells of Patients with Polymorphisms of FSHR and LHB Undergoing in Vitro Fertilization Program. Cell Physiol Biochem. 2017; 43(6):2391-2404. PMID: 29073627.
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Santi D, Spaggiari G, Gilioli L, Potì F, Simoni M, Casarini L. Molecular basis of androgen action on human sexual desire. Mol Cell Endocrinol. 2018 May 15; 467:31-41. PMID: 28893567.
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Schneider EL, Hearn BR, Pfaff SJ, Reid R, Parkes DG, Vrang N, Ashley GW, Santi DV. A Hydrogel-Microsphere Drug Delivery System That Supports Once-Monthly Administration of a GLP-1 Receptor Agonist. ACS Chem Biol. 2017 08 18; 12(8):2107-2116. PMID: 28605180.
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Piccoli M, Mullineris B, Santi D, Gozzo D. Advances in Robotic Transaxillary Thyroidectomy in Europe. Curr Surg Rep. 2017; 5(8):17. PMID: 28680769.
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Santi D, Casarini L, Alviggi C, Simoni M. Efficacy of Follicle-Stimulating Hormone (FSH) Alone, FSH?+?Luteinizing Hormone, Human Menopausal Gonadotropin or FSH?+?Human Chorionic Gonadotropin on Assisted Reproductive Technology Outcomes in the "Personalized" Medicine Era: A Meta-analysis. Front Endocrinol (Lausanne). 2017; 8:114. PMID: 28620352.
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Riccetti L, De Pascali F, Gilioli L, Santi D, Brigante G, Simoni M, Casarini L. Genetics of gonadotropins and their receptors as markers of ovarian reserve and response in controlled ovarian stimulation. Best Pract Res Clin Obstet Gynaecol. 2017 Oct; 44:15-25. PMID: 28506471.
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Melcangi RC, Santi D, Spezzano R, Grimoldi M, Tabacchi T, Fusco ML, Diviccaro S, Giatti S, Carrà G, Caruso D, Simoni M, Cavaletti G. Neuroactive steroid levels and psychiatric and andrological features in post-finasteride patients. J Steroid Biochem Mol Biol. 2017 07; 171:229-235. PMID: 28408350.
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Santi D, Spaggiari G, Casarini L, Fanelli F, Mezzullo M, Pagotto U, Granata ARM, Carani C, Simoni M. Central hypogonadism due to a giant, "silent" FSH-secreting, atypical pituitary adenoma: effects of adenoma dissection and short-term Leydig cell stimulation by luteinizing hormone (LH) and human chorionic gonadotropin (hCG). Aging Male. 2017 Jun; 20(2):96-101. PMID: 28067604.
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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 07. PMID: 27657443.
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Santi D, Granata AR, Pignatti E, Trenti T, Roli L, Bozic R, Zaza S, Pacchioni C, Rochira V, Carani C, Simoni M. Effects of chronic administration of the phosphodiesterase inhibitor vardenafil on serum levels of adrenal and testicular steroids in men with type 2 diabetes mellitus. Endocrine. 2017 May; 56(2):426-437. PMID: 27515804.
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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 07 20; 27(7):1638-44. PMID: 27253622.
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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 09; 31(9):1960-9. PMID: 27329968.
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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 10; 150:144-153. PMID: 27288912.
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Henise J, Hearn BR, Santi DV, Kamata H, Sakai T, Ashley GW. Surgical sealants with tunable swelling, burst pressures, and biodegradation rates. J Biomed Mater Res B Appl Biomater. 2017 08; 105(6):1602-1611. PMID: 27149244.
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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 05 18; 27(5):1210-5. PMID: 26930186.
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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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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.
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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.
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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.
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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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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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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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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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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.
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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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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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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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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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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.
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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 05; 110(6):2318-23. PMID: 23345437; PMCID: PMC3568318.
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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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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.
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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.
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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.
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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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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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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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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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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.
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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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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.
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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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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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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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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.
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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 02; 101(44):15573-8. PMID: 15496466; PMCID: PMC524854.
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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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Kodumal SJ, Santi DV. DNA ligation by selection. Biotechniques. 2004 Jul; 37(1):34, 36, 38 passim. PMID: 15283197.
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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 01; 328(1):51-9. PMID: 15081907.
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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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Carreras CW, Schirmer A, Zhong Z, Santi DV. Filter binding assay for the geldanamycin-heat shock protein 90 interaction. Anal Biochem. 2003 Jun 01; 317(1):40-6. PMID: 12729599.
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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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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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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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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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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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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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Santi DV, Peña VA. Order of substrate binding to tyrosyl-tRNA synthetase of Escherichia coli B. FEBS Lett. 1971 Mar 05; 13(3):157-160. PMID: 11945656.
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