Structure, function, regulation and polymorphism and the clinical significance of human cytochrome P450 1A2

Drug Metabolism Reviews
Shu-Feng ZhouJun-Ping Liu


Human CYP1A2 is one of the major CYPs in human liver and metabolizes a number of clinical drugs (e.g., clozapine, tacrine, tizanidine, and theophylline; n > 110), a number of procarcinogens (e.g., benzo[a]pyrene and aromatic amines), and several important endogenous compounds (e.g., steroids). CYP1A2 is subject to reversible and/or irreversible inhibition by a number of drugs, natural substances, and other compounds. The CYP1A gene cluster has been mapped on to chromosome 15q24.1, with close link between CYP1A1 and 1A2 sharing a common 5'-flanking region. The human CYP1A2 gene spans almost 7.8 kb comprising seven exons and six introns and codes a 515-residue protein with a molecular mass of 58,294 Da. The recently resolved CYP1A2 structure has a relatively compact, planar active site cavity that is highly adapted for the size and shape of its substrates. The architecture of the active site of 1A2 is characterized by multiple residues on helices F and I that constitutes two parallel substrate binding platforms on either side of the cavity. A large interindividual variability in the expression and activity of CYP1A2 has been observed, which is largely caused by genetic, epigenetic and environmental factors (e.g., smoking). CYP1A2...Continue Reading


Dec 1, 1979·The Journal of Pharmacy and Pharmacology·M MelzackaJ Maj
Jan 6, 1992·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·K HiroyaM Hatano
Jun 1, 1992·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·F BerthouP H Beaune
Dec 1, 1992·Clinical Pharmacology and Therapeutics·M V RellingW E Evans
May 1, 1992·Archives of Biochemistry and Biophysics·R W LambrechtJ F Sinclair
Aug 1, 1991·Journal of Biochemistry·M KubotaY Fujii-Kuriyama
Oct 1, 1991·Gastroenterology·T AnderssonI Skånberg
Jan 1, 1991·Clinical Pharmacology and Therapeutics·W Kalow, B K Tang
Nov 1, 1989·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·P KochB R von Wartburg
Apr 6, 1989·Biochimica Et Biophysica Acta·T ShimizuY Fujii-Kuriyama
Apr 28, 1989·Biochemical and Biophysical Research Communications·H FuruyaY Fujii-Kuriyama
Aug 1, 1986·The Journal of Pharmacy and Pharmacology·J SeguraE Tarrus
Mar 1, 1987·Advances in Contraception : the Official Journal of the Society for the Advancement of Contraception·A H BandivdekarA R Sheth
Feb 1, 1988·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·F B GjertsenR R Scheline
Oct 1, 1987·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S A SangsterR L Smith
Jun 5, 1987·Journal of Molecular Biology·T L PoulosA J Howard
Jan 1, 1987·British Journal of Clinical Pharmacology·E TarrusJ Segura
Apr 1, 1987·Annals of Internal Medicine·B L LeeP Jacob
Jan 1, 1967·American Journal of Diseases of Children·N T Shahidi
Aug 17, 1984·European Journal of Pharmacology·E Richelson, A Nelson
Feb 1, 1984·Clinical Pharmacology and Therapeutics·M MillerA G Motulsky
Aug 1, 1983·British Journal of Clinical Pharmacology·H W DevonshireR L Smith
Jun 1, 1980·Environmental Health Perspectives·M D Reuber
Jan 1, 1981·Journal of Supramolecular Structure and Cellular Biochemistry·D H PhillipsE C Miller
Oct 26, 1995·Biochemical Pharmacology·S K RoyM E Dolan
Mar 1, 1995·British Journal of Clinical Pharmacology·K T BattyS R Langton
Mar 1, 1995·British Journal of Clinical Pharmacology·H R HaF Follath


Apr 15, 2010·European Journal of Clinical Pharmacology·Natasa DjordjevicEleni Aklillu
Aug 7, 2012·Plant Foods for Human Nutrition·Janet MorffiJ J Espinosa-Aguirre
Oct 19, 2011·SAR and QSAR in Environmental Research·Jayalakshmi SridharC L Klein Stevens
Oct 11, 2012·Pharmacogenetics and Genomics·Lei HuLan Fan
Mar 16, 2013·Pharmacogenetics and Genomics·Maria DobrinasChin B Eap
Jun 24, 2014·Pharmacogenomics·Gillian G JohnsonAndrew R Pettitt
Sep 23, 2014·Oral Surgery, Oral Medicine, Oral Pathology and Oral Radiology·C KragelundJ Reibel
Dec 3, 2014·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Yan PanChin Eng Ong
Apr 18, 2013·Current Cardiology Reports·Kristopher J SwigerPaul A Gurbel
Jul 10, 2012·Expert Opinion on Therapeutic Patents·Miroslav Pohanka
Nov 30, 2013·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Jiawang LiuMaryam Foroozesh
May 31, 2011·Expert Opinion on Drug Metabolism & Toxicology·Patrick du Souich, Caroline Fradette
Apr 10, 2013·Expert Opinion on Drug Metabolism & Toxicology·José A G AgúndezFélix Javier Jiménez-Jiménez
Feb 26, 2013·Drug Metabolism Reviews·Marilyn N MartinezLauren Trepanier
Feb 18, 2015·Drug Metabolism Reviews·Jolantha BeyerleCornelia M Ulrich
Apr 30, 2013·American Heart Journal·Kevin P BlidenPaul A Gurbel
Jul 4, 2012·Cancer Genetics·Sofia PavanelloUlla Vogel
Sep 11, 2010·Forensic Science International : Synergy·Frank MusshoffBurkhard Madea
Sep 24, 2015·Journal of Medicinal Chemistry·Simon J TaylorJason Witherington
Nov 22, 2012·Basic & Clinical Pharmacology & Toxicology·Liqing WangZe-Neng Cheng
Mar 19, 2011·Human Psychopharmacology·Patty M M NooijenRobert J Flanagan
Jul 25, 2012·Journal of Intellectual Disability Research : JIDR·W BraamL Curfs
Oct 19, 2011·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·Shinji TanakaShigeki Arii
Oct 8, 2015·Biological Psychiatry·Cédric GaléraEDEN Mother-Child Cohort Study Group
Aug 29, 2013·BioMed Research International·M D Ronquillo-SánchezJ J Espinosa-Aguirre
Oct 6, 2011·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Li-Ping YangShu-Feng Zhou
Oct 12, 2010·Drug Metabolism and Pharmacokinetics·Joanne Siok Liu LimBalram Chowbay
Jul 11, 2014·Regulatory Toxicology and Pharmacology : RTP·Neil R HartmanThomas Colatsky
Jul 1, 2015·Frontiers in Pharmacology·Hannu RaunioOlli T Pentikäinen
May 24, 2015·International Journal of Epidemiology·Ask Tybjærg NordestgaardBørge Grønne Nordestgaard
Aug 6, 2013·Toxicology in Vitro : an International Journal Published in Association with BIBRA·M J A JettenJ H M van Delft
Sep 17, 2011·Journal of Ethnopharmacology·Ying GuoCurtis D Klaassen

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