CYP3A4

Summary

Gene Symbol: CYP3A4
Description: cytochrome P450 family 3 subfamily A member 4
Alias: CP33, CP34, CYP3A, CYP3A3, CYPIIIA3, CYPIIIA4, HLP, NF-25, P450C3, P450PCN1, cytochrome P450 3A4, 1,8-cineole 2-exo-monooxygenase, P450-III, steroid inducible, albendazole monooxygenase, albendazole sulfoxidase, cholesterol 25-hydroxylase, cytochrome P450 3A3, cytochrome P450 HLp, cytochrome P450 NF-25, cytochrome P450, family 3, subfamily A, polypeptide 4, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, cytochrome P450-PCN1, glucocorticoid-inducible P450, nifedipine oxidase, quinine 3-monooxygenase, taurochenodeoxycholate 6-alpha-hydroxylase
Species: human

Top Publications

  1. ncbi CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity
    F Sata
    Laboratory of Metabolism, National Cancer Institute, Bethesda, MD 20892, USA
    Clin Pharmacol Ther 67:48-56. 2000
  2. ncbi Novel mutations of CYP3A4 in Chinese
    K P Hsieh
    Department of Pharmacology, National Cheng Kung University, Medical College, 1 University Road, Tainan 70101, Taiwan
    Drug Metab Dispos 29:268-73. 2001
  3. ncbi CYP3A4 and P-glycoprotein activity in healthy controls and transplant patients on cyclosporin vs. tacrolimus vs. sirolimus
    W P D Lemahieu
    Division of Nephrology, University Hospitals Gasthuisberg, University of Leuven, Belgium
    Am J Transplant 4:1514-22. 2004
  4. ncbi Paradoxical role of cytochrome P450 3A in the bioactivation and clinical effects of levo-alpha-acetylmethadol: importance of clinical investigations to validate in vitro drug metabolism studies
    Evan D Kharasch
    Department of Anesthesiology, University of Washington, Seattle, Washington 98195, USA
    Clin Pharmacokinet 44:731-51. 2005
  5. pmc Methadone pharmacokinetics are independent of cytochrome P4503A (CYP3A) activity and gastrointestinal drug transport: insights from methadone interactions with ritonavir/indinavir
    Evan D Kharasch
    Division of Clinical and Translational Research, Department of Anesthesiology, Washington University in St Louis, St Louis, Missouri 63110 1093, USA
    Anesthesiology 110:660-72. 2009
  6. ncbi Recombinant CYP3A4*17 is defective in metabolizing the hypertensive drug nifedipine, and the CYP3A4*17 allele may occur on the same chromosome as CYP3A5*3, representing a new putative defective CYP3A haplotype
    Su Jun Lee
    Human Metabolism Section, Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA
    J Pharmacol Exp Ther 313:302-9. 2005
  7. doi Besides CYP2C19*2, the variant allele CYP2C9*3 is associated with higher on-clopidogrel platelet reactivity in patients on dual antiplatelet therapy undergoing elective coronary stent implantation
    Ankie Harmsze
    Department of Clinical Pharmacy, St Antonius Hospital, Nieuwegein, The Netherlands
    Pharmacogenet Genomics 20:18-25. 2010
  8. pmc Evidence for involvement of human CYP3A in the 3-hydroxylation of quinine
    H Zhang
    School of Pharmacy, University of Otago, Dunedin, New Zealand
    Br J Clin Pharmacol 43:245-52. 1997
  9. ncbi CYP3A5*3 and CYP3A4*18 single nucleotide polymorphisms in a Chinese population
    Yong fang Hu
    Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan 410078, People s Republic of China
    Clin Chim Acta 353:187-92. 2005
  10. ncbi Differences in CYP3A5*3 genotype distribution and combinations with other polymorphisms between Spaniards and Other Caucasian populations
    Guillermo Gervasini
    Department of Pharmacology and Psychiatry, Medical School, and Clinical Pharmacology Unit, Infanta Cristina University Hospital, University of Extremadura, Badajoz, Spain
    Ther Drug Monit 27:819-21. 2005

Research Grants

  1. ALCOHOL-INDUCED HEPATIC P450s IN HCV/HIV OXIDATE INJURY
    STEVEN SHEDLOFSKY; Fiscal Year: 2003
  2. Characterization of a Novel Selective Cytochrome P450 3A5 Substrate
    MICHAEL DARIN CAMERON; Fiscal Year: 2013
  3. Maria Almira Correia; Fiscal Year: 2016
  4. NOVEL HIGH THROUGHPUT PLATFORM FOR SCREENING CYTOCHROME P450 INDUCTION
    MARIA INES MORANO; Fiscal Year: 2013
  5. James R Halpert; Fiscal Year: 2014
  6. PK/PD Issues in the Use of New Therapies for the Treatment of Tuberculosis
    Kelly E Dooley; Fiscal Year: 2013
  7. Mary F Paine; Fiscal Year: 2014
  8. Safety, Efficacy, and Mechanisms in American Ginseng in HIV-Related Fatigue
    Adriana S A Andrade; Fiscal Year: 2012
  9. Activating liver carcinogens in yeast by expressing CYP450 polymorphisms
    MICHAEL THOMAS FASULLO; Fiscal Year: 2010
  10. Does the extreme variability of methadone metabolism have an epigenetic cause?
    Gavin R Schnitzler; Fiscal Year: 2010

Detail Information

Publications254 found, 100 shown here

  1. ncbi CYP3A4 allelic variants with amino acid substitutions in exons 7 and 12: evidence for an allelic variant with altered catalytic activity
    F Sata
    Laboratory of Metabolism, National Cancer Institute, Bethesda, MD 20892, USA
    Clin Pharmacol Ther 67:48-56. 2000
    ..To determine the existence of mutant and variant CgammaP3A4 alleles in three racial groups and to assess functions of the variant alleles by complementary deoxyribonucleic acid (cDNA) expression...
  2. ncbi Novel mutations of CYP3A4 in Chinese
    K P Hsieh
    Department of Pharmacology, National Cheng Kung University, Medical College, 1 University Road, Tainan 70101, Taiwan
    Drug Metab Dispos 29:268-73. 2001
    Human cytochrome P450 3A4 is a major P450 enzyme in the liver and gastrointestinal tract. It plays important roles in the metabolism of a wide variety of drugs, some endogenous steroids, and harmful environmental contaminants...
  3. ncbi CYP3A4 and P-glycoprotein activity in healthy controls and transplant patients on cyclosporin vs. tacrolimus vs. sirolimus
    W P D Lemahieu
    Division of Nephrology, University Hospitals Gasthuisberg, University of Leuven, Belgium
    Am J Transplant 4:1514-22. 2004
    ..A (CsA), tacrolimus (FK506) and sirolimus (Rapa) on the in vivo activity of both intestinal and hepatic cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (PGP) in renal transplant patients...
  4. ncbi Paradoxical role of cytochrome P450 3A in the bioactivation and clinical effects of levo-alpha-acetylmethadol: importance of clinical investigations to validate in vitro drug metabolism studies
    Evan D Kharasch
    Department of Anesthesiology, University of Washington, Seattle, Washington 98195, USA
    Clin Pharmacokinet 44:731-51. 2005
    ..microsomal N-demethylation in vitro is catalysed mainly by cytochrome P450 (CYP) 3A4; however, the role of CYP3A in LAAM disposition in humans in vivo is unknown...
  5. pmc Methadone pharmacokinetics are independent of cytochrome P4503A (CYP3A) activity and gastrointestinal drug transport: insights from methadone interactions with ritonavir/indinavir
    Evan D Kharasch
    Division of Clinical and Translational Research, Department of Anesthesiology, Washington University in St Louis, St Louis, Missouri 63110 1093, USA
    Anesthesiology 110:660-72. 2009
    Methadone clearance is highly variable, and drug interactions are problematic. Both have been attributed to CYP3A, but actual mechanisms are unknown. Drug interactions can provide such mechanistic information...
  6. ncbi Recombinant CYP3A4*17 is defective in metabolizing the hypertensive drug nifedipine, and the CYP3A4*17 allele may occur on the same chromosome as CYP3A5*3, representing a new putative defective CYP3A haplotype
    Su Jun Lee
    Human Metabolism Section, Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, NC 27709, USA
    J Pharmacol Exp Ther 313:302-9. 2005
    ..We previously reported four new CYP3A4 coding variants in three different racial groups...
  7. doi Besides CYP2C19*2, the variant allele CYP2C9*3 is associated with higher on-clopidogrel platelet reactivity in patients on dual antiplatelet therapy undergoing elective coronary stent implantation
    Ankie Harmsze
    Department of Clinical Pharmacy, St Antonius Hospital, Nieuwegein, The Netherlands
    Pharmacogenet Genomics 20:18-25. 2010
    ..Several studies report that the genetic variation in CYP2C19 (*2) is associated with an impaired response to clopidogrel...
  8. pmc Evidence for involvement of human CYP3A in the 3-hydroxylation of quinine
    H Zhang
    School of Pharmacy, University of Otago, Dunedin, New Zealand
    Br J Clin Pharmacol 43:245-52. 1997
    ..metabolism of quinine to form the major metabolite 3-hydroxyquinine is most likely catalysed by human P450 3A (CYP3A)...
  9. ncbi CYP3A5*3 and CYP3A4*18 single nucleotide polymorphisms in a Chinese population
    Yong fang Hu
    Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan 410078, People s Republic of China
    Clin Chim Acta 353:187-92. 2005
    ..Detection of CYP3A5 and CYP3A4 variant alleles and knowledge about their allelic frequency in specific ethnic groups are important to lead to ..
  10. ncbi Differences in CYP3A5*3 genotype distribution and combinations with other polymorphisms between Spaniards and Other Caucasian populations
    Guillermo Gervasini
    Department of Pharmacology and Psychiatry, Medical School, and Clinical Pharmacology Unit, Infanta Cristina University Hospital, University of Extremadura, Badajoz, Spain
    Ther Drug Monit 27:819-21. 2005
    ..The goal of this study was to detect genotypic differences between Spaniards and other related populations regarding CYP3A4*1B, CYP3A5*3, and ABCB1 (MDR1) C3435T polymorphisms...
  11. pmc Genetic polymorphisms in CYP17, CYP3A4, CYP19A1, SRD5A2, IGF-1, and IGFBP-3 and prostate cancer risk in African-American men: the Flint Men's Health Study
    Aruna V Sarma
    Department of Urology, University of Michigan Medical School, Ann Arbor, Michigan, USA
    Prostate 68:296-305. 2008
    ....
  12. doi CYP2C19*2 and CYP2C9*3 alleles are associated with stent thrombosis: a case-control study
    Ankie M Harmsze
    Department of Clinical Pharmacy, St Antonius Hospital, PO Box 2500, Nieuwegein 3430 EM, The Netherlands
    Eur Heart J 31:3046-53. 2010
    ..effect of variations in genes involved in the absorption (ABCB1 C1236T, G2677T/A, C3435T), metabolism (CYP2C19*2 and *3, CYP2C9*2 and *3, CYP3A4*1B and CYP3A5*3), and pharmacodynamics (P2Y1 A1622G) of clopidogrel on the occurrence of ST.
  13. ncbi Human liver microsomal steroid metabolism: identification of the major microsomal steroid hormone 6 beta-hydroxylase cytochrome P-450 enzyme
    D J Waxman
    Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, Massachusetts 02115
    Arch Biochem Biophys 263:424-36. 1988
    ..69-0.83) and with its associated nifedipine oxidase activity (r = 0...
  14. ncbi Gene structure of CYP3A4, an adult-specific form of cytochrome P450 in human livers, and its transcriptional control
    H Hashimoto
    Division of Drug Metabolism, Faculty of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan
    Eur J Biochem 218:585-95. 1993
    ..Nagashima, K. & Kamataki, T. (1990) Biochemistry 29, 4430-4433]. The sequences of three genomic clones for CYP3A4 were analyzed for all exons, exon-intron junctions and the 5'-flanking region from the major transcription site to ..
  15. ncbi Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study
    Jacques Fellay
    Division of Infectious Diseases, University Hospital of Lausanne, Lausanne, Switzerland
    Lancet 359:30-6. 2002
    ..This variability could have a genetic basis. We did a pharmacogenetics study to analyse the association between response to antiretroviral treatment and allelic variants of several genes...
  16. ncbi CYP3A4 variant alleles in white individuals with low CYP3A4 enzyme activity
    Elena Garcia-Martin
    Department of Biochemistry, School of Biological Sciences, University of Extremadura, Badajoz, Spain
    Clin Pharmacol Ther 71:196-204. 2002
    Our objective was to evaluate the presence of CYP3A4 gene variants in white individuals with low CYP3A4 enzyme activity.
  17. ncbi CYP3A4 promoter variant is associated with prostate cancer risk in men with benign prostate hyperplasia
    Mohammed T Tayeb
    Department of Medicine and Therapeutics, University of Aberdeen, Foresterhill, Aberdeen, UK
    Oncol Rep 9:653-5. 2002
    ..Benign prostatic hyperplasia (BPH) is found in the majority of ageing men and has been linked with PRCa. CYP3A4 may influence PRCa through its role in testosterone metabolism...
  18. ncbi Expression of CYP3A4, CYP2B6, and CYP2C9 is regulated by the vitamin D receptor pathway in primary human hepatocytes
    Lionel Drocourt
    INSERM U128, Institut Federatif de Recherche 24, CNRS, 1919 Route de Mende, 34293 Montpellier, Cedex 05, France
    J Biol Chem 277:25125-32. 2002
    The fully active dihydroxylated metabolite of vitamin D(3) induces the expression of CYP3A4 and, to a lesser extent, CYP2B6 and CYP2C9 genes in normal differentiated primary human hepatocytes...
  19. ncbi The CYP3A4*1B polymorphism has no functional significance and is not associated with risk of breast or ovarian cancer
    Amanda B Spurdle
    Cancer and Cell Biology Division, Joint Experimental Oncology Programme, The Queensland Institute of Medical Research and The University of Queensland, Brisbane, Australia
    Pharmacogenetics 12:355-66. 2002
    b>CYP3A4 is involved in the metabolism of endogenous steroids, and an allelic variant, CYP3A4*1B, consisting of an A to G polymorphism within the 5'-flanking region termed the nifedipine-specific response element (NFSE) has been associated ..
  20. ncbi Ethnic differences in the frequency of prostate cancer susceptibility alleles at SRD5A2 and CYP3A4
    C M Zeigler-Johnson
    University of Pennsylvania, Philadelphia, PA, USA
    Hum Hered 54:13-21. 2002
    ..Ethnic differences in genotypes for genes associated with androgen metabolism including SRD5A2 and CYP3A4 also may exist. The aim of this study was to evaluate differences in these genotypes by ethnicity.
  21. ncbi Genetic polymorphisms of the CYP3A4, CYP3A5, and MDR-1 genes and pharmacokinetics of the calcineurin inhibitors cyclosporine and tacrolimus
    Dennis A Hesselink
    Department of Internal Medicine, Renal Tranplant Unit, Erasmus Medical Center, Rotterdam, The Netherlands
    Clin Pharmacol Ther 74:245-54. 2003
    ..The low oral bioavailability of calcineurin inhibitors is thought to result from the actions of the metabolizing enzymes cytochrome P450 (CYP) 3A4 and CYP3A5 and the multidrug efflux pump P-glycoprotein, encoded by MDR-1...
  22. ncbi Pharmacokinetics of citalopram in relation to genetic polymorphism of CYP2C19
    Bang Ning Yu
    Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan 410078, Republic of China
    Drug Metab Dispos 31:1255-9. 2003
    The study was designed to define the contribution of cytochrome p450 2C19 (CYP2C19) and cytochrome p450 3A4 (CYP3A4) to citalopram N-demethylation and to evaluate the relationship between the disposition of citalopram and CYP2C19 ..
  23. ncbi The CYP3A4*1B allele increases risk for small cell lung cancer: effect of gender and smoking dose
    Heike Dally
    Division of Toxicology and Cancer Risk Factors, German Cancer Research Center DKFZ, Heidelberg, Germany
    Pharmacogenetics 13:607-18. 2003
    ..The CYP3A4*1B allele has been associated with a two-fold higher promoter activity and with high-grade prostate cancers...
  24. ncbi CYP3A4 polymorphisms--potential risk factors for breast and prostate cancer: a HuGE review
    Channa Keshava
    Molecular Epidemiology Team, Toxicology and Molecular Biology Branch, National Institute for Occupational Safety and Health, Centers for Disease Control and Prevention, Morgantown, WV 26505 2888, USA
    Am J Epidemiol 160:825-41. 2004
    The steroid hydroxylase CYP3A4 is the most abundant P-450 enzyme in the human liver, and CYP3A enzymes metabolize more than 50% of prescription drugs. The CYP3A4 gene is expressed in the liver, gut, colon, prostate, and breast...
  25. ncbi CYP3A4 is a vitamin D-24- and 25-hydroxylase: analysis of structure function by site-directed mutagenesis
    Ram P Gupta
    Department of Medicine, Medical University of South Carolina, P O Box 250775, Charleston, South Carolina 29425, USA
    J Clin Endocrinol Metab 90:1210-9. 2005
    ..b>CYP3A4, a vitamin D-25-hydroxylase, and CYP1A1 had the highest 24-hydroxylase activity with 1 alpha-hydroxyvitamin D(2) (..
  26. ncbi Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study
    David W Haas
    Program for Human Genetics, Vanderbilt University School of Medicine, 345 24th Avenue North, Nashville, TN 37203, USA
    AIDS 18:2391-400. 2004
    ..Efavirenz is metabolized by cytochrome P4502B6 (CYP2B6). We investigated whether polymorphisms in CYP2B6, CYP3A4, CYP3A5, and MDR1 were associated with efavirenz central nervous system side effects and pharmacokinetics.
  27. ncbi Screening of 12 SNPs of CYP3A4 in a Chinese population using oligonucleotide microarray
    Siyuan Wen
    Beijing Institute of Radiation Medicine, Beijing 100850, P R China
    Genet Test 8:411-6. 2004
    Human cytochrome P450 3A4 (CYP34A) plays an important role in the metabolism of many endo- and xenomaterials. It also exhibits a substantial interindividual variation in enzymatic activity...
  28. pmc CYP3A4 and CYP3A5 genotyping by Pyrosequencing
    Adam A Garsa
    Washington University School of Medicine, Department of Medicine, Division of Oncology, St Louis, MO 63110, USA
    BMC Med Genet 6:19. 2005
    Human cytochrome P450 3A enzymes, particularly CYP3A4 and CYP3A5, play an important role in drug metabolism. CYP3A expression exhibits substantial interindividual variation, much of which may result from genetic variation...
  29. ncbi Influence of CYP3A5 and MDR1 polymorphisms on tacrolimus concentration in the early stage after renal transplantation
    Xin Zhang
    Research Institute of Nephrology, Jinling Hospital, Nanjing University School of Medicine, Nanjing, China
    Clin Transplant 19:638-43. 2005
    ..The objective of this study was to evaluate whether or not CYP3A5*1/*3 or MDR1 C3435T polymorphisms are associated with the tacrolimus concentration per dose...
  30. ncbi Cyp3A4, Cyp3A5, and MDR-1 genetic influences on tacrolimus pharmacokinetics in renal transplant recipients
    Jean Nicholas Roy
    Laboratoire d Immunogénétique, Centre hospitalier de l Université de Montréal CHUM Hôpital Notre Dame, Montreal, Quebec, Canada
    Pharmacogenet Genomics 16:659-65. 2006
    ..b>Cytochrome P450 3A4 (Cyp3A4) and Cyp3A5 are the most important contributors to tacrolimus metabolism while the P-glycoprotein ..
  31. ncbi Systematic screening for polymorphisms in the CYP3A4 gene in the Chinese population
    Jing Du
    Bio X Center, Shanghai Jiaotong University, 1954 Huashan Road, Shanghai 200030, China
    Pharmacogenomics 7:831-41. 2006
    b>Cytochrome P450 3A4 (CYP3A4) is a major CYP enzyme in the liver and intestine. It is involved in the metabolism of over 50% of all drugs currently in use. The present study was designed to determine the genetic basis of CYP3A4 variability.
  32. ncbi Sex-dependent genetic markers of CYP3A4 expression and activity in human liver microsomes
    Markus Schirmer
    Georg August University, Department of Clinical Pharmacology, Gottingen, Germany
    Pharmacogenomics 8:443-53. 2007
    ..To find genetic markers of the individual cytochrome P450 (CYP)3A expression...
  33. ncbi Expression of CYP3A4 as a predictor of response to chemotherapy in peripheral T-cell lymphomas
    Cristina Rodriguez-Antona
    Hereditary Endocrine Cancer Group, Spanish National Cancer Centre, c Melchor Fernandez Almagro no 3, 28029 Madrid, Spain
    Blood 110:3345-51. 2007
    ..were compared with the clinical response and survival of the patients, finding that a high tumoral expression of CYP3A4 was significantly associated with a lower complete remission rate...
  34. doi Post-transcriptional regulation of human pregnane X receptor by micro-RNA affects the expression of cytochrome P450 3A4
    Shingo Takagi
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    J Biol Chem 283:9674-80. 2008
    ..the inducible expression of a variety of transporters and drug-metabolizing enzymes, including CYP3A4 (cytochrome P450 3A4)...
  35. doi Phthalate induction of CYP3A4 is dependent on glucocorticoid regulation of PXR expression
    Beth W Cooper
    Department of Environmental and Molecular Toxicology, North Carolina State University, Raleigh, North Carolina 27695, USA
    Toxicol Sci 103:268-77. 2008
    b>Cytochrome P450 3A4 (CYP3A4) is responsible for oxidative metabolism of more than 60% of all pharmaceuticals...
  36. doi CYP3A7, CYP3A5, CYP3A4, and ABCB1 genetic polymorphisms, cyclosporine concentration, and dose requirement in transplant recipients
    Severine Crettol
    Unité de Biochimie et de Psychopharmacologie Clinique, Centre de Neurosciences Psychiatriques, Departement de Psychiatrie, Centre Hospitalier Universitaire Vaudois et Universite de Lausanne, Hôpital de Cery, Prilly Lausanne, Switzerland
    Ther Drug Monit 30:689-99. 2008
    ..2; 95% confidence interval = 1.4-37.3; P = 0.009). CYP3A4 rs4646437C>T influenced cyclosporine kinetics, the T carriers requiring higher cyclosporine dose...
  37. pmc Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African americans
    David W Haas
    USA
    J Infect Dis 199:872-80. 2009
    ..We characterized associations between genetic polymorphisms and the pharmacokinetics of single doses of nevirapine and efavirenz...
  38. doi Explaining variability in tacrolimus pharmacokinetics to optimize early exposure in adult kidney transplant recipients
    Rogier R Press
    Department of Clinical Pharmacy and Toxicology, Leiden University Medical Center, Albinusdreef 2, Leiden, The Netherlands
    Ther Drug Monit 31:187-97. 2009
    ..albumin concentration, prednisolone dose, TRL dose interval, polymorphisms in genes coding for ABCB1, CYP3A5, CYP3A4, and the pregnane X receptor on TRL pharmacokinetics...
  39. pmc Comprehensive pharmacogenetic analysis of irinotecan neutropenia and pharmacokinetics
    Federico Innocenti
    The University of Chicago, Chicago, IL 60637, USA
    J Clin Oncol 27:2604-14. 2009
    ..We aim to identify genetic variation, in addition to the UGT1A1*28 polymorphism, that can explain the variability in irinotecan (CPT-11) pharmacokinetics and neutropenia in cancer patients...
  40. pmc Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients
    Salvador E Cabrera
    Servicio de Farmacia, Hospital Universitario de Salamanca, Paseo de San Vicente 58, Salamanca, Spain
    Antimicrob Agents Chemother 53:2791-8. 2009
    ..In a subgroup of 32 patients, genetic polymorphisms of the cytochrome P450 2B6 gene (CYP2B6), CYP3A4, and MDR1 were also investigated. Efavirenz oral clearance and the apparent volume of distribution were 9...
  41. pmc Intronic polymorphism in CYP3A4 affects hepatic expression and response to statin drugs
    D Wang
    Department of Pharmacology, Program in Pharmacogenomics, School of Biomedical Science, Ohio State University, Columbus, OH 43210, USA
    Pharmacogenomics J 11:274-86. 2011
    b>Cytochrome P450 3A4 (CYP3A4) metabolizes ∼50% of all clinically used drugs. Although CYP3A4 expression varies widely between individuals, the contribution of genetic factors remains uncertain...
  42. doi A functional polymorphism in the CYP3A4 gene is associated with increased risk of coronary heart disease in the Chinese Han population
    Bao Xia He
    Guangzhou General Hospital of Guangzhou Military Command, 111 Liuhua Road, Guangzhou, Guangdong, China
    Basic Clin Pharmacol Toxicol 108:208-13. 2011
    b>CYP3A4 is a major member of the cytochrome P450 (CYP) enzymes which play crucial roles in cardiovascular diseases. Recently, a novel polymorphism in the CYP3A4 gene, IVS10+12G>A, named CYP3A4*1G (rs2242480), has been identified...
  43. pmc CYP3A4 mediates growth of estrogen receptor-positive breast cancer cells in part by inducing nuclear translocation of phospho-Stat3 through biosynthesis of (±)-14,15-epoxyeicosatrienoic acid (EET)
    Ranjana Mitra
    From the Division of Hematology, Oncology, and Transplantation, University of Minnesota, Minneapolis, Minnesota 55455, USA
    J Biol Chem 286:17543-59. 2011
    b>CYP3A4 expression in breast cancer correlates with decreased overall survival, but the mechanisms are unknown...
  44. doi A new functional CYP3A4 intron 6 polymorphism significantly affects tacrolimus pharmacokinetics in kidney transplant recipients
    Laure Elens
    Department of Clinical Chemistry, Erasmus University Medical Center, Rotterdam, The Netherlands
    Clin Chem 57:1574-83. 2011
    ..Tac pharmacokinetics varies between individuals and thus complicates its use in preventing rejection after kidney transplantation. This variability might be caused by genetic polymorphisms in metabolizing enzymes...
  45. doi The new CYP3A4 intron 6 C>T polymorphism (CYP3A4*22) is associated with an increased risk of delayed graft function and worse renal function in cyclosporine-treated kidney transplant patients
    Laure Elens
    Department of Clinical Chemistry, Erasmus MC, Rotterdam, The Netherlands
    Pharmacogenet Genomics 22:373-80. 2012
    Cyclosporine A (CsA) is a substrate of cytochrome P450 3A4 (CYP3A4)...
  46. doi DNA methylation dynamics in the hepatic CYP3A4 gene promoter
    Marina Kacevska
    Section of Pharmacogenetics, Department of Physiology and Pharmacology, Karolinska Institutet, SE 171 77 Stockholm, Sweden
    Biochimie 94:2338-44. 2012
    The CYP3A4 gene, encoding the major drug metabolizing enzyme in humans, exhibits a high interindividual variation in hepatic expression that can lead to interindividual differences in drug metabolism and associated adverse drug effects...
  47. doi Effects of CYP3A4 and CYP3A5 polymorphisms on tacrolimus pharmacokinetics in Chinese adult renal transplant recipients: a population pharmacokinetic analysis
    Xiao Cong Zuo
    Clinical Pharmacy and Pharmacology Research Institute, The Third Xiangya Hospital of Central South University, Beijing, China
    Pharmacogenet Genomics 23:251-61. 2013
    ..The aim of this study was to examine the association between tacrolimus pharmacokinetic variability and CYP3A4 and CYP3A5 genotypes by a population pharmacokinetic analysis based on routine drug monitoring data in adult renal ..
  48. ncbi Genomic organization of the human CYP3A locus: identification of a new, inducible CYP3A gene
    K Gellner
    EPIDAUROS Biotechnologie AG, Bernried, Germany
    Pharmacogenetics 11:111-21. 2001
    ..The 231 kb locus sequence contains the three CYP3A genes described previously (CYP3A4, CYP3A5 and CYP3A7), three pseudogenes as well as a novel CYP3A gene termed CYP3A43...
  49. ncbi Identification and functional characterization of eight CYP3A4 protein variants
    R Eiselt
    EPIDAUROS Biotechnologie AG, Bernried, Federal Republic of Germany
    Pharmacogenetics 11:447-58. 2001
    The genetic component of the inter-individual variability in CYP3A4 activity has been estimated to be between 60% and 90%, but the underlying genetic factors remain largely unknown...
  50. ncbi CYP3A4-V and prostate cancer in African Americans: causal or confounding association because of population stratification?
    Rick A Kittles
    National Human Genome Center, Howard University, Washington, DC 20060, USA
    Hum Genet 110:553-60. 2002
    b>CYP3A4-V, an A to G promoter variant associated with prostate cancer in African Americans, exhibits large differences in allele frequency between populations...
  51. ncbi Identification of human CYP forms involved in the activation of tamoxifen and irreversible binding to DNA
    David J Boocock
    MRC Molecular Endocrinology Group, Department of Obstetrics and Gynaecology, Robert Kilpatrick Building, University of Leicester, Leicester LE2 7LX, UK
    Carcinogenesis 23:1897-901. 2002
    ..baculovirus expressed recombinant human CYP forms and liquid chromatography-mass spectrometry to show that only CYP3A4 is responsible for the NADPH-dependent alpha-hydroxylation of tamoxifen...
  52. ncbi The CYP3A4*1B variant is related to the onset of puberty, a known risk factor for the development of breast cancer
    Fred F Kadlubar
    Division of Molecular Epidemiology, National Center for Toxicological Research, Jefferson, Arkansas 72079, USA
    Cancer Epidemiol Biomarkers Prev 12:327-31. 2003
    ..High activity CYP3A4, but not CYP3A5, which primarily metabolizes testosterone, showed a striking association with the onset of puberty ..
  53. ncbi CYP3A4 and CYP3A5 genotypes, haplotypes, and risk of prostate cancer
    Sarah J Plummer
    Department of Cancer Biology, Lerner Research Institute, The Cleveland Clinic Foundation, Cleveland, Ohio, USA
    Cancer Epidemiol Biomarkers Prev 12:928-32. 2003
    Previous case-only studies have shown that men with the CYP3A4*1B promoter variant are at an increased risk of developing more aggressive forms of prostate cancer...
  54. ncbi CYP3A4, CYP3A5, and CYP3A43 genotypes and haplotypes in the etiology and severity of prostate cancer
    Charnita Zeigler-Johnson
    Department of Biostatistics and Epidemiology, University of Pennsylvania School of Medicine, Philadelphia, Pennsylvania 19104 6021, USA
    Cancer Res 64:8461-7. 2004
    The CYP3A genes reside on chromosome 7q21 in a multigene cluster. The enzyme products of CYP3A4 and CYP3A43 are involved in testosterone metabolism...
  55. ncbi Pharmacogenetic screening for polymorphisms in drug-metabolizing enzymes and drug transporters in a Dutch population
    T M Bosch
    Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute Slotervaart Hospital, Amsterdam, The Netherlands
    Mol Diagn Ther 10:175-85. 2006
    ..this study was to explore the frequencies of polymorphisms in drug-metabolizing enzymes (CYP1A1, CYP2C9, CYP2C19, CYP3A4, CYP2D6, CYP3A5, DPYD, UGT1A1, GSTM1, GSTP1, GSTT1) and drug transporters (ABCB1[MDR1] and ABCC2[MRP2]), and to ..
  56. ncbi Transcription factor binding to a putative double E-box motif represses CYP3A4 expression in human lung cells
    Jason S Biggs
    Department of Pharmacology and Toxicology, University of Utah, Salt Lake City, UT 84112 5820, USA
    Mol Pharmacol 72:514-25. 2007
    Two vital enzymes of the CYP3A subfamily, CYP3A4 and CYP3A5, are differentially expressed in the human lung. However, the molecular mechanisms that regulate tissue-selective expression of the genes are poorly understood...
  57. doi Influence of polymorphisms of drug metabolizing enzymes (CYP2B6, CYP2C9, CYP2C19, CYP3A4, CYP3A5, GSTA1, GSTP1, ALDH1A1 and ALDH3A1) on the pharmacokinetics of cyclophosphamide and 4-hydroxycyclophosphamide
    Corine Ekhart
    Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute Slotervaart Hospital, Amsterdam, The Netherlands
    Pharmacogenet Genomics 18:515-23. 2008
    ..The purpose of this study was to evaluate the effects of known allelic variants in the CYP2B6, CYP2C9, CYP2C19, CYP3A4, CYP3A5, GSTA1, GSTP1, ALDH1A1 and ALDH3A1 genes on the pharmacokinetics of the anticancer agent, cyclophosphamide,..
  58. pmc Pharmacogenetic pathway analysis of docetaxel elimination
    S D Baker
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, Tennessee, USA
    Clin Pharmacol Ther 85:155-63. 2009
    ..17). However, the simultaneous presence of the CYP3A4*1B and CYP3A5*1A alleles was associated with a 64% increase in docetaxel clearance (P = 0...
  59. pmc Influence of CYP2B6 polymorphisms on the persistence of plasma nevirapine concentrations following a single intra-partum dose for the prevention of mother to child transmission in HIV-infected Thai women
    Soranun Chantarangsu
    Department of Pathology, Faculty of Medicine, Ramathibodi Hospital, Mahidol University, Bangkok, Thailand
    J Antimicrob Chemother 64:1265-73. 2009
    ..To investigate the association of single nucleotide polymorphisms (SNPs) with nevirapine concentrations following intra-partum single-dose nevirapine...
  60. doi The unique complexity of the CYP3A4 upstream region suggests a nongenetic explanation of its expression variability
    Huan Qiu
    Department of Pharmacology, Universitatsmedizin, Johannes Gutenberg University, Mainz, Germany
    Pharmacogenet Genomics 20:167-78. 2010
    The individually variable and unpredictable expression of CYP3A4 compromises therapies with 50% of contemporary drugs. Gene variants explain only a fraction of this variability.
  61. doi Regulation of CYP3A4 by pregnane X receptor: The role of nuclear receptors competing for response element binding
    Monica A Istrate
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Biochem Biophys Res Commun 393:688-93. 2010
    Induction of the major drug metabolizing enzyme CYP3A4 by xenobiotics contributes to the pronounced interindividual variability of its expression and often results in clinically relevant drug-drug interactions...
  62. ncbi Transcriptional regulation of human CYP3A4 basal expression by CCAAT enhancer-binding protein alpha and hepatocyte nuclear factor-3 gamma
    C Rodriguez-Antona
    Departamento de Bioquimica, Facultad de Medicina, Universidad de Valencia, Valencia, Spain
    Mol Pharmacol 63:1180-9. 2003
    b>Cytochrome P450 3A4 (CYP3A4) is involved in the metabolism of more than 50% of currently used therapeutic drugs, yet the mechanisms that control CYP3A4 basal expression in liver are poorly understood...
  63. ncbi Genotype-phenotype associations for common CYP3A4 and CYP3A5 variants in the basal and induced metabolism of midazolam in European- and African-American men and women
    Michael D Floyd
    Division of Clinical Pharmacology, Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6602, USA
    Pharmacogenetics 13:595-606. 2003
    ..individuals and it has been suggested that this has a genetic basis, possibly related to variant alleles in CYP3A4 and CYP3A5 genes...
  64. doi Pharmacogenetics of cyclosporine in children suggests an age-dependent influence of ABCB1 polymorphisms
    Samuel Fanta
    Department of Clinical Pharmacology, University of Helsinki, and Pediatric Nephrology and Transplantation, Hospital for Children and Adolescents, Helsinki University Central Hospital, Helsinki, Finland
    Pharmacogenet Genomics 18:77-90. 2008
    To evaluate whether variations in the ABCB1, ABCC2, SLCO1B1, CYP3A4, CYP3A5, or NR1I2 genes are associated with the pharmacokinetics of cyclosporine in pediatric renal transplant candidates, and whether the effects of these variants are ..
  65. doi Impact of CYP3A5 and CYP3A4 gene polymorphisms on dose requirement of calcineurin inhibitors, cyclosporine and tacrolimus, in renal allograft recipients of North India
    Ranjana Singh
    Department of Urology and Renal Transplantation, Sanjay Gandhi Post Graduate Institute of Medical Sciences, Raebareli Road, Lucknow, Uttar Pradesh, India
    Naunyn Schmiedebergs Arch Pharmacol 380:169-77. 2009
    The present study investigated pharmacogenetic associations of common cytochrome P450 3A (CYP3A5 and CYP3A4) polymorphisms with dose requirements of calcineurin inhibitors, cyclosporine (CsA) and tacrolimus (Tac) in renal transplant ..
  66. doi Association between ABCC2 polymorphism and lopinavir accumulation in peripheral blood mononuclear cells of HIV-infected patients
    Laure Elens
    Louvain Center for Toxicology and Applied Pharmacology LTAP, Universite Catholique de Louvain, 53 02 Avenue E Mounier, 1200 Bruxelles, Belgium
    Pharmacogenomics 10:1589-97. 2009
    ....
  67. ncbi Evidence for the catalysis of dextromethorphan O-demethylation by a CYP2D6-like enzyme in pig liver
    M Jurima-Romet
    Bureau of Biologics and Radiopharmaceuticals, Therapeutic Products Programme, Health Protection Branch, Health Canada, Tunney's Pasture
    Toxicol In Vitro 14:253-63. 2000
    ..antibodies revealed the presence of proteins in pig liver which cross-reacted with anti-human CYP1A2, CYP2D6 and CYP3A4, and with anti-rat CYP2E1 antibodies...
  68. ncbi Cytochrome P450-mediated metabolism and cytotoxicity of aflatoxin B(1) in bovine hepatocytes
    M E Kuilman
    Department of Veterinary Pharmacology, Pharmacy and Toxicology, Utrecht University, PO Box 80152, 3508 TD, The, Utrecht, Netherlands
    Toxicol In Vitro 14:321-7. 2000
    ..alpha-Naphthoflavone and ketoconazole, inhibitors of CYP1A and CYP3A, respectively in humans, were used to evaluate the contribution of specific P450 isoenzymes in bovine ..
  69. ncbi Complexation of membrane-bound enzyme systems
    D Muller-Enoch
    Department of Physiological Chemistry, Universitat Ulm, Germany
    Z Naturforsch C 55:747-52. 2000
    ..The nifedipine oxidase activity of two human P450 forms (CYP3A4, CYP3A4NF14) which differ only in their primary structure by ten ..
  70. pmc Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR
    W Xie
    Gene Expression Laboratory, The Salk Institute for Biological Studies, 10010 North Torrey Pines Road, La Jolla, California 92037, USA
    Genes Dev 14:3014-23. 2000
    The cytochrome P450 (CYP) gene products such as CYP3A and CYP2B are essential for the metabolism of steroid hormones and xenochemicals including prescription drugs...
  71. ncbi Comparison of the levels of enzymes involved in drug metabolism between transgenic or gene-knockout and the parental mice
    N Ariyoshi
    Laboratory of Drug Metabolism, Graduate School of Pharmaceutical Sciences, Hokkaido University, Sapporo, Japan
    Toxicol Pathol 29:161-72. 2001
    ..Results demonstrate that XPA gene knockout appeared to increase constitutive expression of CYP2B and CYP3A isoforms...
  72. ncbi Equally potent inhibitors of cholesterol synthesis in human hepatocytes have distinguishable effects on different cytochrome P450 enzymes
    L H Cohen
    TNO Prevention and Health, Gaubius Laboratory, Leiden, The Netherlands
    Biopharm Drug Dispos 21:353-64. 2000
    ..The following CYP reactions were used: nifedipine aromatization (CYP3A4), testosterone 6beta-hydroxylation (CYP3A4), tolbutamide methylhydroxylation (CYP2C9), S-mephenytoin 4-..
  73. ncbi Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs
    Shufeng Zhou
    Department of Pharmacy, Faculty of Science, National University of Singapore, Singapore
    Clin Pharmacokinet 44:279-304. 2005
    ..However, this unusual low substrate specificity also makes CYP3A4 susceptible to reversible or irreversible inhibition by a variety of drugs...
  74. ncbi Intravenous and oral alfentanil as in vivo probes for hepatic and first-pass cytochrome P450 3A activity: noninvasive assessment by use of pupillary miosis
    Evan D Kharasch
    Department of Anesthesiology, University of Washington, Seattle, 98195, USA
    Clin Pharmacol Ther 76:452-66. 2004
    ..miosis is a surrogate for plasma ALF concentrations, and IV ALF miosis is a noninvasive probe for hepatic CYP3A. This investigation characterized the bioavailability and first-pass metabolism of oral ALF and tested the ..
  75. ncbi Roles of cytochrome P450 3A enzymes in the 2-hydroxylation of 1,4-cineole, a monoterpene cyclic ether, by rat and human liver microsomes
    M Miyazawa
    Department of Applied Chemistry, Faculty of Science and Engineering, Kinki University, Higashiosaka, Osaka, Japan
    Xenobiotica 31:713-23. 2001
    ..2. CYP3A4 was a major enzyme involved in the 2-hydroxylation of 1,4-cineole by human liver microsomes, based on the ..
  76. doi Interactions of pharmaceuticals and other xenobiotics on hepatic pregnane X receptor and cytochrome P450 3A signaling pathway in rainbow trout (Oncorhynchus mykiss)
    Britt Wassmur
    Department of Zoology, University of Gothenburg, Box 463, SE 40530 Goteborg, Sweden
    Aquat Toxicol 100:91-100. 2010
    ..The PXR regulates expression of e.g. cytochrome P450 3A (CYP3A) and the P-glycoprotein (P-gp) that are involved in excretion of lipophilic xenobiotics and endobiotics...
  77. ncbi Role of hepatic and intestinal cytochrome P450 3A and 2B6 in the metabolism, disposition, and miotic effects of methadone
    Evan D Kharasch
    Department of Anesthesiology, University of Washington, 1959 NE Pacific Street, RR 442, Seattle, WA 98195, USA
    Clin Pharmacol Ther 76:250-69. 2004
    ..However, the role of CYP3A4 in human methadone disposition in vivo is unclear...
  78. ncbi Characterization of cytochrome P450 and glutathione S-transferase activity and expression in male and female ob/ob mice
    A L Roe
    Graduate Center for Toxicology, Division of Pharmacology and Experimental Therapeutics, University of Kentucky, Lexington 40536 0082, USA
    Int J Obes Relat Metab Disord 23:48-53. 1999
    ..To characterize the effect(s) of gender, age (glycemic status) and obese state, on hepatic biotransformation activities, expression of cytochrome P450 (CYP450) mRNAs and glutathione transferase activity in the ob/ob mouse...
  79. ncbi Human CYP2C19 is a major omeprazole 5-hydroxylase, as demonstrated with recombinant cytochrome P450 enzymes
    W G Karam
    National Institutes of Health, National Institute of Environmental Health Sciences, Research Triangle Park, NC 27709, USA
    Drug Metab Dispos 24:1081-7. 1996
    ..The present studies assessed the contribution of various CYP2C and CYP3A4 enzymes to OP metabolism by using recombinant human enzymes...
  80. pmc Midazolam metabolism in cytochrome P450 3A knockout mice can be attributed to up-regulated CYP2C enzymes
    Robert A B van Waterschoot
    Division of Experimental Therapy, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands
    Mol Pharmacol 73:1029-36. 2008
    The cytochrome P450 3A (CYP3A) enzymes represent one of the most important drug-metabolizing systems in humans. Recently, our group has generated cytochrome P450 3A knockout mice to study this drug-handling system in vivo...
  81. ncbi Selective induction of cytochrome P450 3A1 by dexamethasone in cultured rat hepatocytes: analysis with a novel reverse transcriptase-polymerase chain reaction assay section sign
    P A Hoen
    Division of Biopharmaceutics, Leiden Amsterdam Center for Drug Research, 2300 RA, Leiden, The Netherlands
    Biochem Pharmacol 60:1509-18. 2000
    ..Nevertheless, the activity of cytochrome P450 3A (CYP3A), one of the most important isoenzymes for drug metabolism, can be elevated by chemical inducers...
  82. doi Short communication: insulin alters hepatic progesterone catabolic enzymes cytochrome P450 2C and 3A in dairy cows
    C O Lemley
    Division of Animal and Nutritional Sciences, Davis College of Agriculture, Forestry and Consumer Sciences, West Virginia University, Morgantown, WV 26506, USA
    J Dairy Sci 91:641-5. 2008
    ..Progesterone catabolism occurs primarily in the liver via the cytochrome P450 2C (CYP2C) and cytochrome P450 3A (CYP3A) subfamilies (EC 1.14.14.1; unspecific monooxygenases)...
  83. ncbi Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4
    Shu Feng Zhou
    Division of Chinese Medicine, School of Health Sciences, WHO Collaborating Center for Traditional Medicine, RMIT University, Victoria, Australia
    Curr Drug Metab 9:310-22. 2008
    ..The crystal structure of bound and unbound CYP3A4 has been recently constructed, and a small active site and a peripheral binding site are identified...
  84. ncbi Antitumour prodrug development using cytochrome P450 (CYP) mediated activation
    L H Patterson
    Department of Pharmaceutical and Biological Chemistry, School of Pharmacy, University of London, UK
    Anticancer Drug Des 14:473-86. 1999
    ..of the CYP activation of AQ4N bioreduction was shown with human lymphoblastoid cell microsomes transfected with CYP3A4, but not those transfected with CYP2B6 or cytochrome P450 reductase...
  85. pmc Impact of the haplotypes of the human pregnane X receptor gene on the basal and St John's wort-induced activity of cytochrome P450 3A4 enzyme
    Xue Ding Wang
    Institute of Clinical Pharmacology, School of Pharmaceutical Sciences, Department of Pharmacy, The First Affiliated Hospital, Sun Yat Sen University, 74 Zhongshan Road, Section 2, Guangzhou, China
    Br J Clin Pharmacol 67:255-61. 2009
    Human pregnane X receptor (PXR/NR1I2) is a key regulator of cytochrome P450 3A4. To date, there are 198 reported SNPs for the human PXR/NR1I2 gene. Some of these SNPs are found to affect the inducing ability of PXR to CYP3A4.
  86. doi Kinetics of electron transfer between NADPH-cytochrome P450 reductase and cytochrome P450 3A4
    Yassar Farooq
    Henry Wellcome Laboratories of Structural Biology, Department of Biochemistry, Henry Wellcome Building, University of Leicester, PO Box 138, Lancaster Road, Leicester LE1 9HN, UK
    Biochem J 432:485-93. 2010
    We have incorporated CYP3A4 (cytochrome P450 3A4) and CPR (NADPH-cytochrome P450 reductase) into liposomes with a high lipid/protein ratio by an improved method...
  87. pmc A double transgenic mouse model expressing human pregnane X receptor and cytochrome P450 3A4
    Xiaochao Ma
    Laboratory of Metabolism, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA
    Drug Metab Dispos 36:2506-12. 2008
    b>Cytochrome P450 3A4 (CYP3A4), the most abundant human cytochrome P450 in liver, participates in the metabolism of approximately 50% of clinically used drugs...
  88. ncbi Significance of the minor cytochrome P450 3A isoforms
    Ann K Daly
    Pharmacogenetics Group, School of Clinical and Laboratory Sciences, University of Newcastle Medical School, Newcastle upon Tyne, UK
    Clin Pharmacokinet 45:13-31. 2006
    ..inducible via the glucocorticoid receptor, pregnane X receptor and constitutive androstane receptor-beta, as for CYP3A4. Although information on the substrate specificity of CYP3A5 is limited compared with CYP3A4, there have been a ..
  89. doi Effect of intravenous iron supplementation on hepatic cytochrome P450 3A4 activity in hemodialysis patients: a prospective, open-label study
    Amy Barton Pai
    University of New Mexico College of Pharmacy, MSC09 5360, Albuquerque, NM 87131, USA
    Clin Ther 29:2699-705. 2007
    ..b>CYP3A4 activity is reduced in hemodialysis (HD) patients and thus may be related to functional iron deficiency.
  90. ncbi Apolipoprotein E2 transgenic rabbits. Modulation of the type III hyperlipoproteinemic phenotype by estrogen and occurrence of spontaneous atherosclerosis
    Y Huang
    Gladstone Institute of Cardiovascular Disease, Cardiovascular Research Institute, University of California, San Francisco, California 94141-9100, USA
    J Biol Chem 272:22685-94. 1997
    ..apo) E2(Cys-158), an apoE variant associated with the human genetic disorder type III hyperlipoproteinemia (HLP)...
  91. doi Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors: Part I
    Christine E Staatz
    School of Pharmacy, University of Queensland, Brisbane, Queensland, Australia
    Clin Pharmacokinet 49:141-75. 2010
    ..Both agents are metabolic substrates for cytochrome P450 (CYP) 3A enzymes--in particular, CYP3A4 and CYP3A5--and are transported out of cells via P-glycoprotein (ABCB1)...
  92. pmc Mechanisms of pulmonary vasoconstriction and bronchoconstriction produced by PAF in the guinea-pig: role of platelets and cyclo-oxygenase metabolites
    L Argiolas
    Department of Pharmacology, , Rome, Italy
    Br J Pharmacol 114:203-9. 1995
    ..may be ascribed to the same mechanisms, we examined the actions of PAF in the heart-lung preparation of guinea-pig (HLP). The role of platelets and of cyclo-oxygenase metabolites was investigated. 2...
  93. doi Effect of CYP3A and ABCB1 single nucleotide polymorphisms on the pharmacokinetics and pharmacodynamics of calcineurin inhibitors: Part II
    Christine E Staatz
    University of Queensland, Brisbane, Australia
    Clin Pharmacokinet 49:207-21. 2010
    ..Both agents are metabolic substrates for cytochrome P450 (CYP) 3A enzymes - in particular, CYP3A4 and CYP3A5 - and are transported out of cells via P-glycoprotein (ABCB1)...
  94. ncbi Overexpression of cytochrome P-450 isoforms involved in aflatoxin B1 bioactivation in human liver with cirrhosis and hepatitis
    G M Kirby
    Lady Davis Institute for Medical Research, Jewish General Hospital, Montreal, Canada
    Toxicol Pathol 24:458-67. 1996
    ..expression and localization of various human cytochrome P-450 isoforms, including CYP2A6, CYP1A2, CYP3A4, and CYP2B1, were examined in normal human liver and liver with hepatitis and cirrhosis...
  95. pmc Contribution of human cytochrome p-450 isoforms to the metabolism of the simplest phenothiazine neuroleptic promazine
    Jacek Wojcikowski
    Department of Pharmacokinetics and Drug Metabolism, Institute of Pharmacology, Polish Academy of Sciences, Smetna 12, 31 343 Krakow, Poland
    Br J Pharmacol 138:1465-74. 2003
    ..CYP2D6-quinidine, CYP2A6+CYP2E1-diethyldithiocarbamic acid, CYP2C9-sulfaphenazole, CYP2C19-ticlopidine, CYP3A4-ketoconazole); (B)...
  96. ncbi General framework for the quantitative prediction of CYP3A4-mediated oral drug interactions based on the AUC increase by coadministration of standard drugs
    Yoshiyuki Ohno
    Department of Pharmacy, University of Tokyo Hospital Faculty of Medicine, University of Tokyo, Tokyo, Japan
    Clin Pharmacokinet 46:681-96. 2007
    ..Even though there are numerous reports regarding drug interactions involving CYP3A4, it is far from easy to estimate all potential interactions, since too many drugs are metabolised by CYP3A4...
  97. ncbi N,N-diethyl-2-[4-(phenylmethyl)phenoxy] ethanamine (DPPE) a chemopotentiating and cytoprotective agent in clinical trials: interaction with histamine at cytochrome P450 3A4 and other isozymes that metabolize antineoplastic drugs
    L J Brandes
    Department of Medicine, University of Manitoba, Winnipeg, Canada
    Cancer Chemother Pharmacol 45:298-304. 2000
    ..Many substrates of P-gp are also substrates of CYP3A4, a P450 isozyme that metabolizes a variety of antineoplastic agents and is highly expressed in some malignant ..
  98. pmc A comprehensive in vitro and in silico analysis of antibiotics that activate pregnane X receptor and induce CYP3A4 in liver and intestine
    Kazuto Yasuda
    Department of Pharmaceutical Sciences, St Jude Children s Research Hospital, Memphis, Tennessee, USA
    Drug Metab Dispos 36:1689-97. 2008
    ..Our focus was to identify those antibiotics that activate pregnane X receptor (PXR) and induce CYP3A4 in human hepatocytes and intestinal cells...
  99. ncbi Rapid determination of rat hepatocyte mRNA induction potential using oligonucleotide probes for CYP1A1, 1A2, 3A and 4A1
    D D Surry
    Department of Drug Metabolism and Pharmacokinetics, Merck Research Laboratories, Harlow, UK
    Xenobiotica 30:441-56. 2000
    ..2. The rat hepatocyte induction potential (RHIP) assays for CYP3A, 1A1, 1A2 and 4A1 are sensitive and selective and have an excellent qualitative relationship with CYP induction ..
  100. pmc Methadone N-demethylation in human liver microsomes: lack of stereoselectivity and involvement of CYP3A4
    D J Foster
    Department of Clinical and Experimental Pharmacology, University of Adelaide, Adelaide 5005, Australia
    Br J Clin Pharmacol 47:403-12. 1999
    ..To investigate the kinetics of CYP-mediated N-demethylation of methadone in human liver microsomes, and examine the role of stereoselectivity and CYP isoforms involved...
  101. ncbi Up-regulation of the alligator CYP3A77 gene by toxaphene and dexamethasone and its short term effect on plasma testosterone concentrations
    M P Gunderson
    Department of Zoology, University of Florida, P O Box 118525, Gainesville, FL 32611 8525, United States
    Aquat Toxicol 78:272-83. 2006
    In this study we describe an alligator hepatic CYP3A gene, CYP3A77, which is inducible by dexamethasone and toxaphene...

Research Grants66

  1. ALCOHOL-INDUCED HEPATIC P450s IN HCV/HIV OXIDATE INJURY
    STEVEN SHEDLOFSKY; Fiscal Year: 2003
    ..P450 isoforms, including the classical ethanol-inducible CYP2El, as well as the most abundant human hepatic P450, CYP3A4, it is possible that alcohol's enhancement of HCV injury is mediated by the increased activities of these P450s...
  2. Characterization of a Novel Selective Cytochrome P450 3A5 Substrate
    MICHAEL DARIN CAMERON; Fiscal Year: 2013
    ..However, tools are not currently available to distinguish between the major CYP3A enzymes, CYP3A4 and CYP3A5. These two enzymes are implicated in the metabolism of more pharmaceuticals than any other P450s...
  3. Maria Almira Correia; Fiscal Year: 2016
    ..e. grapefruit juice furanocoumarins). We have recently shown that the degradation of P450s such as CYP3A4, the major human liver and intestinal P450, and the EtOH-metabolizing CYP2E1 incurs ubiquitination by gp78 and ..
  4. NOVEL HIGH THROUGHPUT PLATFORM FOR SCREENING CYTOCHROME P450 INDUCTION
    MARIA INES MORANO; Fiscal Year: 2013
    ..According to a recent guidance from the FDA, CYP1A2, CYP2B6, and CYP3A4 induction should be evaluated in at least an in vitro system...
  5. James R Halpert; Fiscal Year: 2014
    ..proposed research is to determine the mechanistic basis for the atypical kinetics of substrate oxidation by human CYP3A4, the major P450 in adult liver and intestine...
  6. PK/PD Issues in the Use of New Therapies for the Treatment of Tuberculosis
    Kelly E Dooley; Fiscal Year: 2013
    ..It is metabolized by the cytochrome P450 isoenzyme 3A4 (CYP3A4), so drug interactions with agents used to treat human immunodeficiency virus (HIV) are likely...
  7. Mary F Paine; Fiscal Year: 2014
    ..data indicate that constituents in these mixtures are potent inhibitors of intestinal cytochrome P450 3A (CYP3A)-mediated metabolism (silymarin) or organic anion transporting polypeptide (OATP)-mediated absorptive uptake (GFJ),..
  8. Safety, Efficacy, and Mechanisms in American Ginseng in HIV-Related Fatigue
    Adriana S A Andrade; Fiscal Year: 2012
    ..Preliminary data indicate that AG does not significantly affect CYP3A4 activity, the major metabolic pathway for most ARV drugs...
  9. Activating liver carcinogens in yeast by expressing CYP450 polymorphisms
    MICHAEL THOMAS FASULLO; Fiscal Year: 2010
    ..Cytochrome P450 genes, such as CYP1A1, CYP1A2, CYP3A4, and CYP3A5 encode proteins that activate potent liver carcinogens into genotoxic epoxides...
  10. Does the extreme variability of methadone metabolism have an epigenetic cause?
    Gavin R Schnitzler; Fiscal Year: 2010
    ..of inter-individual expression variability, in the liver and intestines, of the drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4)...
  11. Functional studies of PGRMC1 in cholesterol homeostasis
    PETER JOHN ESPENSHADE; Fiscal Year: 2010
    ..Using transfected cultured cells, we found that PGRMC1 binds tightly to a diverse set of P450 enzymes, including Cyp3A4, Cyp21A2 and Cyp7A1 that function in drug metabolism, steroid and bile acid synthesis, respectively...
  12. Altered Hepatic Disposition of Statins by Diabetes Mellitus
    Fatemeh Akhlaghi; Fiscal Year: 2012
    ..Furthermore, in the livers of diabetic donors, we have shown significant downregulation of cytochrome P450 3A4 (CYP3A4) that is responsible for the biotransformation of approximately 55% of all marketed medications...
  13. Susceptibility to methylmercury toxicity: A role for cytochrome p450 enzymes
    Matthew D Rand; Fiscal Year: 2013
    ..Specific Aims are designed to investigate the functional and genetic association of the human homologs of CYP6g1 (CYP3A4, CYP3A5 and CYP3A7) with tolerance to MeHg toxicity in people...
  14. Christopher A Reilly; Fiscal Year: 2014
    ..The three major CYP3A enzymes (3A4, 3A5, 3A7) are the primary catalysts of GC oxidation in human liver, where much is known about the ..
  15. Xiao bo Zhong; Fiscal Year: 2014
    DESCRIPTION (provided by applicant): The cytochrome P450 3A subfamily (CYP3A) members, such CYP3A4, CYP3A5, and CYP3A7, are the most abundant P450 enzymes expressed in human liver and intestine and are responsible for metabolizing >50%..
  16. Jashvant D Unadkat; Fiscal Year: 2016
    ..most important for metabolism and transport of both illicit and licit drugs in the liver or the placenta, namely CYP3A (Project 1), CYP2B6 and CYP2D6 (Project 2), P-gp and BCRP (Project 3), and OCTS, NET, and SERT (Project 4)...
  17. Santosh Kumar; Fiscal Year: 2016
    ..Since CYP3A4 is known to metabolize important HAART drugs, protease inhibitors (PIs), the role of CYP3A4 is considered critical ..
  18. Bingfang Yan; Fiscal Year: 2016
    ..pregnane X receptor (PXR), a master regulator on the expression of many chemical elimination genes such as cytochrome P450 3A4 (CYP3A4) in humans and CYP3A23 in rats...
  19. Hyunyoung Jeong; Fiscal Year: 2015
    ..2) Elucidate regulatory mechanisms for CYP3A4 induction by PRG. (3) Identify regulatory mechanisms for CYP2D6 induction during pregnancy...
  20. JUNG JA P KIM; Fiscal Year: 2016
    ..Aim 2: To determine the crystal structures of complexes of CYPOR with CYP2D6, CYP3A4, CYP2B4, and human HO-1...
  21. STRUCTURE AND DYNAMICS OF METAL-CONTAINING PROTEINS
    THOMAS CHARLES POCHAPSKY; Fiscal Year: 2012
    ..The binding of substrates and inhibitors in the active sites of mammalian P450 enzymes with CYP2B4 and CYP3A4 will be characterized...
  22. Effects of Anthocyanins on Cytochrome P450 Enzymes and P-glycoprotein
    MICHAEL JOHN HANLEY; Fiscal Year: 2012
    ..In preliminary work, blueberry juice inhibited the in vitro activity of CYP3A and CYP2C9 at concentrations that could easily be achieved in the gastrointestinal tract after BBJ consumption...
  23. PGRMC1: A Regulator of CYP3A Activity
    Erin G Schuetz; Fiscal Year: 2010
    ..by applicant): The long-term objectives of this proposal are to determine the magnitude of PGRMC1's effect on CYP3A4 activity and if this effect is substrate specific. PGRMC1 is a hemoprotein with a cytochrome b5-like domain...
  24. Larisa Y Poluektova; Fiscal Year: 2016
    ..be measured by employing PXR humanization (the androstane receptor with replacement of the mouse Cyp3a with human CYP3A4) in rodents. This can be used to evaluate long-term immune and antiviral responses...
  25. Regulation of PXR by cell cycle and phosphorylation
    Taosheng Chen; Fiscal Year: 2013
    ..b>CYP3A4 catalyzes the metabolism of more than 50% of clinically used drugs...
  26. Antileishmanial Lead Optimization of Quinazolines
    Karl A Werbovetz; Fiscal Year: 2013
    ..Several development-limiting toxicities (i.e. hepatotoxicity, cardiotoxicity, and CYP3A4 inhibition will be evaluated for active 2,4-diaminoquinazolines to prioritize compounds for further testing...
  27. REDUCED DRUG INTERACTIONS OF AZOLE ANTIFUNGAL DRUGS
    Joseph Gal; Fiscal Year: 2003
    ..CYP) enzyme, and the problems of drug-drug interactions are the result of the inhibition of human CYP, mainly CYP3A4, by these azoles...
  28. AGING EFFECT ON DRUG BIOAVAILABILITY
    Stephen Hall; Fiscal Year: 1999
    ..It is clear that for CYP3A substrates the systemic clearance is reduced and bioavailability increased in the elderly, but it is unclear ..
  29. Prediction of Drug-Drug Interactions
    Zeruesenay Desta; Fiscal Year: 2007
    ..We will focus on metabolic drug interactions at the level of the CYP3A enzymes in the liver and intestinal wall because these represent the single most common cause of clinically ..
  30. CECILIA PILAR CHUNG; Fiscal Year: 2016
    ..Particularly important are drug interactions mediated by CYP3A, the cytochrome P-450 (CYP) member that is involved in the metabolism of more than 60% of all drugs...
  31. Cellular Efflux and Metabolism of Protease Inhibitors
    Ashim Mitra; Fiscal Year: 2004
    DESCRIPTION (Provided by the applicant): Cytochrome P450 3A4 (CYP3A4), most abundantly presently both in the liver and upper intestinal enterocytes, limits the systemic bioavailability of anti-HIV agents...
  32. William M Atkins; Fiscal Year: 2016
    ..that are indentified, and to relate these findigns to the behavior of the putative water-bridged Telaprevir-CYP3A4 complex...
  33. Drug-induced liver injury associated with anti-retroviral therapy
    Xiaochao Ma; Fiscal Year: 2012
    ..pretreatment followed by ritonavir-containing protease inhibitor regimens in double transgenic human PXR and CYP3A4 mice...
  34. TeamChip for High-throughput, Predictive Human Metabolism and Toxicology
    Moo Yeal Lee; Fiscal Year: 2010
    ..g., CYP450 isoforms including CYP1A2 and CYP3A4) and demonstrate gene transfection on monolayers of THLE-2 and Beas-2B cells using fluorogenic substrates in a 96-..
  35. Michael N Neely; Fiscal Year: 2016
    ..Therefore it is crucial to quantify the impact of age and illness on the phenotypc activity of CYP2C19, CYP3A4 and flavin mono-oxygenase 3 (FMO3), which together metabolize >90% of voriconazole, and to optimally and ..
  36. Effect of Cirrhosis and Shunts on Drug Disposition
    Stephen Hall; Fiscal Year: 2006
    ..patients with TIPS experience an increase in intestinal availability of midazolam, a selective cytochrome P450 3A (CYP3A) substrate...
  37. Factors Affecting CYP3A-Mediated Metabolism of Drugs of Abuse in HIV+ Patients
    Lauren Oleson; Fiscal Year: 2007
    ..Benzodiazepines are primarily metabolized by the major class of the cytochrome P450 (CYP) family, CYP3A, which exhibits wide inter-individual variability and is inhibited or induced by many currently marketed drugs, ..
  38. MOLECULAR BASIS OF HUMAN CYTOCHROME P450 3A FUNCTION
    JAMES HALPERT; Fiscal Year: 2004
    ..b>CYP3A4 is the most highly expressed P450 in the liver of most humans, is responsible for the metabolism of more ..
  39. Regulatory Oxygenases in Vasculopathic Rickettsioses
    SANJEEV SAHNI; Fiscal Year: 2010
    ..in signaling mechanisms and functional consequences of infection-induced HO-1 using Sheila Smith (highly virulent), HLP (comparatively less pathogenic), and Iowa (avirulent) strains of R rickettsii, and (ii)...
  40. Regulation of Drug Metabolizing Enzyme Ontogeny
    D Gail McCarver; Fiscal Year: 2012
    ..hepatic phase I xenobiotic metabolizing enzymes, the most dramatic changes are observed in the cytochrome P4503A (CYP3A) and flavin-containing monooxygenases (FMO) gene families...
  41. Yan Chun Li; Fiscal Year: 2016
    ..D receptor (VDR), and LCA-VDR signals, like VD-VDR signals, also promote secondary BA catabolism by inducing Cyp3A, which can paradoxically limit LCA's tumor-promoting effects...
  42. Functional Vitamin D Receptor Gene Variants and Racial/Ethnic Cancer Disparities
    Robin Taylor Wilson; Fiscal Year: 2010
    ..Elements (VDRE) located in the promoter region of genes involved in vitamin D metabolism (VDR, CYP24A1 and CYP3A4);2) Molecularly characterize VDRE polymorphic variants alone and in combination with VDR-short and VDR-long ..
  43. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
    ..of garlic, on the processes regulating disposition of the majority of antiretroviral agents (metabolism by CYP3A and transport by P-glycoprotein), and on the pharmacokinetics of two representative antiretrovirals, ritonavir and ..
  44. Sara K Quinney; Fiscal Year: 2016
    ..Pharmacogenetic variations in nifedipine pathway genes, e.g. CYP3A4, CYP3A5, CACNA1C, and CACN1C, will be tested for association with tocolytic response to nifedipine...
  45. Isothiocyanates as specific antagonists of human SXR
    David Eaton; Fiscal Year: 2009
    ..diet) changes in hepatic and intestinal drug disposition. Cytochrome P450 3A4 (CYP3A4) is responsible for the hepatic and intestinal metabolism of numerous xenobiotics, including ..
  46. Nicola Marchi; Fiscal Year: 2016
    ..cells (EC) isolated from drug resistant epileptic patients (DRE);these include AED- metabolizers such as CYP3A4, CYP2C9, etc...
  47. INTERACTIONS OF P GLYCOPROTEIN WITH CYTOCHROME P4503A
    Erin Schuetz; Fiscal Year: 2001
    ..This aim uses our novel cell lines which form polarized epithelium in culture and stably express functional CYP3A4 and Pgp...
  48. Jamie L Renbarger; Fiscal Year: 2016
    ..Two enzymes (CYP3A4 and 3A5) metabolize vincristine;but CYP3A5 is 10-times more efficient as a catalyst of vincristine metabolism...
  49. Wolfgang Sadee; Fiscal Year: 2014
    ..link between genotype of proven function and clinical outcomes (examples: DRD2, TPH2, ACE, VKORC1, CETP, and CYP3A4). These results support a critical role for regulatory polymorphisms in drug response...
  50. Douglas W Billings; Fiscal Year: 2014
    ..test Positively tHrIVing, an HIV behavioral intervention based on modules 2 and 3 of the Healthy Living Project (HLP;a "best evidence" CDC intervention), and then tailored it to fit the unique needs of HIV+ African American men (..
  51. Kathleen E Malone; Fiscal Year: 2014
    ..The enzymes that most affect the conversion of TAM to its key metabolites are CYP2D6, CYP3A4, CYP3A5, but other important phase I and II enzymes include CYP2C9, CYP2C19, CYP2B6, CYP1B1, UGT2B7, UGT2B15, ..
  52. Hongbing Wang; Fiscal Year: 2016
    ..4-OH-CPA) via CYP2B6, but not to the N- dechloroethyl-cyclophosphamide and the toxic chloroacetaldehyde by CYP3A4. Towards this end, we have shown that activation of the human constitutive androstane receptor (hCAR) ..
  53. ANTIRETROVIRAL THERAPIES AND SUBSTANCE ABUSE
    David Greenblatt; Fiscal Year: 2002
    ..HIV PIs and NNRTls may inhibit and/or induce the activity of human Cytochrome P4503A (CYP3A) enzymes, responsible for the metabolism of buprenorphine, methadone, many benzodiazepines and for the formation ..
  54. Computer-based HIV Prevention for Seropositive Men
    Douglas W Billings; Fiscal Year: 2010
    ..This prototype will be based on the core components of modules 2 and 3 of the Healthy Living Project (HLP)...
  55. Regulatory circuits that control transcriptional responses to hypoxia
    Jo Anne Powell Coffman; Fiscal Year: 2010
    ..The C. elegans hif-1, egl-9 and vhl-1 genes are orthologous to the genes encoding the Hlp alpha subunit, the EGLN/ PHD / HPH prolyl hydroxylase, and the VHL tumor suppressor, respectively...
  56. AIDS ASSOCIATED LEUKOPLAKIA--ROLE OF EBV
    Nancy Raab Traub; Fiscal Year: 2004
    EBV is detected in epithelial cells in a unique oral lesion known as "hairy" leukoplakia (HLP), which is a harbinger for the development of the acquired immunodeficiency syndrome (AIDS)...
  57. Older Persons & Drugs: race, gender, and age effects
    Janice B Schwartz; Fiscal Year: 2010
    ..If vitamin D alters clearance of atorvasastatin, it may alter clearance of the many CYP3A substrates administered therapeutically...
  58. Herb-Opioid Interactions
    Danny Shen; Fiscal Year: 2003
    ..The interactions are now recognized to involve induction of two drug disposition mechanisms: cytochrome P450 3A4 enzyme and the active efflux pump, P-glycoprotein, both leading to profound reductions in blood or plasma ..
  59. A Community Trial in Alaska to Prevent Youth's Use of Legal Products to Get High
    Joel W Grube; Fiscal Year: 2013
    ..are to reduce the proportion of increase community readiness to implement environmental strategies to prevent HLP use, pre and early adolescents (5th, 6th, graders) who intend to or do experience inhaling or ingesting HLPs found ..
  60. Formulation Dependent Help Interactions with Chemothera*
    David Kroll; Fiscal Year: 2005
    ..SJW extracts may also interact pharmacokinetically with cancer chemotherapeutics by inducing OR inhibiting CYP3A4 activity depending upon the duration of exposure and the SJW formulation used...
  61. The Effects of Tissue Microstructure on the Development of Ductal Cancer
    KYLE EVAN BROADERS; Fiscal Year: 2013
    ..I will then be able to lead my own interdisciplinary research projects that will hlp to unlock the remaining mysteries in cancer biology and develop new areas for the prevention and treatment of all ..
  62. Pharmacogenetics: Breast Cancer Treatment and Prognosis
    Christine Ambrosone; Fiscal Year: 2005
    ..For example, cyclophosphamide undergoes hepatic activation by CYP3A4 and metabolites may be detoxified by conjugation with glutathione, catalyzed by glutathione S-transferases P1 and ..
  63. Alcohol and HIV protease inhibitors interactions
    Dennis Feierman; Fiscal Year: 2003
    ..Because of the importance of CYP3A4 with respect to HIV-PI drug metabolism, and its induction by ethanol, the interactions of HIV-PI and ethanol are ..
  64. P450 PHENOTYPE AND CHEMOTHERAPY TOXICITY IN THE ELDERLY
    ELIZABETH DEES; Fiscal Year: 2006
    ..Paclitaxel is principally metabolized by CYP2C8 and CYP3A4, and vinorelbine by CYP3A4...
  65. BIOMARKERS OF TREATMENT RELATED LEUKEMIA
    CAROLYN FELIX; Fiscal Year: 2004
    ..The metabolites have genotoxic properties that may be relevant to leukemogenesis. The promoter of the CYP3A4 gene is polymorphic...
  66. DRUG METABOLIZING ENZYMES-RISK FACTORS IN BLADDER CANCER
    Robert Branch; Fiscal Year: 2004
    ..that comprises CYP1A2 (caffeine), CYP2C19 (S-mephenytoin), CYP2D6 (debrisoquine), CYP2E1 (chlorzoxazone) and CYP3A4 (dapsone), as well as mRNA concentrations for each of these CYP enzymes in leukocytes and genotypic identification ..