CYP2B6

Summary

Gene Symbol: CYP2B6
Description: cytochrome P450 family 2 subfamily B member 6
Alias: CPB6, CYP2B, CYP2B7, CYP2B7P, CYPIIB6, EFVM, IIB1, P450, cytochrome P450 2B6, 1,4-cineole 2-exo-monooxygenase, cytochrome P450 IIB1, cytochrome P450, family 2, subfamily B, polypeptide 6, cytochrome P450, subfamily IIB (phenobarbital-inducible), polypeptide 6
Species: human

Top Publications

  1. ncbi A comparison of 2-phenyl-2-(1-piperidinyl)propane (ppp), 1,1',1''-phosphinothioylidynetrisaziridine (thioTEPA), clopidogrel, and ticlopidine as selective inactivators of human cytochrome P450 2B6
    Robert L Walsky
    Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Pfizer, Inc, Groton, CT 06340, USA
    Drug Metab Dispos 35:2053-9. 2007
  2. pmc Nuclear receptor CAR requires early growth response 1 to activate the human cytochrome P450 2B6 gene
    Kaoru Inoue
    Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, NIEHS, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 283:10425-32. 2008
  3. ncbi A single nucleotide polymorphism of CYP2b6 found in Japanese enhances catalytic activity by autoactivation
    N Ariyoshi
    Laboratory of Drug Metabolism, Hokkaido University, Sapporo, 060 0812, Japan
    Biochem Biophys Res Commun 281:1256-60. 2001
  4. pmc CYP2B6*6 is associated with increased breast cancer risk
    Christina Justenhoven
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, University of Tubingen, Stuttgart, Germany
    Int J Cancer 134:426-30. 2014
  5. ncbi Human CYP2B6: expression, inducibility and catalytic activities
    L Gervot
    INSERM U490, Universite Rene Descartes, Paris, France
    Pharmacogenetics 9:295-306. 1999
  6. ncbi Role of polymorphic human CYP2B6 in cyclophosphamide bioactivation
    H J Xie
    Division of Clinical Pharmacology, Department of Medical Laboratory Sciences and Technology, Karolinska Institutet, Huddinge University Hospital, Stockholm, Sweden
    Pharmacogenomics J 3:53-61. 2003
  7. ncbi Functional characterization of cytochrome P450 2B6 allelic variants
    Hideto Jinno
    Division of Environmental Chemistry, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    Drug Metab Dispos 31:398-403. 2003
  8. ncbi Smoking, alcoholism and genetic polymorphisms alter CYP2B6 levels in human brain
    Sharon Miksys
    Centre for Addiction and Mental Health, Department of Pharmacology, University of Toronto, Toronto, Ontario, Canada M5S 1A8
    Neuropharmacology 45:122-32. 2003
  9. ncbi Multiple novel nonsynonymous CYP2B6 gene polymorphisms in Caucasians: demonstration of phenotypic null alleles
    Thomas Lang
    EPIDAUROS Biotechnologie AG, AM Neuland, Bernried, Germany
    J Pharmacol Exp Ther 311:34-43. 2004
  10. ncbi Cytochrome P450 pharmacogenetics as a predictor of toxicity and clinical response to pulse cyclophosphamide in lupus nephritis
    Kazuki Takada
    National Institute of Arthritis and Musculoskeletal and Skin Diseases, NIH, Bethesda, Maryland 20892, USA
    Arthritis Rheum 50:2202-10. 2004

Research Grants

  1. Characterization of a Novel Selective Cytochrome P450 3A5 Substrate
    MICHAEL DARIN CAMERON; Fiscal Year: 2013
  2. Inhibition of Carboxylesterase Metabolism by Ethanol
    Robert B Parker; Fiscal Year: 2011
  3. Maria Almira Correia; Fiscal Year: 2016
  4. NOVEL HIGH THROUGHPUT PLATFORM FOR SCREENING CYTOCHROME P450 INDUCTION
    MARIA INES MORANO; Fiscal Year: 2013
  5. Interaction of Alcohol and HAART in HIV/AIDS and HIV/AIDS and HCV Coinfection
    Elinore F McCance Katz; Fiscal Year: 2011
  6. Angela M Brodie; Fiscal Year: 2014
  7. Christopher A Reilly; Fiscal Year: 2014
  8. EDWARD THOMAS MORGAN; Fiscal Year: 2016
  9. Todd C Skaar; Fiscal Year: 2016
  10. James R Halpert; Fiscal Year: 2014

Detail Information

Publications247 found, 100 shown here

  1. ncbi A comparison of 2-phenyl-2-(1-piperidinyl)propane (ppp), 1,1',1''-phosphinothioylidynetrisaziridine (thioTEPA), clopidogrel, and ticlopidine as selective inactivators of human cytochrome P450 2B6
    Robert L Walsky
    Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Pfizer, Inc, Groton, CT 06340, USA
    Drug Metab Dispos 35:2053-9. 2007
    ..However, the identification of CYP2B6 in the metabolism of drugs has been more challenging because of the lack of a well established inhibitor of this ..
  2. pmc Nuclear receptor CAR requires early growth response 1 to activate the human cytochrome P450 2B6 gene
    Kaoru Inoue
    Pharmacogenetics Section, Laboratory of Reproductive and Developmental Toxicology, NIEHS, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA
    J Biol Chem 283:10425-32. 2008
    ..the signal molecule EGR1 (early growth response 1) determines CAR-mediated activation of the human CYP2B6 (cytochrome P450 2B6) gene. The CYP2B6 enzyme metabolizes commonly used therapeutics and also activates pro-drugs...
  3. ncbi A single nucleotide polymorphism of CYP2b6 found in Japanese enhances catalytic activity by autoactivation
    N Ariyoshi
    Laboratory of Drug Metabolism, Hokkaido University, Sapporo, 060 0812, Japan
    Biochem Biophys Res Commun 281:1256-60. 2001
    A single nucleotide polymorphism (SNP) resulting in a substitution from Gln to His was found in exon 4 of the CYP2B6 gene in Japanese. The frequency of the variant allele was found to be 19.9%...
  4. pmc CYP2B6*6 is associated with increased breast cancer risk
    Christina Justenhoven
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, University of Tubingen, Stuttgart, Germany
    Int J Cancer 134:426-30. 2014
    The cytochrome P450 2B6 (CYP2B6) is involved in the metabolism of testosterone. Functional changes in this enzyme may influence endogenous hormone exposure, which has been associated with risk of breast cancer...
  5. ncbi Human CYP2B6: expression, inducibility and catalytic activities
    L Gervot
    INSERM U490, Universite Rene Descartes, Paris, France
    Pharmacogenetics 9:295-306. 1999
    ..Its expression in Saccharomyces cerevisiae enabled us to obtain, at a high level, an active yeast-expressed CYP2B6 protein, so as to assess its role in the metabolism of ethoxyresorufin, pentoxyresorufin, benzyloxyresorufin, ..
  6. ncbi Role of polymorphic human CYP2B6 in cyclophosphamide bioactivation
    H J Xie
    Division of Clinical Pharmacology, Department of Medical Laboratory Sciences and Technology, Karolinska Institutet, Huddinge University Hospital, Stockholm, Sweden
    Pharmacogenomics J 3:53-61. 2003
    The role of polymorphic CYP2B6 in cyclophosphamide (CPA) bioactivation was investigated in human liver microsomes. A total of 67 human liver specimens were first genotyped with respect to the CYP2B6*5 and CYP2B6*6 variant alleles...
  7. ncbi Functional characterization of cytochrome P450 2B6 allelic variants
    Hideto Jinno
    Division of Environmental Chemistry, National Institute of Health Sciences, 1 18 1 Kamiyoga, Setagaya Ku, Tokyo 158 8501, Japan
    Drug Metab Dispos 31:398-403. 2003
    ..Genetic polymorphisms of CYP2B6 (CYP2B6*2, CYP2B6*3, CYP2B6*4, CYP2B6*5, CYP2B6*6 and CYP2B6*7; wild-type, CYP2B6*1) were found previously in ..
  8. ncbi Smoking, alcoholism and genetic polymorphisms alter CYP2B6 levels in human brain
    Sharon Miksys
    Centre for Addiction and Mental Health, Department of Pharmacology, University of Toronto, Toronto, Ontario, Canada M5S 1A8
    Neuropharmacology 45:122-32. 2003
    b>CYP2B6 metabolizes drugs such as nicotine and bupropion, and many toxins and carcinogens. Nicotine induces CYP2B1 in rat brain and in humans polymorphic variation in CYP2B6 affects smoking cessation rates...
  9. ncbi Multiple novel nonsynonymous CYP2B6 gene polymorphisms in Caucasians: demonstration of phenotypic null alleles
    Thomas Lang
    EPIDAUROS Biotechnologie AG, AM Neuland, Bernried, Germany
    J Pharmacol Exp Ther 311:34-43. 2004
    The human microsomal cytochrome P450, CYP2B6, is involved in the biotransformation of several clinically important drugs...
  10. ncbi Cytochrome P450 pharmacogenetics as a predictor of toxicity and clinical response to pulse cyclophosphamide in lupus nephritis
    Kazuki Takada
    National Institute of Arthritis and Musculoskeletal and Skin Diseases, NIH, Bethesda, Maryland 20892, USA
    Arthritis Rheum 50:2202-10. 2004
    ..Cyclophosphamide is a prodrug that requires activation by cytochrome P450 (CYP) enzymes...
  11. 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)...
  12. ncbi Identification of a novel specific CYP2B6 allele in Africans causing impaired metabolism of the HIV drug efavirenz
    Jue Wang
    Division of Molecular Toxicology, Institute of Environmental Medicine, Karolinska Institute, Stockholm
    Pharmacogenet Genomics 16:191-8. 2006
    ..reverse transcriptase inhibitor efavirenz is mainly metabolised by the polymorphic cytochrome P450 enzyme CYP2B6. Genomic DNA from four subjects in a group of 51 patients being treated with efavirenz and having surprisingly ..
  13. ncbi Predictive value of known and novel alleles of CYP2B6 for efavirenz plasma concentrations in HIV-infected individuals
    M Rotger
    Institute of Microbiology, University of Lausanne, Lausanne, Switzerland
    Clin Pharmacol Ther 81:557-66. 2007
    To assess the association of CYP2B6 allelic diversity with efavirenz (EFV) pharmacokinetics, we performed extensive genotyping of 15 relevant single nucleotide polymorphism in 169 study participants, and full resequencing of CYP2B6 in ..
  14. ncbi Genetic polymorphisms of CYP2B6 affect the pharmacokinetics/pharmacodynamics of cyclophosphamide in Japanese cancer patients
    Miki Nakajima
    Drug Metabolism and Toxicology, Division of Pharmaceutical Sciences, Graduate School of Medical Science, Kanazawa University, Kakuma machi, Kanazawa 920 1192, Japan
    Pharmacogenet Genomics 17:431-45. 2007
    ..To evaluate the effects of genetic polymorphisms of drug metabolizing enzymes on the pharmacokinetics of cyclophosphamide and its active metabolite, 4-hydroxycyclophosphamide, and on the pharmacodynamics...
  15. ncbi Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitro
    Zeruesenay Desta
    Division of Clinical Pharmacology, Department of Medicine, Indiana University School of Medicine, 1001 West 10th Street, WD Myers Bldg, W7123, Indianapolis, IN 46202, USA
    Pharmacogenomics 8:547-58. 2007
    To determine the influence of cytochrome P450 2B6 (CYP2B6) genotype on the rate of oxidative efavirenz metabolism in human liver microsomes.
  16. ncbi Polymorphic CYP2B6: molecular mechanisms and emerging clinical significance
    Ulrich M Zanger
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
    Pharmacogenomics 8:743-59. 2007
    ..polymorphisms of CYP2D6 and CYP2C19, which were discovered by adverse drug reactions, pharmacogenetic study of CYP2B6 was initiated by reverse genetics approaches and subsequent functional and clinical studies...
  17. ncbi High prevalence of the CYP2B6 516G-->T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe
    Christopher Nyakutira
    Department of DMPK and BAC, African Institute of Biomedical Science and Technology AiBST, P O Box 2294, Harare, Zimbabwe
    Eur J Clin Pharmacol 64:357-65. 2008
    The study sought to investigate the relationship between efavirenz exposure and the CYP2B6 516G-->T(*6) genotype in HIV/AIDS outpatients, using pharmacokinetic modelling and simulation.
  18. pmc Impact of CYP2B6 983T>C polymorphism on non-nucleoside reverse transcriptase inhibitor plasma concentrations in HIV-infected patients
    Christoph Wyen
    Department of Internal Medicine, University of Cologne, Koln, Germany
    J Antimicrob Chemother 61:914-8. 2008
    The aim of this study was to investigate the frequency of CYP2B6 polymorphisms (according to ethnicity) and the influence of heterozygosity and homozygosity on plasma concentrations of efavirenz and nevirapine.
  19. pmc CYP2B6 G516T polymorphism but not rifampin coadministration influences steady-state pharmacokinetics of efavirenz in human immunodeficiency virus-infected patients in South India
    Geetha Ramachandran
    Department of Clinical Research, Tuberculosis Research Centre, Chetput, Chennai, India
    Antimicrob Agents Chemother 53:863-8. 2009
    ..Plasma efavirenz was estimated by high-performance liquid chromatography, and genotyping of CYP2B6 G516T polymorphism was performed by sequencing...
  20. 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
    Polymorphisms in CYP2B6 affect the steady-state plasma concentrations of nevirapine and efavirenz...
  21. 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...
  22. ncbi Plasma efavirenz concentrations and the association with CYP2B6-516G >T polymorphism in HIV-infected Thai children
    Thanyawee Puthanakit
    Research Institute for Health Sciences, Chiang Mai University, Chiang Mai, Thailand
    Antivir Ther 14:315-20. 2009
    ..Single nucleotide polymorphisms of the hepatic cytochrome P450 isoenzyme 2B6 (CYP2B6) gene have been associated with high interindividual variations in EFV plasma concentrations...
  23. pmc Effect of rifampicin-based antitubercular therapy and the cytochrome P450 2B6 516G>T polymorphism on efavirenz concentrations in adults in South Africa
    Karen Cohen
    Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Cape Town, South Africa
    Antivir Ther 14:687-95. 2009
    Rifampicin induces expression of the cytochrome P450 isoenzyme 2B6 (CYP2B6), which metabolizes efavirenz. The CYP2B6 516G>T polymorphism impairs efavirenz metabolism and occurs more commonly in Africans than in Caucasians...
  24. doi Hepatic CYP2B6 is altered by genetic, physiologic, and environmental factors but plays little role in nicotine metabolism
    N Al Koudsi
    Department of Pharmacology and Toxicology, University of Toronto, Toronto, ON, Canada
    Xenobiotica 40:381-92. 2010
    Human cytochrome P4502B6 (CYP2B6) is predominantly expressed in the liver and it plays a major role in the metabolism of several therapeutically important drugs and environmental toxicants...
  25. pmc Sequence variants at CHRNB3-CHRNA6 and CYP2A6 affect smoking behavior
    Thorgeir E Thorgeirsson
    1 deCODE genetics, Reykjavik, Iceland 2 Center for Biomolecular Science and Engineering, Jack Baskin School of Engineering, University of California, Santa Cruz, California, USA
    Nat Genet 42:448-53. 2010
    ..Among the genes at the two newly associated loci are genes encoding nicotine-metabolizing enzymes (CYP2A6 and CYP2B6) and nicotinic acetylcholine receptor subunits (CHRNB3 and CHRNA6), all of which have been highlighted in previous ..
  26. pmc Haplotype structure of CYP2B6 and association with plasma efavirenz concentrations in a Chilean HIV cohort
    Daniel F Carr
    Department of Pharmacology and Therapeutics, University of Liverpool, Liverpool, UK
    J Antimicrob Chemother 65:1889-93. 2010
    Efavirenz is extensively metabolized by CYP2B6, and associations between CYP2B6 polymorphisms and plasma efavirenz exposure have been reported...
  27. pmc Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS Clinical Trials Group study
    Heather J Ribaudo
    Statistical Data Analysis Center, Harvard School of Public Health, Harvard University, Boston, MA, USA
    J Infect Dis 202:717-22. 2010
    ..Clinical Trials Group protocols 384, A5095, and A5097s, we characterized relationships between 22 polymorphisms in CYP2B6, ABCB1, and CYP3A5; plasma efavirenz exposure; and/or treatment responses...
  28. doi CYP2B6 polymorphisms influence the plasma concentration and clearance of the methadone S-enantiomer
    Sheng Chang Wang
    Division of Mental Health and Addiction Medicine, Institute of Population Health Sciences, National Health Research Institutes, Zhunan, Miaoli County, Taiwan
    J Clin Psychopharmacol 31:463-9. 2011
    ..We thus tested whether CYP2B6 gene polymorphisms had any influence on the concentration or clearance of methadone...
  29. doi Functional characterization of CYP2B6 allelic variants in demethylation of antimalarial artemether
    Masashi Honda
    Laboratory of Pharmacotherapy of Life Style Related Diseases, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan
    Drug Metab Dispos 39:1860-5. 2011
    ..P450 (P450) isozymes responsible for the demethylation of AM and to evaluate functional differences between 26 CYP2B6 allelic variants in vitro...
  30. doi Q172H replacement overcomes effects on the metabolism of cyclophosphamide and efavirenz caused by CYP2B6 variant with Arg262
    Noritaka Ariyoshi
    Division of Pharmacy, University Hospital, Chiba University School of Medicine, 1 8 1 Inohana, Chuo Ku, Chiba 260 8677, Japan
    Drug Metab Dispos 39:2045-8. 2011
    There are a number of reports indicating that CYP2B6*6 (c.516G>T and c...
  31. pmc Effects of the CYP2B6*6 allele on catalytic properties and inhibition of CYP2B6 in vitro: implication for the mechanism of reduced efavirenz metabolism and other CYP2B6 substrates in vivo
    Cong Xu
    Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Drug Metab Dispos 40:717-25. 2012
    The mechanism by which CYP2B6*6 allele alters drug metabolism in vitro and in vivo is not fully understood...
  32. pmc Worldwide variation in human drug-metabolism enzyme genes CYP2B6 and UGT2B7: implications for HIV/AIDS treatment
    Jing Li
    Department of Evolutionary Genetics, Max Planck Institute for Evolutionary Anthropology, Leipzig, Germany
    Pharmacogenomics 13:555-70. 2012
    Hepatic enzymes, CYP2B6 and UGT2B7 play a major role in the metabolism of the widely used antiretroviral drugs efavirenz, nevirapine and zidovudine...
  33. doi Contribution of CYP2B6 alleles in explaining extreme (S)-methadone plasma levels: a CYP2B6 gene resequencing study
    Maria Dobrinas
    Unit of Pharmacogenetics and Clinical Psychopharmacology, Department of Psychiatry, Centre for Psychiatric Neurosciences, University Hospital Center, University of Lausanne, Lausanne
    Pharmacogenet Genomics 23:84-93. 2013
    S)-Methadone, metabolized mainly by CYP2B6, shows a wide interindividual variability in its pharmacokinetics and pharmacodynamics.
  34. pmc CYP2B6 non-coding variation associated with smoking cessation is also associated with differences in allelic expression, splicing, and nicotine metabolism independent of common amino-acid changes
    A Joseph Bloom
    Department of Psychiatry, Washington University School of Medicine, St Louis, Missouri, United States of America
    PLoS ONE 8:e79700. 2013
    The Cytochrome P450 2B6 (CYP2B6) enzyme makes a small contribution to hepatic nicotine metabolism relative to CYP2A6, but CYP2B6 is the primary enzyme responsible for metabolism of the smoking cessation drug bupropion...
  35. ncbi Homozygous CYP2B6 *6 (Q172H and K262R) correlates with high plasma efavirenz concentrations in HIV-1 patients treated with standard efavirenz-containing regimens
    Kiyoto Tsuchiya
    AIDS Clinical Center, International Medical Center of Japan, Tokyo 162 8655, Japan
    Biochem Biophys Res Commun 319:1322-6. 2004
    Efavirenz (EFV) is metabolized by cytochrome P450 2B6 (CYP2B6) in the liver. We analyzed the genotypes of CYP2B6 and their contribution to plasma EFV concentrations in 35 EFV-treated patients in International Medical Center of Japan...
  36. ncbi Association of cyclophosphamide pharmacokinetics to polymorphic cytochrome P450 2C19
    R Timm
    Institute of Pharmacology, Ernst Moritz Arndt University Greifswald, Germany
    Pharmacogenomics J 5:365-73. 2005
    ..patients using a global and a population pharmacokinetic model considering functionally relevant polymorphisms of CYP2B6, CYP2C9, CYP2C19, CYP3A5, and GSTA1...
  37. ncbi Pharmacogenetics of cyclophosphamide in patients with hematological malignancies
    Hanjing Xie
    Department of Laboratory Medicine, Division of Clinical Pharmacology, Karolinska Institutet, SE 141 86 Stockholm, Sweden
    Eur J Pharm Sci 27:54-61. 2006
    ..The pharmacokinetics of CPA and its active metabolite were related to the genotype of CYP2B6, CYP2C9 and CYP2C19. The influence of liver function on CPA metabolism was also evaluated.
  38. pmc Interpatient variability in the pharmacokinetics of the HIV non-nucleoside reverse transcriptase inhibitor efavirenz: the effect of gender, race, and CYP2B6 polymorphism
    David Burger
    Radboud University Medical Center Nijmegen, The Netherlands
    Br J Clin Pharmacol 61:148-54. 2006
    ..To characterize the demographic and pharmacogenetic factors that influence interpatient variability in the plasma concentrations of the HIV non-nucleoside reverse transcriptase inhibitor efavirenz...
  39. ncbi ABCB1 and cytochrome P450 genotypes and phenotypes: influence on methadone plasma levels and response to treatment
    Severine Crettol
    Unite de Biochimie et Psychopharmacologie Clinique, Centre de Neurosciences Psychiatriques, Département de Psychiatrie Centre Hospitalier Universitaire Vaudois, Hôpital de Cery, Prilly Lausanne, Switzerland
    Clin Pharmacol Ther 80:668-81. 2006
    The in vivo implication of various cytochrome P450 (CYP) isoforms and of P-glycoprotein on methadone kinetics is unclear. We aimed to thoroughly examine the genetic factors influencing methadone kinetics and response to treatment.
  40. ncbi CYP2B6 genotype alters abstinence rates in a bupropion smoking cessation trial
    Anna M Lee
    Centre for Addiction and Mental Health and the Department of Pharmacology, University of Toronto, 1 King s College Circle Toronto, Ontario, Canada
    Biol Psychiatry 62:635-41. 2007
    b>CYP2B6 is the primary enzyme involved in bupropion (Zyban; GlaxoSmithKline, Research Triangle Park, North Carolina) metabolism...
  41. ncbi Efavirenz pharmacokinetics in HIV-1-infected children are associated with CYP2B6-G516T polymorphism
    Akihiko Saitoh
    Division of Infectious Diseases, Department of Pediatrics, University of California, San Diego, La Jolla, CA 92093 0672, USA
    J Acquir Immune Defic Syndr 45:280-5. 2007
    The CYP2B6-G516T polymorphism has been shown to alter plasma efavirenz (EFV) concentrations in adults...
  42. ncbi Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6 *6 and *26
    Hiroyuki Gatanaga
    AIDS Clinical Center, International Medical Center of Japan, Tokyo, Japan
    Clin Infect Dis 45:1230-7. 2007
    Efavirenz (EFV) is metabolized primarily by cytochrome P450 2B6 (CYP2B6), and high plasma concentrations of the drug are associated with a G-->T polymorphism at position 516 (516G-->T) of CYP2B6 and frequent central nervous system (..
  43. ncbi Gene-gene interactions between CYP2B6 and CYP2A6 in nicotine metabolism
    Huijun Z Ring
    Center for Health Sciences, SRI International, Menlo Park, CA, USA
    Pharmacogenet Genomics 17:1007-15. 2007
    ..We investigated the influence of genetic variation in another potential nicotine-metabolizing enzyme, CYP2B6, and its interaction with CYP2A6, on the metabolism of nicotine.
  44. doi Aberrant splicing caused by single nucleotide polymorphism c.516G>T [Q172H], a marker of CYP2B6*6, is responsible for decreased expression and activity of CYP2B6 in liver
    Marco H Hofmann
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany and University of Tübingen, Auerbachstrasse 112, 70376 Stuttgart, Germany
    J Pharmacol Exp Ther 325:284-92. 2008
    b>CYP2B6 is a polymorphic human drug metabolizing cytochrome P450 with clinical relevance for several drug substrates including cyclophosphamide, bupropion, and efavirenz. The common allele CYP2B6*6 [c. 516G>T, Q172H, and c...
  45. pmc Pharmacokinetics of efavirenz when co-administered with rifampin in TB/HIV co-infected patients: pharmacogenetic effect of CYP2B6 variation
    Awewura Kwara
    The Miriam Hospital, 164 Summit Avenue, Providence, RI 02906, USA
    J Clin Pharmacol 48:1032-40. 2008
    The goal of this study was to determine the effect of CYP2B6 genetic variation on the steady-state pharmacokinetics of efavirenz (600 mg/d) in TB/HIV co-infected patients receiving concomitant rifampin, a potent CYP inducer...
  46. pmc CYP2B6 (c.516G-->T) and CYP2A6 (*9B and/or *17) polymorphisms are independent predictors of efavirenz plasma concentrations in HIV-infected patients
    Awewura Kwara
    The Miriam Hospital, Providence, RI 02906, USA
    Br J Clin Pharmacol 67:427-36. 2009
    Interindividual variability in efavirenz pharmacokinetics is not entirely explained by the well-recognized CYP2B6 516G-->T single nucleotide polymorphism...
  47. pmc A novel polymorphism in ABCB1 gene, CYP2B6*6 and sex predict single-dose efavirenz population pharmacokinetics in Ugandans
    Jackson K Mukonzo
    Division of Clinical Pharmacology, Department of Laboratory Medicine, Karolinska University Hospital Huddinge, Karolinska Institutet, Stockholm, Sweden
    Br J Clin Pharmacol 68:690-9. 2009
    ....
  48. doi CYP2B6 gene single nucleotide polymorphisms and leukemia susceptibility
    Zhong hai Yuan
    Department of Hematology, Peking University First Hospital, Beijing, China
    Ann Hematol 90:293-9. 2011
    b>CYP2B6 is a highly variable and polymorphic cytochrome P450 enzyme which plays a vital role in the degradation of some endogenous metabolites, xenobiotics, and harmful compounds...
  49. ncbi CYP2B6 and OPRM1 gene variations predict methadone-related deaths
    Hannah Bunten
    Centre for Forensic Sciences, Bournemouth University, UK
    Addict Biol 16:142-4. 2011
    ..A significant association between high methadone concentrations and the CYP2B6*6 allele characteristic of the slow metabolizer phenotype was identified...
  50. ncbi Determinants of the rate of nicotine metabolism and effects on smoking behavior
    Elaine Johnstone
    Department of Clinical Pharmacology, Cancer Research UK Medical Statistics Group, Centre for Statistics in Medicine, University of Oxford, Oxford, United Kingdom
    Clin Pharmacol Ther 80:319-30. 2006
    Studies on cytochrome P450 (CYP) 2A6 suggest that genotype affects the rate of nicotine metabolism and, consequently, cigarette consumption...
  51. ncbi cDNA cloning and sequence and cDNA-directed expression of human P450 IIB1: identification of a normal and two variant cDNAs derived from the CYP2B locus on chromosome 19 and differential expression of the IIB mRNAs in human liver
    S Yamano
    Laboratory of Molecular Carcinogenesis, National Cancer Institute, Bethesda, Maryland 20892
    Biochemistry 28:7340-8. 1989
    A cDNA designated hIIB1, representing the entire coding sequence of a P450 in the IIB gene family, was isolated from a human liver lambda gt11 library by using the rat IIB1 cDNA as a probe...
  52. pmc Alternative splicing in the human cytochrome P450IIB6 gene generates a high level of aberrant messages
    J S Miles
    Imperial Cancer Research Fund, University Department of Biochemistry, Edinburgh, UK
    Nucleic Acids Res 17:8241-55. 1989
    Polymorphisms within the human cytochrome P450 system can have severe clinical consequences and have been associated with adverse drug side effects and susceptibility to environmentally linked diseases such as cancer...
  53. ncbi Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver
    T Lang
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Pharmacogenetics 11:399-415. 2001
    ..A specific direct sequencing strategy was developed based on CYP2B6 and CYP2B7 genomic sequence information and DNA from 35 subjects was completely analysed for mutations throughout all nine ..
  54. ncbi Pharmacogenetic investigation of smoking cessation treatment
    Caryn Lerman
    Department of Psychiatry, Abramson Cancer Center, University of Pennsylvania, Philadelphia, PA 19104, USA
    Pharmacogenetics 12:627-34. 2002
    Despite the efficacy of bupropion for smoking cessation, smokers exhibit variability in treatment outcome. The CYP2B6 gene has been implicated in bupropion kinetics and nicotine metabolism, and is a plausible candidate for pharmacogenetic ..
  55. pmc Prevalence of CYP2B6 alleles in malaria-endemic populations of West Africa and Papua New Guinea
    Rajeev K Mehlotra
    Center for Global Health and Diseases, School of Medicine, Case Western Reserve University, Wolstein Research Building 4204, Cleveland, OH 44106 7286, USA
    Eur J Clin Pharmacol 62:267-75. 2006
    b>Cytochrome P450 2B6 (CYP2B6) is involved in the metabolism of artemisinin drugs, a novel series of antimalarials...
  56. pmc Pharmacogenetic clinical trial of sustained-release bupropion for smoking cessation
    Sean P David
    Brown University Center for Primary Care and Prevention, Providence, RI 02860, USA
    Nicotine Tob Res 9:821-33. 2007
    ..were genotyped for the dopamine D2 receptor (DRD2-Taq1A), dopamine transporter (SLC6A3 3' VNTR), and cytochrome P450 2B6 (CYP2B6 1459 CT) polymorphisms...
  57. ncbi CYP2B6 genetic variants are associated with nevirapine pharmacokinetics and clinical response in HIV-1-infected children
    Akihiko Saitoh
    Division of Infectious Diseases, Department of Pediatrics, University of California, San Diego, La Jolla, California 92093 0672, USA
    AIDS 21:2191-9. 2007
    b>Cytochrome P450 2B6 (CYP2B6)-G516T genotype is associated with altered activity of hepatic CYP2B6 and efavirenz pharmacokinetics, but the relationship between the CYP2B6-G516T genotype and nevirapine (NVP) pharmacokinetics in plasma and ..
  58. 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 ..
  59. pmc Polymorphisms of drug-metabolizing enzymes (GST, CYP2B6 and CYP3A) affect the pharmacokinetics of thiotepa and tepa
    Corine Ekhart
    Department of Pharmacy and Pharmacology, The Netherlands Cancer Institute Slotervaart Hospital, Amsterdam, The Netherlands
    Br J Clin Pharmacol 67:50-60. 2009
    ..The purpose of this study was to evaluate effects of known allelic variants in CYP2B6, CYP3A4, CYP3A5, GSTA1 and GSTP1 genes on pharmacokinetics of thiotepa and tepa.
  60. doi Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals
    M Arab-Alameddine
    Division of Clinical Pharmacology and Toxicology, University Hospital Center, University of Lausanne, Lausanne, Switzerland
    Clin Pharmacol Ther 85:485-94. 2009
    Besides CYP2B6, other polymorphic enzymes contribute to efavirenz (EFV) interindividual variability. This study was aimed at quantifying the impact of multiple alleles on EFV disposition...
  61. doi CYP2B6 G516T genotyping in a UK cohort of HIV-positive patients: polymorphism frequency and influence on efavirenz discontinuation
    Vicki Powers
    Department of Biochemistry, University Hospitals Bristol NHS Foundation Trust, Bristol Royal Infirmary, Bristol, UK
    HIV Med 10:520-3. 2009
    ..reverse transcriptase inhibitor (NNRTI) efavirenz undergoes phase I metabolism by the cytochrome P450 enzyme, CYP2B6. Previous studies outside of the United Kingdom have shown associations between the CYP2B6 polymorphism G516T and ..
  62. 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...
  63. doi Influence of host genetic factors on efavirenz plasma and intracellular pharmacokinetics in HIV-1-infected patients
    Laure Elens
    Louvain Centre for Toxicology and applied Pharmacology, Universite Catholique de Louvain, 53 02, avenue E Mounier, 1200 Bruxelles, Belgium
    Pharmacogenomics 11:1223-34. 2010
    ..Previous studies have identified some possible genetic determinants of the variability in plasma concentrations. However, their impact on EFV intracellular pharmacokinetics remains mostly unexplored...
  64. pmc Effect of CYP2B6*6 and CYP2C19*2 genotype on chlorpyrifos metabolism
    Alice L Crane
    Department of Pharmacology and Toxicology, State University of New York at Buffalo, Buffalo, NY 14214, USA
    Toxicology 293:115-22. 2012
    ..Human CYP2B6 has the highest reported Vmax)/Km (intrinsic clearance--CL(int)) for bioactivation while CYP2C19 has the highest ..
  65. pmc CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients
    Awewura Kwara
    Warren Alpert Medical School of Brown University, Rhode Island, USA
    AIDS 23:2101-6. 2009
    ..In this study, we determined whether selected UGT2B7 polymorphisms could be used to enhance the prediction of efavirenz plasma concentrations from CYP2B6 and CYP2A6 genotypes.
  66. ncbi Mechanisms of multidrug resistance in cancer treatment
    A L Harris
    Molecular Oncology Laboratory, University of Oxford, John Radcliffe Hospital, Headington, UK
    Acta Oncol 31:205-13. 1992
    ..g. A45. 5) Drug activation. Mitomycin C as well as cyclophosphamide and VP16 require activation for their effects. Low levels of cytochrome p450 reductase are associated with MMC resistance.
  67. ncbi [Cardiac side effects of anti-HIV agents]
    J J Monsuez
    , , Villejuif
    Arch Mal Coeur Vaiss 93:835-40. 2000
    ..the prevention more effective, especially with the association with HIV antiproteases which inhibit the cytochrome P450. The diagnosis of iatrogenic myocardial dysfunction is more difficult, except when it occurs acutely as with ..
  68. pmc Conversion of glyceryl trinitrate to nitric oxide in tolerant and non-tolerant smooth muscle and endothelial cells
    D Salvemini
    William Harvey Research Institute, St Bartholomew s Hospital Medical College, Charterhouse Square, London
    Br J Pharmacol 108:162-9. 1993
    ..SBP) an inhibitor of glutathione-S-transferase (GST), by metyrapone or SKF-525A inhibitors of cytochrome P450. These experiments were confirmed by organ bath studies using rabbit aortic strips denuded of endothelium and ..
  69. ncbi Site-directed mutagenesis of cytochrome P450scc. II. Effect of replacement of the Arg425 and Arg426 residues on the structural and functional properties of the cytochrome P450scc
    T N Azeva
    Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Minsk, 220141, Belarus
    Biochemistry (Mosc) 66:564-75. 2001
    Cytochrome P450-dependent monooxygenases, in spite of their wide distribution, can be simply divided into a few groups differing in the location of the electron transfer chain and their composition...
  70. ncbi Role of hepatocellular regeneration in CCl4 autoprotection
    K N Thakore
    Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson 39216 4505
    Toxicol Pathol 19:47-58. 1991
    The destruction of liver microsomal cytochromes P450 by a previously administered low dose of CCl4 has been widely accepted as the mechanism of CCl4 autoprotection...
  71. ncbi Lipid peroxidation and cancer: a critical reconsideration
    M U Dianzani
    Department of Experimental Medicine and Oncology, University of Turin, Italy
    Tumori 75:351-7. 1989
    ..chain, whereas ascorbate/iron-induced stimulation does not require the presence of an efficient cytochrome P450-chain...
  72. pmc Selective inhibition by barbiturates of the synthesis of endothelium-derived hyperpolarizing factor in the rabbit carotid artery
    V Lischke
    Centre of Physiology, Johann Wolfgang Goethe University Clinic, Frankfurt am Main, Germany
    Br J Pharmacol 115:969-74. 1995
    ..01-10 microM), on the other hand, was only marginally affected by these anaesthetics. 4. The cytochrome P450 inhibitor, clotrimazole (3-100 microM), mimicked the inhibitory effect of thiopentone and methohexitone on the NO/..
  73. pmc Characterization and modulation of EDHF-mediated relaxations in the rat isolated superior mesenteric arterial bed
    A I McCulloch
    Department of Physiology and Pharmacology, University of Nottingham Medical School, Queen s Medical Centre
    Br J Pharmacol 120:1431-8. 1997
    ..4 +/- 3.4% high K+, n = 7; 83.1 +/- 3.1% control, n = 7). 5. In the presence of the cytochrome P450 inhibitor, clotrimazole (1 microM, n = 5 and 10 microM, n = 4), the dose-response curve to carbachol was ..
  74. ncbi Effect of extracellular matrix on the expression of peroxisome proliferation associated genes in cultured rat hepatocytes
    J T Hong
    Graduate Center for Toxicology, University of Kentucky, Lexington, KY 40506, USA
    Toxicol In Vitro 14:177-84. 2000
    ..beta-oxidation pathway, and lauric acid hydroxylase (LAH), which represents the activity of the cytochrome P450 4A subfamily-in rat hepatocytes cultured on different plates: plastic, collagen-coated, thin and thick Matrigel, ..
  75. 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
    ..In the present study, immunoblotting with polyclonal anti-rat and anti-human cytochrome P450 (CYP) antibodies revealed the presence of proteins in pig liver which cross-reacted with anti-human CYP1A2, CYP2D6 ..
  76. ncbi Induction by xenobiotics of phase I and phase II enzyme activities in the human keratinocyte cell line NCTC 2544
    A Gelardi
    Department of Experimental Medicine, General Pathology Division, University of Genoa, Via L.B. Alberti, 16132, Genova, Italy
    Toxicol In Vitro 15:701-11. 2001
    ..During incubations lasting up to 144 h in the presence of the classical cytochrome P450 inducers beta-naphthoflavone (BNF), 3-methylcholanthrene (MC) and phenobarbital (PB), a considerable and ..
  77. ncbi Endothelial regulation of vascular tone and growth
    T F Luscher
    Department of Medicine, University Hospital, Basel, Switzerland
    Am J Hypertens 6:283S-293S. 1993
    ..endothelium-derived relaxing factors include a hyperpolarizing factor, lipooxygenase products, and the cytochrome P450 pathway...
  78. pmc Inhibitory effects of nordihydroguaiaretic acid on ETA-receptor-mediated contractions to endothelin-1 in rat trachea
    P J Henry
    Department of Pharmacology, University of Western Australia, Nedlands
    Br J Pharmacol 111:561-9. 1994
    ..contractions were not the result of any significant actions of NDGA on lipoxygenase, cytochrome P450, L- orT-type Ca2+-channels, Na+-channels or protein kinase C.8...
  79. ncbi Blue light mediated photoreduction of the flavoprotein NADPH-cytochrome P450 reductase. A Förster-type energy transfer
    D Muller-Enoch
    Abteilung Physiologische Chemie, Universitat Ulm, Germany
    Z Naturforsch C 52:605-14. 1997
    ..of the fluorophores umbelliferone, FAD and FMN and of the FAD and FMN containing flavoprotein NADPH-cytochrome P450 reductase of different oxydation-reduction states are documented...
  80. ncbi Molecular and cellular mechanisms used in the acute phase of stimulated steroidogenesis
    M Thomson
    Department of Biological Sciences, University of Western Sydney Nepean, Kingswood, Australia
    Horm Metab Res 30:16-28. 1998
    ..Cholesterol is transported through the contact sites to the inner membrane and on reaching cytochrome P450 side chain cleavage (P450scc), cholesterol is converted to pregnenolone...
  81. ncbi Abnormal pressure-natriuresis in hypertension: role of cytochrome P450 metabolites of arachidonic acid
    C Moreno
    Department of Physiology, Medical College of Wisconsin, Milwaukee 53226, USA
    Am J Hypertens 14:90S-97S. 2001
    ..In the kidney, cytochrome P450 (CYP) enzymes metabolize AA primarily to 20-HETE and EETs...
  82. ncbi Cocaine hepatotoxicity in mice: histologic and enzymatic studies
    S Z Mehanny
    Department of Pharmacology Toxicology, New Jersey Medical School UMDNJ, Newark 07103 2714
    Toxicol Pathol 19:24-9. 1991
    ..Although hepatic cytochrome P450 was slightly increased in the low dose groups, a reduction in the enzyme activity was noticed in the group treated ..
  83. 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
    Aflatoxin B(1) (AFB(1)) biotransformation comprises cytochrome P450-mediated reactions resulting in hydroxylated and demethylated metabolites as well as AFB(1) epoxides...
  84. ncbi Role of residue 480 in substrate specificity of cytochrome P450 2B5 and 2B11
    J Liu
    Department of Pharmacology and Toxicology, College of Pharmacy, University of Arizona, Tucson 85721, USA
    Arch Biochem Biophys 327:167-73. 1996
    The role of residue 480 as a determinant of the specificities of cytochrome P450 2B5 and 2B11 toward androstenedione, progesterone, 2,2',4,4',5,5'-hexachlorobiphenyl (245-HCB), and benzyloxyresorufin has been investigated...
  85. pmc NH2-terminal substitutions of basic amino acids induce translocation across the microsomal membrane and glycosylation of rabbit cytochrome P450IIC2
    E Szczesna-Skorupa
    Department of Physiology and Biophysics, University of Illinois, Urbana 61801
    J Cell Biol 108:1237-43. 1989
    ..cleavage in the hybrid protein occurred after glycine 25, which is derived from [2-lys,3-arg]P450IIC2, cytochrome P450 sequences COOH terminal to the cleavage site must decrease cleavage efficiency...
  86. ncbi The role of the cytochrome P450-dependent metabolites of arachidonic acid in blood pressure regulation and renal function: a review
    M Rahman
    Department of Medicine, Case Western Reserve University, School of Medicine, Cleveland, Ohio 44106-4982, USA
    Am J Hypertens 10:356-65. 1997
    Arachidonic acid metabolism through the cytochrome P450-dependent monooxygenase system has been the subject of considerable research interest over the last several years...
  87. ncbi Inducible membranes in yeast: relation to the unfolded-protein-response pathway
    R Menzel
    Department of Cell Biology, , Berlin Buch, Germany
    Yeast 13:1211-29. 1997
    Overproduction of an endoplasmic reticulum (ER)-resident membrane protein (cytochrome P450 52A3) and of a secretory protein (invertase) was used to study the regulation of the luminal ER protein Kar2p under conditions that lead to ER ..
  88. ncbi [A new cause of resistant arterial hypertension: coprescription with anticonvulsant treatments]
    P Iaria
    , , Paris
    Arch Mal Coeur Vaiss 92:1005-8. 1999
    ..explanation can be hypothesis: several antihypertensive drugs are liver-metabolised by microsomal cytochrome P450 3A4 isoform that could explain a significantly decreased half-life in association with enzymatic inducers, such as ..
  89. ncbi Causal connection between detoxification enzyme activity and consumption of a toxic plant compound
    M J Snyder
    Department of Entomology, University of Arizona, Tucson 85721, USA
    J Comp Physiol A 179:255-61. 1996
    ..For example, larval tobacco hornworms (Manduca sexta) experience a dramatic increase in cytochrome P450 activity against nicotine after ingesting nicotine...
  90. 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...
  91. ncbi [Calcium inhibitors in the management of hypertensive patients on cyclosporine]
    C Bagnis
    , , Paris
    Arch Mal Coeur Vaiss 91:411-4. 1998
    ..Cyclosporine is metabolised in the liver by cytochrome P450 3A4 dependant enzymes...
  92. 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...
  93. ncbi Coronary vasodilator responses to bradykinin in euglycemic and diabetic rats
    M B Given
    Department of Medicine, Louisiana State University Medical Center, New Orleans, USA
    Am J Hypertens 14:446-54. 2001
    ..Bradykinin-stimulated vasodilation of the rat coronary vasculature is mediated by a cytochrome P450-1A (CYP-1A)- inhibitable metabolite that activates KCa, but not KATP, channels on the coronary vascular smooth ..
  94. ncbi Effects of interferon-gamma and streptolysin O on hepatic procainamide N-acetyltransferase and various microsomal cytochrome P450-dependent monooxygenases in rats
    R Walter
    Department of Pharmacology, Medical Faculty of the Ernst-Moritz-Arndt University, Greifswald, Germany
    Immunopharmacol Immunotoxicol 18:571-86. 1996
    ..O (SLO, 100 HU/kg iv for 5 days) on hepatic cytosolic N-acetyltransferase (NAT) and microsomal cytochrome P450 (CYP)-dependent monooxygenases in male Wistar rats. Both IFN gamma and SLO activated NAT to 120% (P < 0...
  95. ncbi A direct, highly sensitive fluorometric assay for a microsomal cytochrome P450-mediated O-demethylation using a novel coumarin analog as substrate
    R Roser

    Z Naturforsch C 55:915-22. 2000
    ..as substrate enables the fluorometric determination of the O-dealkylation activity of a cytochrome P450-dependent monooxygenase system in rat liver which is inducible by phenobarbital but not by 3-methylcholanthrene.
  96. ncbi [Acute phenytoin poisoning secondary to an interaction with ticlopidine]
    N López-Ariztegui
    Servicio de Neurologia, Hospital General Universitario Gregorio Maranon, Madrid, Espana
    Rev Neurol 26:1017-8. 1998
    ..Their association is not uncommon, since there is a high incidence of epileptic crises of vascular origin in adults...
  97. ncbi St John's wort, a herbal antidepressant, activates the steroid X receptor
    J M Wentworth
    Department of Medicine, University of Cambridge, Addenbrooke's Hospital, Cambridge, CB2 2QQ, UK
    J Endocrinol 166:R11-6. 2000
    ..Steroid X receptor (SXR), an orphan nuclear receptor, induces hepatic cytochrome P450 gene expression in response to diverse endogenous steroids, xenobiotics and drugs...
  98. ncbi Effects of ethyl carbamate and its metabolites on the antibody response in splenocyte cultures from female Balb/C mice
    T C Jeong
    Toxicology Research Center, Korea Research Institute of Chemical Technology, Taejon
    Immunopharmacol Immunotoxicol 18:91-103. 1996
    To investigate a possible role by cytochrome P450 (P450) in ethyl carbamate-induced immunosuppression, an attempt to assess the ability of ethyl carbamate, its metabolites produced by P450 (i.e...
  99. ncbi P450 monooxygenase in biotechnology. I. Single-step, large-scale purification method for cytochrome P450 BM-3 by anion-exchange chromatography
    U Schwaneberg
    , , Germany
    J Chromatogr A 848:149-59. 1999
    An efficient single-step purification protocol for recombinant cytochrome P450 BM-3 from Bacillus megaterium, expressed in E. coli, was developed. Functional crude protein was obtained by disintegrating induced E...
  100. ncbi Chloroform bioactivation leading to nucleic acids binding
    A Colacci
    Istituto Nazionale per la Ricerca sul Cancro, IST-Genova, Italy
    Tumori 77:285-90. 1991
    ..In an in vitro cell-free system, chloroform was bioactivated by cytochrome P450-dependent microsomal fractions, by cytosolic GSH-transferases from rat and mouse liver, and particularly by the ..

Research Grants71

  1. Characterization of a Novel Selective Cytochrome P450 3A5 Substrate
    MICHAEL DARIN CAMERON; Fiscal Year: 2013
    ..drugs interferes with the activity of key enzymes involved in drug metabolism, chiefly enzymes in the cytochrome P450 family...
  2. Inhibition of Carboxylesterase Metabolism by Ethanol
    Robert B Parker; Fiscal Year: 2011
    ..Drug interactions involving inhibition of cytochrome P450 enzymes are well known causes of adverse drug events...
  3. Maria Almira Correia; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): The hepatic cytochromes P450 (P450s) are endoplasmic-reticulum membrane-anchored enzymes engaged in the breakdown of endo- and xenobiotics i.e...
  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. Interaction of Alcohol and HAART in HIV/AIDS and HIV/AIDS and HCV Coinfection
    Elinore F McCance Katz; Fiscal Year: 2011
    ..significant interactions which may occur between drugs commonly used to treat HIV disease known to be cytochrome P450 (CYP450) inducers or inhibitors and alcohol, the most frequently abused substance in the United States...
  6. Angela M Brodie; Fiscal Year: 2014
    ..the hERG mediated potassium currents in Human Embryonic Kidney cells and minimal effects on a panel of cytochrome P450 enzymes commonly used to predict drug-drug interactions...
  7. Christopher A Reilly; Fiscal Year: 2014
    DESCRIPTION (provided by applicant): Bioactivation of xenobiotics to toxic intermediates through cytochrome P450 oxygenation mechanisms is a well recognized process...
  8. EDWARD THOMAS MORGAN; Fiscal Year: 2016
    ..Elevated production of NO in rat hepatocytes caused by inflammatory stimuli elicits the stimulated degradation of CYP2B enzymes via the ubiquitin-proteasome system, and there is evidence that a similar mechanism exists in human ..
  9. Todd C Skaar; Fiscal Year: 2016
    ..factor that contributes to variable drug metabolism is developmental change in the expression of the cytochrome P450 (CYP450) enzymes;this is a particularly important factor to consider in infants and young children...
  10. James R Halpert; Fiscal Year: 2014
    ..is to determine the mechanistic basis for the atypical kinetics of substrate oxidation by human CYP3A4, the major P450 in adult liver and intestine...
  11. Phase 2 SBIR: Zebrafish Cytochrome P450 Assays for Assessing Drug Metabolism and
    CHUNQI LI; Fiscal Year: 2010
    Cytochrome P450 (CYP) enzymes catalyze the majority of known drug metabolism and the bulk of these reactions occur in the liver...
  12. 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 ..
  13. Hepatic drug metabolism in inflammation
    Romi Ghose; Fiscal Year: 2009
    ..be directly targeted by lipopolysaccharide (LPS) from gram negative bacteria resulting in suppression of Cytochrome P450 gene expression...
  14. Molecular Mechanisms &Importance of Oxidative Stress in Estrogen-Induced Carcino
    Hari K Bhat; Fiscal Year: 2011
    ..2);the role of oxidative stress in modifying ER-dependent gene regulation (Specific Aim 3);and, the role cytochrome P450 1B1 in estrogen-induced oxidative stress and subsequent carcinogenesis (Specific Aim 4)...
  15. 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...
  16. 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%..
  17. Xinxin Ding; Fiscal Year: 2016
    ..DESCRIPTION (provided by applicant): The long-term objective is to determine the role of respiratory tract cytochrome P450 (P450 or CYP) enzymes in target tissue metabolic activation and toxicity of environmental chemicals...
  18. Mariana Cherner; Fiscal Year: 2015
    DESCRIPTION (provided by applicant): Although cytochrome P450-2D6 (CYP2D6) is the primary enzyme responsible for methamphetamine (meth) metabolism, no work has been conducted outside of our group on its role in meth-related brain ..
  19. Tamoxifen biotransformation pathway pharmacogenomics
    MATTHEW PHILIP GOETZ; Fiscal Year: 2013
    ..Tamoxifen requires metabolic activation by cytochrome P450 (CYP) 2D6 to fully elicit its pharmacological activity...
  20. Lucy A Waskell; Fiscal Year: 2014
    DESCRIPTION (provided by applicant): The cytochrome P450 (cyt P450) superfamily consists of more than 11,000 members...
  21. Sunil Parikh; Fiscal Year: 2016
    ..ACTs exhibit complex pharmacology, undergo activation and/or metabolism via cytochrome p450 pathways and are susceptible to physiological differences and drug-drug interactions with ARTs...
  22. John C Hackett; Fiscal Year: 2014
    DESCRIPTION (provided by applicant): The cytochrome P450 enzymes (CYPs) are essential for the biosynthesis of numerous natural products, steroid hormones, and eicosanoids, as well as the clearance of most drugs...
  23. Herb-Drug Glucuronidation Interactions
    Reginald F Frye; Fiscal Year: 2011
    ..Accordingly, serious adverse herb- drug interactions resulting from the induction or inhibition of cytochrome P450 enzymes and/or the efflux transporter P-glycoprotein have been reported...
  24. ZHUO MICHAEL WANG; Fiscal Year: 2014
    ..The human cytochrome P450 4F (CYP4F) subfamily of enzymes has recently been demonstrated to play a significant role in the metabolism of both ..
  25. 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 ..
  26. Mary F Paine; Fiscal Year: 2014
    ..Preliminary 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 ..
  27. Disulfiram Interactions With HIV Medications: Clinical Implications
    Elinore F McCance Katz; Fiscal Year: 2010
    ..DIS is an inhibitor of aldehyde dehydrogenases (ALDH) and has been reported to alter hepatic cytochrome P450 enzyme function important to metabolism of many drugs frequently used in the treatment of HIV/AIDS...
  28. Concurrent HAART and Tuberculosis Treatment: Drug to Drug Interactions
    AWEWURA JACOB KWARA; Fiscal Year: 2010
    ..Further, the interaction between rifampin and CYP2B6*6 carrier status and other host factors on the disposition and responses to efavirenz will determined...
  29. Stephen G Sligar; Fiscal Year: 2014
    ..Efforts focus on the human hepatic cytochromes P450 that are central players in drug metabolism...
  30. SIG Program: AKTAxpress FPLC System for Protein Purification
    Frances H Arnold; Fiscal Year: 2010
    ..This instrument will support research into the structural basis of cytochrome P450 function and engineering new P450s for synthesis of human metabolites and drug lead diversification (Arnold), ..
  31. Genetic predictors of thiazolidinedione response
    Christina L Aquilante; Fiscal Year: 2010
    ..The studies proposed within this application will focus on genetic variation within the cytochrome P450 2C8 (CYP2C8) metabolizing enzyme gene. CYP2C8 is responsible for the hepatic metabolism of TZDs...
  32. Safety, Efficacy, and Mechanisms in American Ginseng in HIV-Related Fatigue
    Adriana S A Andrade; Fiscal Year: 2012
    ..However, data are lacking for CYP2B6, another important isoenzyme...
  33. Early Disease Biomarkers of PCB-exposed Human Population
    Sisir K Dutta; Fiscal Year: 2010
    ..several PCBs and metabolites of PCBs that have been isolated from human blood and tissues, and the gene cytochrome P450 (CYP1A1), which mediates production of OH-PCB by oxidative metabolism, has been found to be 65-fold increased by ..
  34. Maria Almira Correia; Fiscal Year: 2016
    ..causes global translational arrest of de novo synthesis of a myriad of hepatic proteins including cytochromes P450 (P450s), hemoprotein enzymes engaged in the breakdown and clearance of endo- and xenobiotics such as drugs, ..
  35. Linda J Roman; Fiscal Year: 2016
    ..NADPH-cytochrome P450 oxidoreductase (POR) is the sole provider of electrons to the microsomal cytochromes P450 and to heme oxygenase, ..
  36. Human hepatocytes for drug toxicity screening from Cardiac Death Donor livers
    Mark G Clemens; Fiscal Year: 2012
    ..The cells will then be cultured and assessed for urea and albumin production. In addition, cytochrome P450 activity and induction will also be evaluated...
  37. Hepatic CYP enzymes and host-pathogen interactions
    Edward T Morgan; Fiscal Year: 2013
    DESCRIPTION (provided by applicant): Cytochrome P450 (P450) enzymes play crucial roles in the clearance of drugs from the circulation, and therefore changes in their activities can significantly influence the therapeutic and adverse ..
  38. Eric F Johnson; Fiscal Year: 2015
    DESCRIPTION (provided by applicant): Cytochrome P450 (CYP) monooxygenases oxidize a large variety of nutritive and non-nutritive lipids including man-made xenobiotics to reduce toxicity and increase their elimination...
  39. Genetic Susceptibility Factors in Porphyria Cutanea Tarda (PCT)
    Karl Anderson; Fiscal Year: 2009
    ..models, and limited human studies, that polymorphisms in phase I and phase II enzymes, such as cytochrome P450 enzymes (CYPs) and glutathione transferases (GSTs) may contribute to developing PCT...
  40. 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)...
  41. Role of Mitochondrial Aldehyde Dehydrogenases in Ethanol Metabolism and Toxicity
    Vasilis Vasiliou; Fiscal Year: 2010
    ..Ethanol is metabolized to acetaldehyde by the alcohol dehydrogenase enzymes (ADHs), ethanol-inducible cytochrome P450 (CYP2E1) and catalase...
  42. Control of HIV drug resistance in older patients
    Alonso Heredia; Fiscal Year: 2010
    ..unlike HIV non-nucleoside reverse transcriptase and protease inhibitors, neither induce nor inhibit cytochrome P450 3A4, which is responsible for the metabolism of many medications commonly used by the elderly...
  43. Role of hepatic and pulmonary P4501A enzymes in neonatal hyperoxic tissue injury
    XANTHI IOANNA COUROUCLI; Fiscal Year: 2013
    ..The central hypothesis of the proposed study is that hepatic and pulmonary cytochrome P450 (CYP)1A enzymes play a protective role against acute and long-term injury to lung and other organs by oxygen...
  44. Robert J Turesky; Fiscal Year: 2014
    ..These studies will be done with hepatocytes, colorectal cytosols, and in a mouse model where the NADPH- cytochrome P450 reductase gene has been selectively deleted in either the liver or in the small and large intestines...
  45. HEMOPROTEIN OXIDATION AND HEME CATABOLISM
    Paul R Ortiz de Montellano; Fiscal Year: 2013
    ..4. Define the interactions of HO-1 and HO-2 with naturally occurring polymorphic cytochrome P450 reductase (CPR) variants associated with human disease.
  46. Steven M Kawut; Fiscal Year: 2016
    ..Estradiol is metabolized by cytochrome P450 1B1 (CYP1B1) to metabolites which have both pro-angiogenic (16alpha-OHE{1}) and anti-angiogenic (2-OHE, 2-..
  47. COLIN ROBERT JEFCOATE; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): Cytochrome P450 1b1 (Cyp1b1) participates in embryogenesis and is expressed in endothelia, fibroblasts and adipocytes...
  48. Thomas A Kocarek; Fiscal Year: 2014
    ..g., squalestatin 1) selectively induce cytochrome P450 2B (CYP2B) gene expression by causing an endogenous farnesoid to accumulate, which activates the constitutive androstane ..
  49. Interplay between metabolism and FXR activation in scoparone signaling
    Bingfang Yan; Fiscal Year: 2013
    ..In contrast, the enhancement was significantly increased in cells transfected with cytochrome P450 1A2 (CYP1A2), a drug-metabolizing enzyme...
  50. Functional studies of PGRMC1 in cholesterol homeostasis
    PETER JOHN ESPENSHADE; Fiscal Year: 2010
    ..Cytochrome P450 monoxygenases play a key role in regulating cholesterol homeostasis through their functions in cholesterol, ..
  51. Laura L Furge; Fiscal Year: 2015
    DESCRIPTION (provided by applicant): Cytochrome P450 enzymes (CYPs) in humans are a family of heme-containing enzymes involved in metabolism of steroids, vitamins, eiconsanoids, and xenobiotics such as drugs, complex plant alkaloids, ..
  52. The role of PGRMC1 in hepatic cholesterol homeostasis
    RITA THOMAS BROOKHEART; Fiscal Year: 2013
    ..Key regulators of cholesterol synthesis and metabolism are the cytochrome P450 monooxygenases. The synthesis of cholesterol from lanosterol requires the P450 enzyme, Cyp51A1...
  53. Retinoic Acid Modulation for Scleroderma
    BERT J W M OEHLEN; Fiscal Year: 2012
    ..Endogenous ATRA levels can be modulated by inhibition of the Cytochrome P450 CYP26, the key enzyme responsible for ATRA metabolism...
  54. Irina A Pikuleva; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): Cholesterol removal from different organs always involves cytochrome P450 enzymes (CYP or P450) that play key roles in maintenance of cholesterol homeostasis...
  55. The role of cAMP signaling changes in alcoholic liver disease
    VICTORIA LYELL PRINCE; Fiscal Year: 2012
    ..potentially coupled with altered PKA localization, is responsible for mitochondrial localization of the Cytochrome P450 2E1 (CYP2E1) observed during chronic alcohol consumption, and 3) increased PKA activity is responsible for ..
  56. Treatment for alcoholic liver disease
    BERT J W M OEHLEN; Fiscal Year: 2010
    ..Several studies have shown that inhibition of certain cytochrome P450 enzymes in vivo can boost endogenous ATRA levels and result in retinoid-like activity in dermatological and ..
  57. The Impact of Genetic Variability on Human Susceptibility to Chlorpyrifos
    ALICE LANGFORD CRANE; Fiscal Year: 2013
    ..CPF-O is a potent cholinesterase (ChE) inhibitor. Genetic variability in CYP2B6, the CYP enzyme primarily responsible for CPF bioactivation may therefore account for interindividual variability ..
  58. Tobacco/nicotine, cytochrome P450, and HIV-1
    Santosh Kumar; Fiscal Year: 2012
    ..metabolite, cotinine, and other important tobacco-specific compounds are predominantly metabolized by cytochrome P450 2A6 (CYP2A6), especially in the liver, and by lung-specific CYP2A13...
  59. Susceptibility to methylmercury toxicity: A role for cytochrome p450 enzymes
    Matthew D Rand; Fiscal Year: 2013
    ..In a screen for genes that confer tolerance to MeHg during development in Drosophila, we have identified cytochrome p450 (CYP) family members as candidates...
  60. Christopher A Reilly; Fiscal Year: 2014
    ..GCs act locally within the lung where their concentrations are highest and are then metabolized by cytochrome P450 enzymes in situ...
  61. Tracey J Woodruff; Fiscal Year: 2014
    ..we will also generate original human data on whether fetal exposures to PBDEs alter gene expression of cytochrome P450 (CYP) enzymes in the second-trimester human fetal liver and placenta...
  62. Resolution of Inflammation After Trauma/Insult by Cytochrome P450 4F Family
    JORDAN C BELL; Fiscal Year: 2010
    ..This project focuses on the direct role human cytochrome P450 4F (CYP4F) isoforms play in controlling the effects of inflammation signaling...
  63. NADPH P450 REDUCTASE--THYROID HORMONE REGULATION
    David Waxman; Fiscal Year: 2002
    DESCRIPTION: (Adapted from the Investigator's Abstract) NADPH-cytochrome P450 reductase (P450 reductase) is a microsomal flavoprotein that transfers electrons from NADPH to microsomal cytochrome P450...
  64. Cytochrome P450-reductase interactions in P450 1A subfamily
    GRAZYNA SZKLARZ; Fiscal Year: 2007
    unreadable] DESCRIPTION (provided by applicant): Cytochromes P450 (P450s) are heme-containing monooxygenases that play a key role in the metabolic activation of chemical carcinogens and in the metabolism of drugs...
  65. SOLUBLE CYTOCHROME P450 HYDROXYLASES FROM BACTERIA
    ARMAND FULCO; Fiscal Year: 2001
    ..of the research project is the elucidation of the biochemistry, molecular biology, and functions of the cytochrome P450 enzymes induced by barbiturates in the bacterium, Bacillus megaterium...
  66. INTESTINAL AND COLONIC CYTOCHROME P450 GENE EXPRESSION
    Peter Traber; Fiscal Year: 1993
    ..Cytochrome P450 isoenzymes, which are encoded by a large superfamily of related genes play an important role in the metabolism of ..
  67. COMPARISON OF RAT & TROUT HEPATIC P450 INDUCTION
    JOHN LECH; Fiscal Year: 1993
    ..g. other barbiturates, PCBs with ortho chlorines, DDT, phenytoin, 5,5- diphenylhydantoin) hepatic cytochrome P450 inducers control gene expression by using a responsive (rat) and non-responsive model (rainbow trout) to identify ..
  68. DAVID FERNANDO ESTRADA; Fiscal Year: 2014
    DESCRIPTION (provided by applicant): Human cytochrome P450 enzymes are responsible for >90% of drug metabolism and synthesis of important endogenous compounds including hormones...
  69. CYTOCHROME P450 ACTIVE OXYGEN STRUCTURE AND MECHANISMS
    John Dawson; Fiscal Year: 2000
    DESCRIPTION: Understanding dioxygen activation by the cytochrome P450 mono-oxygenases requires knowledge of structure at the molecular level...
  70. 10th International Symposium on Cytochrome P450 Biodiversity and Biotechnology
    John J Stegeman; Fiscal Year: 2010
    ..is for funding for graduate students and post-docs to attend the 10th International Symposium on Cytochrome P450 Biodiversity and Biotechnology...
  71. STRUCTURAL DETERMINANTS OF FUNCTIONAL CYTOCHROME P450
    Byron Kemper; Fiscal Year: 2009
    ..objective of this research is to understand the structural basis for the production of a functional cytochrome P450 (P450) molecule...