K M Giacomini

Summary

Affiliation: University of California
Country: USA

Publications

  1. doi request reprint International Transporter Consortium commentary on clinically important transporter polymorphisms
    K M Giacomini
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 94:23-6. 2013
  2. ncbi request reprint Pharmacogenomics and patient care: one size does not fit all
    Kathleen M Giacomini
    Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, San Francisco, CA 94143, USA
    Sci Transl Med 4:153ps18. 2012
  3. pmc Role of organic cation transporter 1, OCT1 in the pharmacokinetics and toxicity of cis-diammine(pyridine)chloroplatinum(II) and oxaliplatin in mice
    Shuanglian Li
    Department of Bioengineering and Therapeutic Sciences, University of California, 1550 4th Street, San Francisco, California 94158, USA
    Pharm Res 28:610-25. 2011
  4. ncbi request reprint The pharmacogenetics research network: from SNP discovery to clinical drug response
    K M Giacomini
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 81:328-45. 2007
  5. pmc Organic anion transporter 2 (SLC22A7) is a facilitative transporter of cGMP
    Cheryl D Cropp
    Department of Biopharmaceutical Sciences, 1550 4th Street, RH584, Box 2911, University of California, San Francisco, CA 94158 2911, USA
    Mol Pharmacol 73:1151-8. 2008
  6. ncbi request reprint Arginine 454 and lysine 370 are essential for the anion specificity of the organic anion transporter, rOAT3
    B Feng
    Department of Biopharmaceutical Sciences and Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 94143, USA
    Biochemistry 40:5511-20. 2001
  7. pmc Functional characterization of liver enhancers that regulate drug-associated transporters
    M J Kim
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 89:571-8. 2011
  8. pmc Genetic and epigenetic regulation of the organic cation transporter 3, SLC22A3
    L Chen
    Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, CA 94158, USA
    Pharmacogenomics J 13:110-20. 2013
  9. doi request reprint The UCSF-FDA TransPortal: a public drug transporter database
    K M Morrissey
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, USA
    Clin Pharmacol Ther 92:545-6. 2012
  10. ncbi request reprint Molecular cloning of a Na+-dependent nucleoside transporter from rabbit intestine
    K M Gerstin
    Department of Biopharmaceutical Sciences, University of California, San Francisco 94143 0446, USA
    Pharm Res 17:906-10. 2000

Collaborators

Detail Information

Publications77

  1. doi request reprint International Transporter Consortium commentary on clinically important transporter polymorphisms
    K M Giacomini
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 94:23-6. 2013
    ..Recommendations for incorporating studies of transporter polymorphisms in drug development are provided, along with the regulatory implications...
  2. ncbi request reprint Pharmacogenomics and patient care: one size does not fit all
    Kathleen M Giacomini
    Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, San Francisco, CA 94143, USA
    Sci Transl Med 4:153ps18. 2012
    ..Here, we describe the status of the field and approaches for addressing some of the open questions in pharmacogenomics research and use of genetic testing in guiding drug therapy...
  3. pmc Role of organic cation transporter 1, OCT1 in the pharmacokinetics and toxicity of cis-diammine(pyridine)chloroplatinum(II) and oxaliplatin in mice
    Shuanglian Li
    Department of Bioengineering and Therapeutic Sciences, University of California, 1550 4th Street, San Francisco, California 94158, USA
    Pharm Res 28:610-25. 2011
    ....
  4. ncbi request reprint The pharmacogenetics research network: from SNP discovery to clinical drug response
    K M Giacomini
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 81:328-45. 2007
    ..Seven major topics are included: informatics (PharmGKB), cardiovascular, pulmonary, addiction, cancer, transport, and metabolism...
  5. pmc Organic anion transporter 2 (SLC22A7) is a facilitative transporter of cGMP
    Cheryl D Cropp
    Department of Biopharmaceutical Sciences, 1550 4th Street, RH584, Box 2911, University of California, San Francisco, CA 94158 2911, USA
    Mol Pharmacol 73:1151-8. 2008
    ..We conclude that hOAT2 is a highly efficient, facilitative transporter of cGMP and may be involved in cGMP signaling in many tissues. Our study suggests that hOAT2 represents a potential new drug target for regulating cGMP levels...
  6. ncbi request reprint Arginine 454 and lysine 370 are essential for the anion specificity of the organic anion transporter, rOAT3
    B Feng
    Department of Biopharmaceutical Sciences and Department of Pharmaceutical Chemistry, School of Pharmacy, University of California, San Francisco 94143, USA
    Biochemistry 40:5511-20. 2001
    ..The studies provide the first insights into the molecular determinants that are critical for recognition and translocation of organic anions by a member of the organic anion transporter family...
  7. pmc Functional characterization of liver enhancers that regulate drug-associated transporters
    M J Kim
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 89:571-8. 2011
    ..This work provides a general model for the rapid characterization of liver enhancers and identifies associations between enhancer variants and drug response...
  8. pmc Genetic and epigenetic regulation of the organic cation transporter 3, SLC22A3
    L Chen
    Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, CA 94158, USA
    Pharmacogenomics J 13:110-20. 2013
    ..Aberrant methylation contributes to the reduced expression of OCT3 in prostate cancer...
  9. doi request reprint The UCSF-FDA TransPortal: a public drug transporter database
    K M Morrissey
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, USA
    Clin Pharmacol Ther 92:545-6. 2012
    ..In this article, we inform the scientific community about the UCSF-FDA TransPortal, a new and valuable online resource for research and drug development...
  10. ncbi request reprint Molecular cloning of a Na+-dependent nucleoside transporter from rabbit intestine
    K M Gerstin
    Department of Biopharmaceutical Sciences, University of California, San Francisco 94143 0446, USA
    Pharm Res 17:906-10. 2000
    ..The goal of the present study was to clone the nucleoside transporters present in rabbit, an important preclinical animal model, and to functionally characterize the clone(s)...
  11. ncbi request reprint Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin
    T J Urban
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 83:416-21. 2008
    ..These results provide clinical evidence of the role of genetic variation in renal drug transporters in active drug secretion in vivo...
  12. ncbi request reprint Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A)
    L Zhang
    Department of Biopharmaceutical Sciences, University of California, San Francisco, California 94143, USA
    J Biol Chem 272:16548-54. 1997
    ..These studies demonstrate the presence of a functional, alternatively spliced organic cation transporter (rOCT1A) in rat kidney...
  13. pmc The effect of novel promoter variants in MATE1 and MATE2 on the pharmacokinetics and pharmacodynamics of metformin
    S L Stocker
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 93:186-94. 2013
    ..These findings suggest that promoter variants of MATE1 and MATE2 are important determinants of metformin disposition and response in healthy volunteers and diabetic patients...
  14. doi request reprint Profiling solute carrier transporters in the human blood-brain barrier
    E G Geier
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 94:636-9. 2013
    ..In this work, expression profiling of 359 SLC transporters, comparative expression analysis with kidney and liver, and immunoassays in brain microvessels (BMVs) identified previously unknown transporters at the human BBB. ..
  15. ncbi request reprint Localization of GFP-tagged concentrative nucleoside transporters in a renal polarized epithelial cell line
    L M Mangravite
    Department of Biopharmaceutical Sciences, Cardiovascular Research Institute, University of California-San Francisco, San Francisco, CA 94143-0446, USA
    Am J Physiol Renal Physiol 280:F879-85. 2001
    ..Apical localization of these transporters suggests a role in renal nucleoside reabsorption and regulation of tubular function via the adenosine pathway...
  16. pmc Discovery of regulatory elements in human ATP-binding cassette transporters through expression quantitative trait mapping
    P Matsson
    Department of Bioengineering and Therapeutic Sciences, University of California San Francisco, San Francisco, CA, USA
    Pharmacogenomics J 12:214-26. 2012
    ..Several of the associations were experimentally validated in reporter assays. Through influencing ABC expression levels, these single-nucleotide polymorphisms may affect disease susceptibility and response to drugs...
  17. ncbi request reprint A novel proton-dependent nucleoside transporter, CeCNT3, from Caenorhabditis elegans
    G Xiao
    Department of Biopharmaceutical Sciences, School of Pharmacy, University of California, San Francisco, San Francisco, California, USA
    Mol Pharmacol 59:339-48. 2001
    ..The broad nucleoside specificity of CeCNT3 may be explained by this and other residues that restrict purine and pyrimidine nucleoside uptake and that discriminate among pyrimidine nucleosides...
  18. pmc Genetic variation in drug transporters in ethnic populations
    C D Cropp
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 84:412-6. 2008
  19. ncbi request reprint Molecular cloning and functional expression of a rabbit renal organic cation transporter
    S Terashita
    Department of Biopharmaceutical Sciences, University of California, San Francisco 94143, USA
    Biochim Biophys Acta 1369:1-6. 1998
    ..rbOCT1 mRNA transcripts are expressed in the kidney, liver, and intestine...
  20. pmc The pharmacogenomics of membrane transporters project: research at the interface of genomics and transporter pharmacology
    D L Kroetz
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 87:109-16. 2010
    ..At the crossroads of pharmacogenomics and transporter biology is the National Institutes of Health-funded Pharmacogenomics of Membrane Transporters (PMT) project, centered at the University of California, San Francisco...
  21. ncbi request reprint Functional analysis of genetic variants in the human concentrative nucleoside transporter 3 (CNT3; SLC28A3)
    I Badagnani
    Department of Biopharmaceutical Sciences, University of California, San Francisco, CA 94143 0446, USA
    Pharmacogenomics J 5:157-65. 2005
    ..The genetic analysis and functional characterization of CNT3 variants suggest that this transporter does not tolerate nonsynonymous changes and is important for human fitness...
  22. ncbi request reprint Transporters involved in the elimination of drugs in the kidney: organic anion transporters and organic cation transporters
    M J Dresser
    Department of Biopharmaceutical Sciences, University of California San Francisco, 513 Parnassus Avenue, S-926, San Francisco, CA 94143-0446, USA
    J Pharm Sci 90:397-421. 2001
    ..With the development of new assays, reagents, and experimental methods, we will soon have a better understanding of the roles of each transporter isoform in the renal elimination of drugs...
  23. ncbi request reprint Functional characterization and haplotype analysis of polymorphisms in the human equilibrative nucleoside transporter, ENT2
    Ryan P Owen
    Department of Biopharmaceutical Sciences, University of California, San Francisco, California 94158, USA
    Drug Metab Dispos 34:12-5. 2006
    ..The low overall genetic diversity in SLC29A2 makes it unlikely that variation in the coding region contributes significantly to clinically observed differences in drug response...
  24. ncbi request reprint Sequence diversity and haplotype structure in the human ABCB1 (MDR1, multidrug resistance transporter) gene
    Deanna L Kroetz
    Department of Biopharmaceutical Sciences, University of California San Francisco, 513 Parnassus Avenue, San Francisco, CA 94143 0446, USA
    Pharmacogenetics 13:481-94. 2003
    ....
  25. doi request reprint Genetic variation in human P450 oxidoreductase
    Walter L Miller
    Department of Pediatrics, University of California, San Francisco, United States
    Mol Cell Endocrinol 300:180-4. 2009
    ..A503V reduces both activities of P450c17 in half, but had no effect on CYP1A2 or 2C19. POR variants are a previously unappreciated source of genetic variation in patterns of steroid synthesis and drug metabolism...
  26. ncbi request reprint Localization of human equilibrative nucleoside transporters, hENT1 and hENT2, in renal epithelial cells
    Lara M Mangravite
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, California 94143 0446, USA
    Am J Physiol Renal Physiol 284:F902-10. 2003
    ..These data suggest that hENT1 and hENT2 on the basolateral membrane function with concentrative nucleoside transporters on the apical membrane to mediate active reabsorption of nucleosides within the kidney...
  27. ncbi request reprint Genetic analysis and functional characterization of polymorphisms in the human concentrative nucleoside transporter, CNT2
    Ryan P Owen
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, California, USA
    Pharmacogenet Genomics 15:83-90. 2005
    ..However, CNT2-F355S (3% allele frequency in the African-American sample) was found to alter specificity for naturally occurring nucleosides, which may have implications for nucleoside homeostasis...
  28. ncbi request reprint The concentrative nucleoside transporter family, SLC28
    Jennifer H Gray
    Department of Biopharmaceutical Sciences, University of California San Francisco, 513 Parnassus Ave, S 926, San Francisco, CA 94143 0446, USA
    Pflugers Arch 447:728-34. 2004
    ..Further, this family is involved in the absorption and disposition of many nucleoside analogs. Several CNT single nucleoside polymorphisms (SNPs) have been identified, but have yet to be characterized...
  29. pmc Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics
    Y Shu
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 83:273-80. 2008
    ..Our studies suggest that OCT1 genotype is a determinant of metformin pharmacokinetics...
  30. ncbi request reprint Screening a large reference sample to identify very low frequency sequence variants: comparisons between two genes
    C E Glatt
    Neurogenetics Laboratory, Program in Human Genetics, University of California San Francisco, San Francisco, California, USA
    Nat Genet 27:435-8. 2001
    ..Both genes have unique roles in neuronal transmission, and variants in either gene might be associated with neurobehavioral phenotypes...
  31. ncbi request reprint Cloning and functional expression of a human liver organic cation transporter
    L Zhang
    Department of Biopharmaceutical Sciences, University of California San Francisco 94143, USA
    Mol Pharmacol 51:913-21. 1997
    ..The functional expression of hOCT1 will provide a powerful tool for elucidation of the mechanisms of organic cation transport in the human liver and understanding of the mechanisms involved in the disposition and hepatotoxicity of drugs...
  32. pmc Genetic variants of human organic anion transporter 4 demonstrate altered transport of endogenous substrates
    James E Shima
    Dept of Bioengineering and Therapeutics Sciences, University of California, San Francisco, California 94143 2911, USA
    Am J Physiol Renal Physiol 299:F767-75. 2010
    ....
  33. ncbi request reprint Molecular determinants of specificity for synthetic nucleoside analogs in the concentrative nucleoside transporter, CNT2
    Ryan P Owen
    Department of Biopharmaceutical Sciences, The University of California, San Francisco, San Francisco, California 94158, USA
    J Biol Chem 281:26675-82. 2006
    ..Our data are consistent with a model in which an increased capability for hydrogen bonding in critical amino acids that reside in the C terminus of rCNT2 contributes to its enhanced selectivity for 2CdA...
  34. ncbi request reprint Polymorphisms in a human kidney xenobiotic transporter, OCT2, exhibit altered function
    Maya K Leabman
    Department of Biopharmaceutical Sciences, Program in Human Genetics, University of California, San Francisco, CA 94143 0443, USA
    Pharmacogenetics 12:395-405. 2002
    ..This selection may be due to a necessary role of OCT2 in the renal elimination of endogenous amines or xenobiotics, including environmental toxins, neurotoxic amines and therapeutic drugs...
  35. ncbi request reprint Nucleoside transporters in the disposition and targeting of nucleoside analogs in the kidney
    Lara M Mangravite
    Department of Biopharmaceutical Sciences, University of California, San Francisco, 513 Parnassus Avenue, San Francisco, CA 94143 0446, USA
    Eur J Pharmacol 479:269-81. 2003
    ..This review examines the role that these transporters play in renal disposition of nucleosides and nucleoside analogs in both systemic and kidney-specific therapies...
  36. ncbi request reprint Role of aromatic transmembrane residues of the organic anion transporter, rOAT3, in substrate recognition
    Bo Feng
    Department of Biopharmaceutical Sciences, School of Pharmacy, University of California San Francisco, San Francisco, CA 94143 0446, USA
    Biochemistry 41:8941-7. 2002
    ..Aromatic residues in this pocket may interact directly with substrates of rOAT3 through hydrogen bonds and pi-pi interactions...
  37. ncbi request reprint Functional characteristics and steroid hormone-mediated regulation of an organic cation transporter in Madin-Darby canine kidney cells
    Y Shu
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California 94143 0446, USA
    J Pharmacol Exp Ther 299:392-8. 2001
    ..Furthermore, our data demonstrate that steroid hormones induce the transcription of OCT2 in the kidney...
  38. pmc Transport of thyroid hormones is selectively inhibited by 3-iodothyronamine
    Alexandra G Ianculescu
    Department of Biochemistry and Biophysics, University of California at San Francisco, San Francisco, California, USA
    Mol Biosyst 6:1403-10. 2010
    ..Given that OATP1A2, OATP1C1, and MCT8 are all present in the brain, T(1)AM may play an important role in modulating thyroid hormone delivery and activity in specific target regions in the central nervous system...
  39. pmc Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1
    Yan Shu
    Department of Biopharmaceutical Sciences, Division of Clinical Pharmacology and Experimental Therapeutics, University of California, San Francisco, CA 94143 0446, USA
    Proc Natl Acad Sci U S A 100:5902-7. 2003
    ....
  40. ncbi request reprint Specificity of human and rat orthologs of the concentrative nucleoside transporter, SPNT
    Karin M Gerstin
    Department of Biopharmaceutical Sciences, University of California, San Francisco, California 94143, USA
    Am J Physiol Renal Physiol 283:F344-9. 2002
    ..These data suggest that there are notable species differences in the specificity of SPNT for synthetic nucleoside analogs...
  41. ncbi request reprint Functional and genetic diversity in the concentrative nucleoside transporter, CNT1, in human populations
    Jennifer H Gray
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, CA 94143 0446, USA
    Mol Pharmacol 65:512-9. 2004
    ..3 +/- 1.5 microM for CNT1-Val189Ile, p<0.05). These data suggest that common genetic variants of CNT1 may contribute to variation in systemic and intracellular levels of anti-cancer nucleoside analogs...
  42. pmc Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function
    Ying Chen
    Division of Clinical Pharmacology and Experimental Therapeutics, Department of Biopharmaceutical Sciences, University of California at San Francisco, San Francisco, CA 94158, USA
    Pharmacogenomics J 9:127-36. 2009
    ..These data suggest that nonsynonymous variants in hMATE1 may alter drug disposition and ultimately affect clinical drug response...
  43. pmc Organic cation transporters are determinants of oxaliplatin cytotoxicity
    Shuzhong Zhang
    Department of Biopharmaceutical Sciences, Comprehensive Cancer Center, University of California at San Francisco, San Francisco, CA 94158, USA
    Cancer Res 66:8847-57. 2006
    ..The development of new anticancer drugs, specifically targeted to OCTs, represents a novel strategy for targeted drug therapy. The results of the present structure-activity studies indicate specific tactics for realizing this goal...
  44. pmc Identification and characterization of 3-iodothyronamine intracellular transport
    Alexandra G Ianculescu
    Department of Biochemistry and Biophysics, University of California, San Francisco, San Francisco, California 94143, USA
    Endocrinology 150:1991-9. 2009
    ..This type of transporter small interfering RNA screening approach can be used in general to identify the constellation of transporters that participate in the intracellular disposition of compounds...
  45. pmc Functional genetic variation in the basal promoter of the organic cation/carnitine transporters OCTN1 (SLC22A4) and OCTN2 (SLC22A5)
    Harunobu Tahara
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, CA 94158 2911, USA
    J Pharmacol Exp Ther 329:262-71. 2009
    ..However, there were significant effects of gender on carnitine plasma levels (p < 0.01). Further in vivo studies of OCTN2 promoter variants on carnitine disposition and variation in drug response are warranted...
  46. pmc Novel variants in human Aquaporin-4 reduce cellular water permeability
    MARCO D SORANI
    Program in Biological and Medical Informatics, University of California, San Francisco, San Francisco, CA 94110, USA
    Hum Mol Genet 17:2379-89. 2008
    ..Our experiments provide insight into the function of the AQP4 protein. These nsSNPs may have clinical implications for patients with cerebral edema and related disorders...
  47. ncbi request reprint Na(+)-dependent purine nucleoside transporter from human kidney: cloning and functional characterization
    J Wang
    Department of Biopharmaceutical Sciences, University of California, San Francisco 94143, USA
    Am J Physiol 273:F1058-65. 1997
    ..In contrast, rat SPNT transcripts are absent in kidney and highly localized to liver and intestine. The hSPNT1 gene was localized to chromosome 15. This is the first demonstration of a purine nucleoside transporter in human kidney...
  48. doi request reprint Transporters in drug development and clinical pharmacology
    K M Giacomini
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA
    Clin Pharmacol Ther 94:3-9. 2013
    ..Importantly, transporters may represent the rate-determining step of drug absorption, distribution, and elimination in the intestine, liver, kidney, and blood-brain barrier (BBB), and they are often the sites of drug-drug interactions...
  49. pmc Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin
    Ying Chen
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, California 94158, USA
    Pharmacogenet Genomics 19:497-504. 2009
    ..The goal of this study was to determine the effect of a genetic variant in the organic cation transporter 2 (OCT2), OCT2-808G/T, which results in an amino acid change, A270S, on the pharmacokinetics of the antidiabetic drug, metformin...
  50. pmc Genetic variation in the proximal promoter of ABC and SLC superfamilies: liver and kidney specific expression and promoter activity predict variation
    Stephanie E Hesselson
    Cardiovascular Research Institute, University of California San Francisco, San Francisco, California, United States of America
    PLoS ONE 4:e6942. 2009
    ..Collectively, these results suggest that the proximal promoter region of membrane transporters is rich in variation and that variants in these regions may play a role in interindividual variation in drug disposition and response...
  51. ncbi request reprint Functional characterization in yeast of genetic variants in the human equilibrative nucleoside transporter, ENT1
    Douglas H Osato
    Department of Biopharmaceutical Sciences, University of California San Francisco, San Francisco, California 94143 0446, USA
    Pharmacogenetics 13:297-301. 2003
    ..These results, together with the observation that there are few haplotypes of ENT1, indicate that coding region variants of ENT1 do not contribute to inter-individual differences in response to nucleoside analog drugs...
  52. pmc The human multidrug resistance protein 4 (MRP4, ABCC4): functional analysis of a highly polymorphic gene
    Nada Abla
    Department of Biopharmaceutical Sciences, University of California, San Francisco, California, USA
    J Pharmacol Exp Ther 325:859-68. 2008
    ..Further studies are required to assess the clinical significance of this altered function and expression and to evaluate substrate specificity of this functional change...
  53. pmc Functional genomics of membrane transporters in human populations
    Thomas J Urban
    Department of Biopharmaceutical Sciences, San Francisco, CA 94143, USA
    Genome Res 16:223-30. 2006
    ..These variants and the reduced function variants provide plausible candidates for disease susceptibility or variation in clinical drug response...
  54. ncbi request reprint Sorting of rat SPNT in renal epithelium is independent of N-glycosylation
    Lara M Mangravite
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, California 94143 0446, USA
    Pharm Res 20:319-23. 2003
    ..Preliminary studies suggested that glycosylation affects surface expression of SPNT but not CNT1...
  55. ncbi request reprint The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics
    Andrew R Erdman
    Department of Biopharmaceutical Sciences, University of California, San Francisco 94143 0446, USA
    Am J Physiol Renal Physiol 290:F905-12. 2006
    ..This variant exhibited a reduced ability to transport ES, but a preserved ability to transport CIM. These data suggest that genetic variation in OAT3 may contribute to variation in the disposition of drugs...
  56. ncbi request reprint Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants
    Ilaria Badagnani
    Department of Biopharmaceutical Sciences, University of California, 1550 4th Street, Box 2911, San Francisco, CA 94158, USA
    J Pharmacol Exp Ther 318:521-9. 2006
    ..Furthermore, genetic variation in OATP1A2 may contribute to variation in MTX disposition and response...
  57. pmc Identification and characterization of proximal promoter polymorphisms in the human concentrative nucleoside transporter 2 (SLC28A2)
    Sook Wah Yee
    Department of Biopharmaceutical Sciences, University of California, 1550 4th Street, RH584, Box 2911, San Francisco, CA 94158 2911, USA
    J Pharmacol Exp Ther 328:699-707. 2009
    ..This SNP may play a role in variation in the pharmacokinetics and pharmacological effects of nucleoside analogs...
  58. pmc Interactions of tyrosine kinase inhibitors with organic cation transporters and multidrug and toxic compound extrusion proteins
    Tsuyoshi Minematsu
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, 1550 4th Street, San Francisco, CA 94158, USA
    Mol Cancer Ther 10:531-9. 2011
    ..The study provides the basis for further clinical DDI studies with TKIs...
  59. ncbi request reprint Transport of drugs in the kidney by the human organic cation transporter, OCT2 and its genetic variants
    Tomoe Fujita
    Department of Biopharmaceutical Sciences, University of California San Francisco, USA
    J Pharm Sci 95:25-36. 2006
    ..A variety of structurally diverse compounds have been shown to interact with OCT2, including endogenous compounds, drugs, and dietary supplements...
  60. ncbi request reprint Transport of paraquat by human organic cation transporters and multidrug and toxic compound extrusion family
    Ying Chen
    Department of Biopharmaceutical Sciences, University of California, San Francisco, 1550 4th St, San Francisco, CA 94158, USA
    J Pharmacol Exp Ther 322:695-700. 2007
    ..These transporters may play an important role in the accumulation and renal excretion of PQ, and they may serve as molecular targets for the prevention and treatment of PQ-induced nephrotoxicity...
  61. ncbi request reprint Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2)
    Mark J Dresser
    Department of Biopharmaceutical Sciences, University of California, San Francisco, 94143 0446, USA
    Pharm Res 19:1244-7. 2002
  62. ncbi request reprint Functional effects of protein sequence polymorphisms in the organic cation/ergothioneine transporter OCTN1 (SLC22A4)
    Thomas J Urban
    Departments of aBiopharmaceutical Sciences, University of California San Francisco, San Francisco, California, USA
    Pharmacogenet Genomics 17:773-82. 2007
    ..Genetic variation in OCTN1 may help to explain interindividual variability in the pharmacokinetics of many cationic or zwitterionic drugs...
  63. pmc Genetic polymorphisms in organic cation transporter 1 (OCT1) in Chinese and Japanese populations exhibit altered function
    Ligong Chen
    Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, CA 94158, USA
    J Pharmacol Exp Ther 335:42-50. 2010
    ..This study suggests that nonsynonymous variants of OCT1 in Chinese and Japanese populations may affect the differential response to metformin...
  64. pmc Organic cation transporters modulate the uptake and cytotoxicity of picoplatin, a third-generation platinum analogue
    Swati S More
    Department of Bioengineering and Therapeutic Sciences, University of California, 1550 4th Street, San Francisco, CA 94158, USA
    Mol Cancer Ther 9:1058-69. 2010
    ..Mol Cancer Ther; 9(4); 1058-69. (c)2010 AACR...
  65. pmc Genetics of P450 oxidoreductase: sequence variation in 842 individuals of four ethnicities and activities of 15 missense mutations
    Ningwu Huang
    Departments of Pediatrics and Biopharmaceutical Sciences, University of California, San Francisco, CA 94143, USA
    Proc Natl Acad Sci U S A 105:1733-8. 2008
    ..The activity of A503V was reduced to a modest but statistically significant degree in all four assays, suggesting that it may play an important role in interindividual variation in drug response...
  66. ncbi request reprint Estimating the contribution of genes and environment to variation in renal drug clearance
    Maya K Leabman
    Department of Biopharmaceutical Sciences, University of California, San Francisco, San Francisco, CA 94143 0446, USA
    Pharmacogenetics 13:581-4. 2003
    ..g. glomerular filtration and passive secretion/reabsorption). The low rGC values of iohexol, digoxin and terodiline suggest that environmental factors may contribute to variation in their renal clearance...
  67. ncbi request reprint Functional analysis of polymorphisms in the organic anion transporter, SLC22A6 (OAT1)
    Tomoe Fujita
    Department of Pharmacology, Kitasato University School of Medicine, Sagamihara, Kanagawa, 228 8555, Japan
    Pharmacogenet Genomics 15:201-9. 2005
    ..The goal of this study was to identify and functionally characterize OAT1 variants as a first step towards understanding whether genetic variation in OAT1 may contribute to interindividual differences in renal elimination of xenobiotics...
  68. pmc Identifying genetic risk factors for serious adverse drug reactions: current progress and challenges
    Russell A Wilke
    Department of Medicine, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, Wisconsin 53226, USA
    Nat Rev Drug Discov 6:904-16. 2007
    ..Key challenges for the discovery of predictive risk alleles for these SADRs are also considered...
  69. ncbi request reprint PharmGKB submission update: IV. PMT submissions of genetic variations in ATP-Binding cassette transporters to the PharmGKB network
    Tan D Nguyen
    Department of Biopharmaceutical Sciences, University of California, San Francisco, USA
    Pharmacol Rev 58:1-2. 2006
  70. ncbi request reprint PharmGKB submission update: V. PMT submissions of genetic variation in SLC22 family transporters
    Yan Shu
    Department of Biopharmaceutical Sciences, University of California, San Francisco, USA
    Pharmacol Rev 58:3-4. 2006
  71. ncbi request reprint PharmGKB submission update: VI. PMT submissions of genetic variations in neurotransmitter transporters (SLC6, SLC17, and SLC18) to the PharmGKB network
    Ilaria Badagnani
    Department of Biopharmaceutical Sciences, University of California, San Francisco, USA
    Pharmacol Rev 58:5-6. 2006
  72. ncbi request reprint Pharmacogenomics: challenges and opportunities
    Dan M Roden
    Vanderbilt University, Nashville, Tennessee, USA
    Ann Intern Med 145:749-57. 2006
    ..Overcoming these challenges holds the promise of improving new drug development and ultimately individualizing the selection of appropriate drugs and dosages for individual patients...
  73. ncbi request reprint PharmGKB update: I. Genetic variants of the organic cation transporter 2 (OCT2, SLC22A2)
    Maya K Leabman
    Pharmacogenetics of Membrane Transporters Group, Department of Biopharmaceutical Sciences, University of California San Francisco, USA
    Pharmacol Rev 55:399. 2003
  74. pmc Creating and evaluating genetic tests predictive of drug response
    Scott T Weiss
    Channing Laboratory, Brigham and Women s Hospital, 181 Longwood Ave, Boston, Massachusetts 02115, USA
    Nat Rev Drug Discov 7:568-74. 2008
    ....
  75. ncbi request reprint Haplotype structure and ethnic-specific allele frequencies at the OCTN locus: implications for the genetics of Crohn's disease
    Thomas J Urban
    Inflamm Bowel Dis 11:78-9. 2005
  76. pmc cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospects
    Katherine S Lovejoy
    Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA
    Proc Natl Acad Sci U S A 105:8902-7. 2008
    ..These exceptional characteristics indicate that cDPCP and related complexes merit consideration as therapeutic options for treating colorectal and other cancers bearing appropriate cation transporters...
  77. pmc Natural variation in human membrane transporter genes reveals evolutionary and functional constraints
    Maya K Leabman
    Department of Biopharmaceutical Sciences, University of California, San Francisco, CA 94143 0446, USA
    Proc Natl Acad Sci U S A 100:5896-901. 2003
    ..In addition, African Americans exhibited a much higher frequency of population specific medium-frequency alleles than did European Americans...