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    Kathy Giacomini, PhD

    TitleProfessor
    SchoolUCSF School of Pharmacy
    DepartmentBioengineering and Therapeutic Sciences
    Address1550 4th Street, Rock Hall
    San Francisco CA 94158
    Phone415-476-1936
    Emailkathy.giacomini@ucsf.edu
      Other Positions
      TitleChair, Bioengineering and Therapeutic Sciences


       Biography 
       Awards and Honors
      School of Pharmacy, University of California, San Francisco1983Long Foundation Award for Excellence in Teaching
      American Association of University Women1984UCSF Nominee for Recognition Award for Young Scholar
      Swedish Academy of Pharmaceutical Scientists2011Scheele Award
      University of California, San Francisco, Academic Senate1985Distinguished Teaching Award
      American Society for Clinical Pharmacology and Therapeutics1990Leon Goldberg Young Investigator Award
      National Institutes of Health1992Fogarty International Fellowship
      University of California, San Francisco1994Martin Luther King, Jr. Award for the Advancement of Minorities
      University of California, San Francisco1997Chancellor's Award for the Advancement of Women
      University of California, San Francisco1999Recognition Award for Distinguished Achievement of a Filipino at UCSF
      International Pharmaceutical Federation (FIP)1999Scientist of the Year
      University of Kentucky2000Guttman Lecturer
      University of California, San Francisco2002Honored Celebrating Women Faculty
      U.S. Food and Drug Administration2002Distinguished Bill Abram's Lectureship
      State University of New York at Buffalo2002Distinguished Gerhard Levy Lectureship
      American Association of Colleges of Pharmacy2005Paul Dawson Biotechnology Award
      American Association of Pharmaceutical Scientists2006Distinguished Scientist Award in Drug Metabolism
      Institute of Medicine of the National Academy of Sciences2006Elected Member
      Pharmaceutical Sciences World Congress2007Research Achievement Award
      Academy of Pharmaceutical Sciences and Technology, Japan2007International Woman Scientist Award
      Japan Society for the Promotion of Science2008Invitation Fellowship Program for Research in Japan
      American Society for Clinical Pharmacology and Therapeutics2009Rawls-Palmer Progress in Medicine Award
      Postdoctoral Scholars Association, University of California, San Francisco2009Outstanding Mentor Award
      American College of Clinical Pharmacy 2010Therapeutic Frontiers Lecture Award
      Swedish Academy of Pharmaceutical Scientists2011Scheele Award

       Overview 
       Overview
      Kathy Giacomini's research group focuses on membrane transporters, which are of great pharmacological importance as they play a major role in drug disposition and response. Major questions addressed in the laboratory include: What is the in vivo role of membrane transporters in drug disposition and response? How does genetic variation in membrane transporters affect clinical drug response? What is the endogenous role of membrane transporters? What are the structural determinants of specificity?

      As PI of the major project funded by NIH, Pharmacogenetics of Membrane Transporters, Giacomini is leading an effort to understand the implications of genetic variation in over 100 membrane transporters on clinical drug response. Studies of the project, ranging from discovery to clinical studies, have demonstrated that common variants of membrane transporters contribute to variation in drug response. Ultimately, the information obtained from these studies may be used in personalizing drug therapy and may even be used to design drugs to better treat subsets of patients who do not respond to standard treatments.

      Research in the laboratory focuses on the anti-diabetic drug, metformin, and on anti-cancer drugs. By mediating influx of efflux in tumor cells, many membrane transporters play critical roles in sensitivity and resistance to anti-cancer drugs. Giacomini and her colleagues seek to determine whether genetic variation in transporters contributes to variation in sensitivity and resistance to anti-cancer drugs. She is particularly interested in modifying anti-cancer drugs to target transporters in tumors thereby enhancing their uptake and efficacy.

       Interests
      Pharmaceutical sciences, pharmacogenomics, pharmacogenetics, membrane transporters, metformin, regulatory sciences, bioengineering, therapeutics.


       Bibliographic 
       Publications
      Publications by year:
      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.
      1. Geier EG, Schlessinger A, Fan H, Gable JE, Irwin JJ, Sali A, Giacomini KM. Structure-based ligand discovery for the Large-neutral Amino Acid Transporter 1, LAT-1. Proc Natl Acad Sci U S A. 2013 Apr 2; 110(14):5480-5.
        View in: PubMed
      2. Dahlin A, Geier E, Stocker SL, Cropp CD, Grigorenko E, Bloomer M, Siegenthaler J, Xu L, Basile AS, Tang-Liu DD, Giacomini KM. Gene Expression Profiling of Transporters in the Solute Carrier and ATP-Binding Cassette Superfamilies in Human Eye Substructures. Mol Pharm. 2013 Feb 4; 10(2):650-63.
        View in: PubMed
      3. Wittwer MB, Zur AA, Khuri N, Kido Y, Kosaka A, Zhang X, Morrissey KM, Sali A, Huang Y, Giacomini KM. Discovery of Potent, Selective Multidrug and Toxin Extrusion Transporter 1 (MATE1, SLC47A1) Inhibitors Through Prescription Drug Profiling and Computational Modeling. J Med Chem. 2013 Feb 14; 56(3):781-95.
        View in: PubMed
      4. Morrissey KM, Stocker SL, Wittwer MB, Xu L, Giacomini KM. Renal transporters in drug development. Annu Rev Pharmacol Toxicol. 2013 Jan 6; 53:503-29.
        View in: PubMed
      5. Gong L, Goswami S, Giacomini KM, Altman RB, Klein TE. Metformin pathways: pharmacokinetics and pharmacodynamics. Pharmacogenet Genomics. 2012 Nov; 22(11):820-7.
        View in: PubMed
      6. Zamek-Gliszczynski MJ, Hoffmaster KA, Tweedie DJ, Giacomini KM, Hillgren KM. Highlights from the international transporter consortium second workshop. Clin Pharmacol Ther. 2012 Nov; 92(5):553-6.
        View in: PubMed
      7. Morrissey KM, Wen CC, Johns SJ, Zhang L, Huang SM, Giacomini KM. The UCSF-FDA TransPortal: A Public Drug Transporter Database. Clin Pharmacol Ther. 2012 Nov; 92(5):545-6.
        View in: PubMed
      8. Stocker SL, Morrissey KM, Yee SW, Castro RA, Xu L, Dahlin A, Ramirez AH, Roden DM, Wilke RA, McCarty CA, Davis RL, Brett CM, Giacomini KM. The Effect of Novel Promoter Variants in MATE1 and MATE2 on the Pharmacokinetics and Pharmacodynamics of Metformin. Clin Pharmacol Ther. 2013 Feb; 93(2):186-94.
        View in: PubMed
      9. Giacomini KM, Yee SW, Ratain MJ, Weinshilboum RM, Kamatani N, Nakamura Y. Pharmacogenomics and patient care: one size does not fit all. Sci Transl Med. 2012 Sep 26; 4(153):153ps18.
        View in: PubMed
      10. Dubois SG, Geier E, Batra V, Yee SW, Neuhaus J, Segal M, Martinez D, Pawel B, Yanik G, Naranjo A, London WB, Kreissman S, Baker D, Attiyeh E, Hogarty MD, Maris JM, Giacomini K, Matthay KK. Evaluation of Norepinephrine Transporter Expression and Metaiodobenzylguanidine Avidity in Neuroblastoma: A Report from the Children's Oncology Group. Int J Mol Imaging. 2012; 2012:250834.
        View in: PubMed
      11. Schlessinger A, Wittwer MB, Dahlin A, Khuri N, Bonomi M, Fan H, Giacomini KM, Sali A. High Selectivity of the ?-Aminobutyric Acid Transporter 2 (GAT-2, SLC6A13) Revealed by Structure-based Approach. J Biol Chem. 2012 Nov 2; 287(45):37745-56.
        View in: PubMed
      12. Smith DE, Rowland M, Giacomini KM, Amidon GL. Dedication to professor Leslie Z. Benet: 50 years of scientific excellence and still going strong! Pharm Res. 2012 Sep; 29(9):2345-53.
        View in: PubMed
      13. Yee SW, Chen L, Giacomini KM. The role of ATM in response to metformin treatment and activation of AMPK. Nat Genet. 2012 Apr; 44(4):359-60.
        View in: PubMed
      14. Chen L, Hong C, Chen EC, Yee SW, Xu L, Almof EU, Wen C, Fujii K, Johns SJ, Stryke D, Ferrin TE, Simko J, Chen X, Costello JF, Giacomini KM. Genetic and epigenetic regulation of the organic cation transporter 3, SLC22A3. Pharmacogenomics J. 2013 Apr; 13(2):110-20.
        View in: PubMed
      15. Ramsey LB, Bruun GH, Yang W, Treviño LR, Vattathil S, Scheet P, Cheng C, Rosner GL, Giacomini KM, Fan Y, Sparreboom A, Mikkelsen TS, Corydon TJ, Pui CH, Evans WE, Relling MV. Rare versus common variants in pharmacogenetics: SLCO1B1 variation and methotrexate disposition. Genome Res. 2012 Jan; 22(1):1-8.
        View in: PubMed
      16. Innocenti F, Owzar K, Cox NL, Evans P, Kubo M, Zembutsu H, Jiang C, Hollis D, Mushiroda T, Li L, Friedman P, Wang L, Glubb D, Hurwitz H, Giacomini KM, McLeod HL, Goldberg RM, Schilsky RL, Kindler HL, Nakamura Y, Ratain MJ. A genome-wide association study of overall survival in pancreatic cancer patients treated with gemcitabine in CALGB 80303. Clin Cancer Res. 2012 Jan 15; 18(2):577-84.
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      17. Choi JH, Yee SW, Ramirez AH, Morrissey KM, Jang GH, Joski PJ, Mefford JA, Hesselson SE, Schlessinger A, Jenkins G, Castro RA, Johns SJ, Stryke D, Sali A, Ferrin TE, Witte JS, Kwok PY, Roden DM, Wilke RA, McCarty CA, Davis RL, Giacomini KM. A common 5'-UTR variant in MATE2-K is associated with poor response to metformin. Clin Pharmacol Ther. 2011 Nov; 90(5):674-84.
        View in: PubMed
      18. Schlessinger A, Geier E, Fan H, Irwin JJ, Shoichet BK, Giacomini KM, Sali A. Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET. Proc Natl Acad Sci U S A. 2011 Sep 20; 108(38):15810-5.
        View in: PubMed
      19. Kido Y, Matsson P, Giacomini KM. Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. J Med Chem. 2011 Jul 14; 54(13):4548-58.
        View in: PubMed
      20. Picard N, Levoir L, Lamoureux F, Yee SW, Giacomini KM, Marquet P. Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica. 2011 Sep; 41(9):752-7.
        View in: PubMed
      21. More SS, Itsara M, Yang X, Geier EG, Tadano MK, Seo Y, Vanbrocklin HF, Weiss WA, Mueller S, Haas-Kogan DA, Dubois SG, Matthay KK, Giacomini KM. Vorinostat increases expression of functional norepinephrine transporter in neuroblastoma in vitro and in vivo model systems. Clin Cancer Res. 2011 Apr 15; 17(8):2339-49.
        View in: PubMed
      22. Matsson P, Yee SW, Markova S, Morrissey K, Jenkins G, Xuan J, Jorgenson E, Kroetz DL, Giacomini KM. Discovery of regulatory elements in human ATP-binding cassette transporters through expression quantitative trait mapping. Pharmacogenomics J. 2012 Jun; 12(3):214-26.
        View in: PubMed
      23. Kim MJ, Skewes-Cox P, Fukushima H, Hesselson S, Yee SW, Ramsey LB, Nguyen L, Eshragh JL, Castro RA, Wen CC, Stryke D, Johns SJ, Ferrin TE, Kwok PY, Relling MV, Giacomini KM, Kroetz DL, Ahituv N. Functional characterization of liver enhancers that regulate drug-associated transporters. Clin Pharmacol Ther. 2011 Apr; 89(4):571-8.
        View in: PubMed
      24. Minematsu T, Giacomini KM. Interactions of tyrosine kinase inhibitors with organic cation transporters and multidrug and toxic compound extrusion proteins. Mol Cancer Ther. 2011 Mar; 10(3):531-9.
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      25. Chen L, Xue L, Giacomini KM, Casida JE. GABAA receptor open-state conformation determines non-competitive antagonist binding. Toxicol Appl Pharmacol. 2011 Feb 1; 250(3):221-8.
        View in: PubMed
      26. Li S, Chen Y, Zhang S, More SS, Huang X, Giacomini KM. Role of organic cation transporter 1, OCT1 in the pharmacokinetics and toxicity of cis-diammine(pyridine)chloroplatinum(II) and oxaliplatin in mice. Pharm Res. 2011 Mar; 28(3):610-25.
        View in: PubMed
      27. Miller WL, Agrawal V, Sandee D, Tee MK, Huang N, Choi JH, Morrissey K, Giacomini KM. Consequences of POR mutations and polymorphisms. Mol Cell Endocrinol. 2011 Apr 10; 336(1-2):174-9.
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      28. Sandee D, Morrissey K, Agrawal V, Tam HK, Kramer MA, Tracy TS, Giacomini KM, Miller WL. Effects of genetic variants of human P450 oxidoreductase on catalysis by CYP2D6 in vitro. Pharmacogenet Genomics. 2010 Nov; 20(11):677-86.
        View in: PubMed
      29. Chen L, Pawlikowski B, Schlessinger A, More SS, Stryke D, Johns SJ, Portman MA, Chen E, Ferrin TE, Sali A, Giacomini KM. Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin. Pharmacogenet Genomics. 2010 Nov; 20(11):687-99.
        View in: PubMed
      30. Yee SW, Gong L, Badagnani I, Giacomini KM, Klein TE, Altman RB. SLC19A1 pharmacogenomics summary. Pharmacogenet Genomics. 2010 Nov; 20(11):708-15.
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      31. Agrawal V, Choi JH, Giacomini KM, Miller WL. Substrate-specific modulation of CYP3A4 activity by genetic variants of cytochrome P450 oxidoreductase. Pharmacogenet Genomics. 2010 Oct; 20(10):611-8.
        View in: PubMed
      32. Shima JE, Komori T, Taylor TR, Stryke D, Kawamoto M, Johns SJ, Carlson EJ, Ferrin TE, Giacomini KM. Genetic variants of human organic anion transporter 4 demonstrate altered transport of endogenous substrates. Am J Physiol Renal Physiol. 2010 Oct; 299(4):F767-75.
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      33. Chen L, Takizawa M, Chen E, Schlessinger A, Segenthelar J, Choi JH, Sali A, Kubo M, Nakamura S, Iwamoto Y, Iwasaki N, Giacomini KM. Genetic polymorphisms in organic cation transporter 1 (OCT1) in Chinese and Japanese populations exhibit altered function. J Pharmacol Exp Ther. 2010 Oct; 335(1):42-50.
        View in: PubMed
      34. More SS, Akil O, Ianculescu AG, Geier EG, Lustig LR, Giacomini KM. Role of the copper transporter, CTR1, in platinum-induced ototoxicity. J Neurosci. 2010 Jul 14; 30(28):9500-9.
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      35. Ahlin G, Chen L, Lazorova L, Chen Y, Ianculescu AG, Davis RL, Giacomini KM, Artursson P. Genotype-dependent effects of inhibitors of the organic cation transporter, OCT1: predictions of metformin interactions. Pharmacogenomics J. 2011 Dec; 11(6):400-11.
        View in: PubMed
      36. More SS, Li S, Yee SW, Chen L, Xu Z, Jablons DM, Giacomini KM. Organic cation transporters modulate the uptake and cytotoxicity of picoplatin, a third-generation platinum analogue. Mol Cancer Ther. 2010 Apr; 9(4):1058-69.
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      37. Yee SW, Chen L, Giacomini KM. Pharmacogenomics of membrane transporters: past, present and future. Pharmacogenomics. 2010 Apr; 11(4):475-9.
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      38. Ianculescu AG, Friesema EC, Visser TJ, Giacomini KM, Scanlan TS. Transport of thyroid hormones is selectively inhibited by 3-iodothyronamine. Mol Biosyst. 2010 Aug; 6(8):1403-10.
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      39. Membrane transporters in drug development. Nat Rev Drug Discov. 2010 Mar; 9(3):215-36.
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      40. Schlessinger A, Matsson P, Shima JE, Pieper U, Yee SW, Kelly L, Apeltsin L, Stroud RM, Ferrin TE, Giacomini KM, Sali A. Comparison of human solute carriers. Protein Sci. 2010 Mar; 19(3):412-28.
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      41. Huang SM, Zhang L, Giacomini KM. The International Transporter Consortium: a collaborative group of scientists from academia, industry, and the FDA. Clin Pharmacol Ther. 2010 Jan; 87(1):32-6.
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      42. Kroetz DL, Yee SW, Giacomini KM. The pharmacogenomics of membrane transporters project: research at the interface of genomics and transporter pharmacology. Clin Pharmacol Ther. 2010 Jan; 87(1):109-16.
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      43. Treviño LR, Shimasaki N, Yang W, Panetta JC, Cheng C, Pei D, Chan D, Sparreboom A, Giacomini KM, Pui CH, Evans WE, Relling MV. Germline genetic variation in an organic anion transporter polypeptide associated with methotrexate pharmacokinetics and clinical effects. J Clin Oncol. 2009 Dec 10; 27(35):5972-8.
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      44. Picard N, Yee SW, Woillard JB, Lebranchu Y, Le Meur Y, Giacomini KM, Marquet P. The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokinetics. Clin Pharmacol Ther. 2010 Jan; 87(1):100-8.
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      45. Kroetz DL, Ahituv N, Burchard EG, Guo S, Sali A, Giacomini KM. Institutional Profile: The University of California Pharmacogenomics Center: at the interface of genomics, biological mechanisms and drug therapy. Pharmacogenomics. 2009 Oct; 10(10):1569-76.
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      46. Ha Choi J, Wah Yee S, Kim MJ, Nguyen L, Ho Lee J, Kang JO, Hesselson S, Castro RA, Stryke D, Johns SJ, Kwok PY, Ferrin TE, Goo Lee M, Black BL, Ahituv N, Giacomini KM. Identification and characterization of novel polymorphisms in the basal promoter of the human transporter, MATE1. Pharmacogenet Genomics. 2009 Oct; 19(10):770-80.
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      47. Kelly L, Pieper U, Eswar N, Hays FA, Li M, Roe-Zurz Z, Kroetz DL, Giacomini KM, Stroud RM, Sali A. A survey of integral alpha-helical membrane proteins. J Struct Funct Genomics. 2009 Dec; 10(4):269-80.
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      48. Hesselson SE, Matsson P, Shima JE, Fukushima H, Yee SW, Kobayashi Y, Gow JM, Ha C, Ma B, Poon A, Johns SJ, Stryke D, Castro RA, Tahara H, Choi JH, Chen L, Picard N, Sjödin E, Roelofs MJ, Ferrin TE, Myers R, Kroetz DL, Kwok PY, Giacomini KM. Genetic variation in the proximal promoter of ABC and SLC superfamilies: liver and kidney specific expression and promoter activity predict variation. PLoS One. 2009; 4(9):e6942.
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      49. Chen Y, Li S, Brown C, Cheatham S, Castro RA, Leabman MK, Urban TJ, Chen L, Yee SW, Choi JH, Huang Y, Brett CM, Burchard EG, Giacomini KM. Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin. Pharmacogenet Genomics. 2009 Jul; 19(7):497-504.
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      50. McBride BF, Yang T, Liu K, Urban TJ, Giacomini KM, Kim RB, Roden DM. The organic cation transporter, OCTN1, expressed in the human heart, potentiates antagonism of the HERG potassium channel. J Cardiovasc Pharmacol. 2009 Jul; 54(1):63-71.
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      51. Chen Y, Teranishi K, Li S, Yee SW, Hesselson S, Stryke D, Johns SJ, Ferrin TE, Kwok P, Giacomini KM. Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function. Pharmacogenomics J. 2009 Apr; 9(2):127-36.
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      52. Tahara H, Yee SW, Urban TJ, Hesselson S, Castro RA, Kawamoto M, Stryke D, Johns SJ, Ferrin TE, Kwok PY, Giacomini KM. Functional genetic variation in the basal promoter of the organic cation/carnitine transporters OCTN1 (SLC22A4) and OCTN2 (SLC22A5). J Pharmacol Exp Ther. 2009 Apr; 329(1):262-71.
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      53. Yee SW, Shima JE, Hesselson S, Nguyen L, De Val S, Lafond RJ, Kawamoto M, Johns SJ, Stryke D, Kwok PY, Ferrin TE, Black BL, Gurwitz D, Ahituv N, Giacomini KM. Identification and characterization of proximal promoter polymorphisms in the human concentrative nucleoside transporter 2 (SLC28A2). J Pharmacol Exp Ther. 2009 Mar; 328(3):699-707.
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      54. Ianculescu AG, Giacomini KM, Scanlan TS. Identification and characterization of 3-iodothyronamine intracellular transport. Endocrinology. 2009 Apr; 150(4):1991-9.
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      55. Li M, Hays FA, Roe-Zurz Z, Vuong L, Kelly L, Ho CM, Robbins RM, Pieper U, O'Connell JD, Miercke LJ, Giacomini KM, Sali A, Stroud RM. Selecting optimum eukaryotic integral membrane proteins for structure determination by rapid expression and solubilization screening. J Mol Biol. 2009 Jan 23; 385(3):820-30.
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      56. Miller WL, Huang N, Agrawal V, Giacomini KM. Genetic variation in human P450 oxidoreductase. Mol Cell Endocrinol. 2009 Mar 5; 300(1-2):180-4.
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      57. Sorani MD, Manley GT, Giacomini KM. Genetic variation in human aquaporins and effects on phenotypes of water homeostasis. Hum Mutat. 2008 Sep; 29(9):1108-17.
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      58. Lovejoy KS, Todd RC, Zhang S, McCormick MS, D'Aquino JA, Reardon JT, Sancar A, Giacomini KM, Lippard SJ. cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospects. Proc Natl Acad Sci U S A. 2008 Jul 1; 105(26):8902-7.
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      59. Weiss ST, McLeod HL, Flockhart DA, Dolan ME, Benowitz NL, Johnson JA, Ratain MJ, Giacomini KM. Creating and evaluating genetic tests predictive of drug response. Nat Rev Drug Discov. 2008 Jul; 7(7):568-74.
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      60. Cropp CD, Yee SW, Giacomini KM. Genetic variation in drug transporters in ethnic populations. Clin Pharmacol Ther. 2008 Sep; 84(3):412-6.
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      61. Sorani MD, Zador Z, Hurowitz E, Yan D, Giacomini KM, Manley GT. Novel variants in human Aquaporin-4 reduce cellular water permeability. Hum Mol Genet. 2008 Aug 1; 17(15):2379-89.
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      62. Sorani MD, Morabito D, Rosenthal G, Giacomini KM, Manley GT. Characterizing the dose-response relationship between mannitol and intracranial pressure in traumatic brain injury patients using a high-frequency physiological data collection system. J Neurotrauma. 2008 Apr; 25(4):291-8.
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      63. Abla N, Chinn LW, Nakamura T, Liu L, Huang CC, Johns SJ, Kawamoto M, Stryke D, Taylor TR, Ferrin TE, Giacomini KM, Kroetz DL. The human multidrug resistance protein 4 (MRP4, ABCC4): functional analysis of a highly polymorphic gene. J Pharmacol Exp Ther. 2008 Jun; 325(3):859-68.
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      64. Huang N, Agrawal V, Giacomini KM, Miller WL. Genetics of P450 oxidoreductase: sequence variation in 842 individuals of four ethnicities and activities of 15 missense mutations. Proc Natl Acad Sci U S A. 2008 Feb 5; 105(5):1733-8.
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      65. Cropp CD, Komori T, Shima JE, Urban TJ, Yee SW, More SS, Giacomini KM. Organic anion transporter 2 (SLC22A7) is a facilitative transporter of cGMP. Mol Pharmacol. 2008 Apr; 73(4):1151-8.
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      66. Wilke RA, Lin DW, Roden DM, Watkins PB, Flockhart D, Zineh I, Giacomini KM, Krauss RM. Identifying genetic risk factors for serious adverse drug reactions: current progress and challenges. Nat Rev Drug Discov. 2007 Nov; 6(11):904-16.
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      67. Urban TJ, Yang C, Lagpacan LL, Brown C, Castro RA, Taylor TR, Huang CC, Stryke D, Johns SJ, Kawamoto M, Carlson EJ, Ferrin TE, Burchard EG, Giacomini KM. Functional effects of protein sequence polymorphisms in the organic cation/ergothioneine transporter OCTN1 (SLC22A4). Pharmacogenet Genomics. 2007 Sep; 17(9):773-82.
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      68. Shu Y, Brown C, Castro RA, Shi RJ, Lin ET, Owen RP, Sheardown SA, Yue L, Burchard EG, Brett CM, Giacomini KM. Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics. Clin Pharmacol Ther. 2008 Feb; 83(2):273-80.
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      69. Urban TJ, Brown C, Castro RA, Shah N, Mercer R, Huang Y, Brett CM, Burchard EG, Giacomini KM. Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin. Clin Pharmacol Ther. 2008 Mar; 83(3):416-21.
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      70. Chen Y, Zhang S, Sorani M, Giacomini KM. Transport of paraquat by human organic cation transporters and multidrug and toxic compound extrusion family. J Pharmacol Exp Ther. 2007 Aug; 322(2):695-700.
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      71. Altman RB, Benowitz N, Gurwitz D, Lunshof J, Relling M, Lamba J, Wieben E, Mooney S, Giacomini K, Weiss S, Johnson JA, McLeod H, Flockhart D, Weinshilboum R, Shuldiner AR, Roden D, Krauss RM, Ratain M. Genetic nondiscrimination legislation: a critical prerequisite for pharmacogenomics data sharing. Pharmacogenomics. 2007 May; 8(5):519.
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      72. Shu Y, Sheardown SA, Brown C, Owen RP, Zhang S, Castro RA, Ianculescu AG, Yue L, Lo JC, Burchard EG, Brett CM, Giacomini KM. Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. J Clin Invest. 2007 May; 117(5):1422-31.
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      73. Giacomini KM, Krauss RM, Roden DM, Eichelbaum M, Hayden MR, Nakamura Y. When good drugs go bad. Nature. 2007 Apr 26; 446(7139):975-7.
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      74. Giacomini KM, Brett CM, Altman RB, Benowitz NL, Dolan ME, Flockhart DA, Johnson JA, Hayes DF, Klein T, Krauss RM, Kroetz DL, McLeod HL, Nguyen AT, Ratain MJ, Relling MV, Reus V, Roden DM, Schaefer CA, Shuldiner AR, Skaar T, Tantisira K, Tyndale RF, Wang L, Weinshilboum RM, Weiss ST, Zineh I. The pharmacogenetics research network: from SNP discovery to clinical drug response. Clin Pharmacol Ther. 2007 Mar; 81(3):328-45.
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      75. Roden DM, Altman RB, Benowitz NL, Flockhart DA, Giacomini KM, Johnson JA, Krauss RM, McLeod HL, Ratain MJ, Relling MV, Ring HZ, Shuldiner AR, Weinshilboum RM, Weiss ST. Pharmacogenomics: challenges and opportunities. Ann Intern Med. 2006 Nov 21; 145(10):749-57.
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      76. Zhang S, Lovejoy KS, Shima JE, Lagpacan LL, Shu Y, Lapuk A, Chen Y, Komori T, Gray JW, Chen X, Lippard SJ, Giacomini KM. Organic cation transporters are determinants of oxaliplatin cytotoxicity. Cancer Res. 2006 Sep 1; 66(17):8847-57.
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      77. Urban TJ, Gallagher RC, Brown C, Castro RA, Lagpacan LL, Brett CM, Taylor TR, Carlson EJ, Ferrin TE, Burchard EG, Packman S, Giacomini KM. Functional genetic diversity in the high-affinity carnitine transporter OCTN2 (SLC22A5). Mol Pharmacol. 2006 Nov; 70(5):1602-11.
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      78. Owen RP, Badagnani I, Giacomini KM. Molecular determinants of specificity for synthetic nucleoside analogs in the concentrative nucleoside transporter, CNT2. J Biol Chem. 2006 Sep 8; 281(36):26675-82.
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      79. Badagnani I, Castro RA, Taylor TR, Brett CM, Huang CC, Stryke D, Kawamoto M, Johns SJ, Ferrin TE, Carlson EJ, Burchard EG, Giacomini KM. Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants. J Pharmacol Exp Ther. 2006 Aug; 318(2):521-9.
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      80. Shu Y, Urban TJ, Leabman MK, Fujita T, Erdman AR, Lagpacan LL, Brown C, Castro RA, Huang CC, Stryke D, Kawamoto M, Johns SJ, Taylor TR, Chan W, De La Cruz M, Carlson EJ, Ferrin TE, Brett CM, Burchard EG, Herskowitz I, Kroetz DL, Giacomini KM. PharmGKB submission update: V. PMT submissions of genetic variation in SLC22 family transporters. Pharmacol Rev. 2006 Mar; 58(1):3-4.
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      117. Zhang L, Gorset W, Washington CB, Blaschke TF, Kroetz DL, Giacomini KM. Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system. Drug Metab Dispos. 2000 Mar; 28(3):329-34.
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      118. Dresser MJ, Gray AT, Giacomini KM. Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1). J Pharmacol Exp Ther. 2000 Mar; 292(3):1146-52.
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      121. Wang J, Giacomini KM. Characterization of a bioengineered chimeric Na+-nucleoside transporter. Mol Pharmacol. 1999 Feb; 55(2):234-40.
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      122. Wang J, Giacomini KM. Serine 318 is essential for the pyrimidine selectivity of the N2 Na+-nucleoside transporter. J Biol Chem. 1999 Jan 22; 274(4):2298-302.
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      126. Zevin S, Schaner ME, Giacomini KM. Nicotine transport in a human choriocarcinoma cell line (JAR). J Pharm Sci. 1998 Jun; 87(6):702-6.
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      132. Ramanathan VK, Brett CM, Giacomini KM. Na+-dependent gamma-aminobutyric acid (GABA) transport in the choroid plexus of rabbit. Biochim Biophys Acta. 1997 Nov 13; 1330(1):94-102.
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      135. Chun JK, Zhang L, Piquette-Miller M, Lau E, Tong LQ, Giacomini KM. Characterization of guanidine transport in human renal brush border membranes. Pharm Res. 1997 Jul; 14(7):936-41.
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      136. Zhang L, Dresser MJ, Chun JK, Babbitt PC, Giacomini KM. Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A). J Biol Chem. 1997 Jun 27; 272(26):16548-54.
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      138. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM. Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol. 1997 Jun; 51(6):913-21.
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      148. Lubic SP, Giacomini KM, Giacomini JC. The effects of modulation of calcium influx through the voltage-sensitive calcium channel on cardiomyocyte hypertrophy. J Mol Cell Cardiol. 1995 Mar; 27(3):917-25.
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      155. Ott RJ, Chan JK, Ramanathan VK, Hui AC, Giacomini KM. Effect of phenylisothiocyanate on organic cation transport in opossum kidney cells. J Pharmacol Exp Ther. 1994 Apr; 269(1):204-8.
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      158. Cashman JR, Park SB, Yang ZC, Washington CB, Gomez DY, Giacomini KM, Brett CM. Chemical, enzymatic, and human enantioselective S-oxygenation of cimetidine. Drug Metab Dispos. 1993 Jul-Aug; 21(4):587-97.
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      159. Wu X, Hui AC, Giacomini KM. Formycin B elimination from the cerebrospinal fluid of the rat. Pharm Res. 1993 Apr; 10(4):611-5.
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      161. Chang SW, Dutton D, Wang HL, He LS, Stearns R, Hui A, Giacomini KM, Ortiz de Montellano P, Voelkel NF. Intact lung cytochrome P-450 is not required for hypoxic pulmonary vasoconstriction. Am J Physiol. 1992 Oct; 263(4 Pt 1):L446-53.
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      173. Chin SK, Hui AC, Giacomini KM. High-performance liquid chromatographic determination of the enantiomers of beta-adrenoceptor blocking agents in biological fluids. II. Studies with atenolol. J Chromatogr. 1989 Apr 14; 489(2):438-45.
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      175. Boyd RA, Chin SK, Don-Pedro O, Williams RL, Giacomini KM. The pharmacokinetics of the enantiomers of atenolol. Clin Pharmacol Ther. 1989 Apr; 45(4):403-10.
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      176. Boyd RA, Giacomini JC, Giacomini KM. Species differences in the negative inotropic response of 1,4-dihydropyridine calcium channel blockers in myocardium. J Cardiovasc Pharmacol. 1988 Dec; 12(6):650-7.
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      177. Whittico MT, Giacomini KM. Cimetidine elimination from the cerebrospinal fluid of the rat. Pharm Res. 1988 Oct; 5(10):628-33.
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      180. Valdivieso L, Giacomini KM, Nelson WL, Pershe R, Blaschke TF. Stereoselective binding of disopyramide to plasma proteins. Pharm Res. 1988 May; 5(5):316-8.
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      181. Gisclon LG, Giacomini KM. Inhibition of cimetidine transport by creatinine in luminal membrane vesicles prepared from rabbit kidney. Drug Metab Dispos. 1988 Mar-Apr; 16(2):331-2.
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      182. Hsyu PH, Gisclon LG, Hui AC, Giacomini KM. Interactions of organic anions with the organic cation transporter in renal BBMV. Am J Physiol. 1988 Jan; 254(1 Pt 2):F56-61.
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      185. Hsyu PH, Giacomini KM. Essential tyrosine residues in transport of organic cations in renal BBMV. Am J Physiol. 1987 Jun; 252(6 Pt 2):F1065-72.
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      187. Theodore LJ, Nelson WL, Zobrist RH, Giacomini KM, Giacomini JC. Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil. J Med Chem. 1986 Sep; 29(9):1789-92.
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      188. Zobrist RH, Giacomini KM, Nelson WL, Giacomini JC. The interaction of phenylalkylamine calcium channel blockers with the 1,4-dihydropyridine binding site. J Mol Cell Cardiol. 1986 Sep; 18(9):963-74.
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      189. Giacomini KM, Nelson WL, Pershe RA, Valdivieso L, Turner-Tamiyasu K, Blaschke TF. In vivo interaction of the enantiomers of disopyramide in human subjects. J Pharmacokinet Biopharm. 1986 Aug; 14(4):335-56.
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      190. Hsyu PH, Giacomini KM. High performance liquid chromatographic determination of the enantiomers of beta-adrenoceptor blocking agents in biological fluids. I: Studies with pindolol. J Pharm Sci. 1986 Jun; 75(6):601-5.
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      191. Giacomini JC, Nelson WL, Wong FM, Boyd R, Zobrist RH, Giacomini KM. Stereoselective interactions of 2-[(2',6'-dimethoxyphenoxyethyl)aminomethyl]-1,4-benzodioxane (WB-4101) with the calcium channel. Biochem Pharmacol. 1986 Feb 15; 35(4):716-8.
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      192. Hsyu PH, Giacomini KM. Stereoselective renal clearance of pindolol in humans. J Clin Invest. 1985 Nov; 76(5):1720-6.
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      193. Giacomini JC, Giacomini KM, Nelson WL, Harrison DC, Blaschke TF. Electrophysiology of the enantiomers of disopyramide in dogs. J Cardiovasc Pharmacol. 1985 Sep-Oct; 7(5):884-90.
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      194. Giacomini JC, Nelson WL, Theodore L, Wong FM, Rood D, Giacomini KM. The pharmacokinetics and pharmacodynamics of d- and dl-verapamil in rabbits. J Cardiovasc Pharmacol. 1985 May-Jun; 7(3):469-75.
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      195. Giacomini KM, Massoud N, Wong FM, Giacomini JC. Decreased binding of verapamil to plasma proteins in patients with liver disease. J Cardiovasc Pharmacol. 1984 Sep-Oct; 6(5):924-8.
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      196. Smith GA, Giacomini KM, Smith CT, Gregory PB, Robinson WS, Merigan TC, Blaschke TF. High-performance liquid chromatographic analysis of hypoxanthine arabinoside in plasma. J Chromatogr. 1984 May 11; 307(2):410-5.
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      197. Giacomini KM, Blaschke TF. Effect of concentration-dependent binding to plasma proteins on the pharmacokinetics and pharmacodynamics of disopyramide. Clin Pharmacokinet. 1984 Jan; 9 Suppl 1:42-8.
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      198. Schulz P, Turner-Tamiyasu K, Smith G, Giacomini KM, Blaschke TF. Amitriptyline disposition in young and elderly normal men. Clin Pharmacol Ther. 1983 Mar; 33(3):360-6.
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      199. Schulz P, Abang A, Giacomini JC, Blaschke TF, Giacomini KM. Effect of heparin on the red blood cell-to-plasma concentration ratio of diphenylhydantoin and prazosin. Ther Drug Monit. 1983; 5(4):497-9.
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      200. Schulz P, Giacomini KM, Luttrell S, Turner-Tamiyasu K, Blaschke TF. Effect of low doses of heparin on the plasma binding of phenytoin and prazosin in normal man. Eur J Clin Pharmacol. 1983; 25(2):211-4.
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      201. Giacomini KM, Abang A, Blaschke TF. Calculation of drug concentration in plasma after equilibrium dialysis. Br J Clin Pharmacol. 1982 Nov; 14(5):752-4.
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      202. Pollick C, Giacomini KM, Blaschke TF, Nelson WL, Turner-Tamiyasu K, Briskin V, Popp RL. The cardiac effects of d- and l-disopyramide in normal subjects: a noninvasive study. Circulation. 1982 Aug; 66(2):447-53.
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      203. Smith GA, Schulz P, Giacomini KM, Blaschke TF. High-pressure liquid chromatographic determination of amitriptyline and its major metabolites in human whole blood. J Pharm Sci. 1982 May; 71(5):581-3.
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      204. Swezey SF, Giacomini KM, Abang A, Brass C, Stevens DA, Blaschke TF. Measurement of ketoconazole, a new antifungal agent, by high-performance liquid chromatography. J Chromatogr. 1982 Feb 12; 227(2):510-5.
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      205. Giacomini KM, Swezey SE, Turner-Tamiyasu K, Blaschke TF. The effect of saturable binding to plasma proteins on the pharmacokinetic properties of disopyramide. J Pharmacokinet Biopharm. 1982 Feb; 10(1):1-14.
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      206. Nelson WL, Sneed CK, Giacomini KM, Giacomini JC, Stauss J, Blaschke TF, Cox BM. Synthesis and anticholinergic properties of the enantiomers of 4-(isopropylamino)-2-(2-pyridyl)-2-phenylbutyramide, the mono-N-dealkylated metabolite of disopyramide. J Med Chem. 1981 May; 24(5):614-7.
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      207. Giacomini KM, Roberts SM, Levy G. Evaluation of methods for producing renal dysfunction in rats. J Pharm Sci. 1981 Feb; 70(2):117-21.
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      208. Giacomini KM, Giacomini JC, Blaschke TF. Absence of effect of heparin on the binding of prazosin and phenytoin to plasma proteins. Biochem Pharmacol. 1980 Dec; 29(24):3337-40.
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      209. Giacomini KM, Giacomini JC, Swezey SE, Harrison DC, Nelson WL, Burke TR, Blaschke TF. The stereoselective disposition of disopyramide in the dog. J Cardiovasc Pharmacol. 1980 Nov-Dec; 2(6):825-32.
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      210. Giacomini KM, Cox BM, Blaschke TF. Comparative anticholinergic potencies of R- and S- disopyramide in longitudinal muscle strips from guinea pig ileum. Life Sci. 1980 Sep 29; 27(13):1191-7.
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      211. Giacomini KM, Giacomini JC, Gibson TP, Levy G. Propoxyphene and norpropoxyphene plasma concentrations after oral propoxyphene in cirrhotic patients with and without surgically constructed portacaval shunt. Clin Pharmacol Ther. 1980 Sep; 28(3):417-24.
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      212. Giacomini KM, Swezey SE, Giacomini JC, Blaschke TF. Administration of heparin causes in vitro release of non-esterified fatty acids in human plasma. Life Sci. 1980 Sep 1; 27(9):771-80.
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      213. Giacomini KM, Nakeeb SM, Levy G. Pharmacokinetic studies of propoxyphene I:Effect of portacaval shunt on systemic availability in dogs. J Pharm Sci. 1980 Jul; 69(7):786-9.
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      214. Gibson TP, Giacomini KM, Briggs WA, Whitman W, Levy G. Propoxyphene and norpropoxyphene plasma concentrations in the anephric patient. Clin Pharmacol Ther. 1980 May; 27(5):665-70.
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      215. Giacomini KM, Gibson TP, Levy G. Effect of hemodialysis on propoxyphene and norpropoxyphene concentrations in blood of anephric patients. Clin Pharmacol Ther. 1980 Apr; 27(4):508-14.
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      216. Levy G, Giacomini KM. Rational aspirin dosage regimens. Clin Pharmacol Ther. 1978 Mar; 23(3):247-52.
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