Teri Klein, PhD3 and J. Steven Leeder, PharmD, PhD1,2 Purpose: Owing to its highly polymorphic nature and major contri- bution to the metabolism and bioactivation of numerous clinically used drugs, CYP2D6 is one of the most extensively studied drug- metabolizing enzymes and pharma...
Defining screening panel of functional variants of CYP1A1, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 genes in Serbian populationCytochrome P450Molecular autopsyDrug metabolismPlethora of drugs and toxic substances is metabolized by cytochrome P450 enzymes (CYP450). These enzymes are coded by highly ...
There is evidence that the CYP2D6*2 alleles (except CYP2D6*2A) have reduced function, although this is some- what substrate-dependent.41–44 However, the c.1584C>G poly- morphism found in CYP2D6*2A increases protein production, possibly through increased induction, which compensates for the ...
The bioactivation of tamoxifen involves several CYP450 drug metabolizing enzymes (DMEs) including, CYP2D6, CYP3A4, CYP3A5, CYP2C9, and CYP2C19, with key roles for CYP2D6 and CYP3A [5]. The wide interindividual variability in the concentration of tamoxifen and its metabolites was mainly ...
Genetic polymorphisms of cytochrome P450 enzymes: CYP2C9, CYP2C19, CYP2D6, CYP3A4, and CYP3A5 in the Croatian population. Drug Metab. Pers. Ther. 2017, 32, 11–21. [Google Scholar] [CrossRef] [PubMed] Gaedigk, A.; Sangkuhl, K.; Whirl-Carrillo, M.; Klein, T.; Leeder, J.S....
Along with CYP3A4, the most im- portant enzyme involved in the metabolism of over 50% of all drugs, CYP2D6 is vital as well for the metabolism of clinically used drugs [3]. Although it accounts only for 2–5% of the total hepatic P450 isoenzymes, it also ac- counts for 25% of ...
Within each "*" allele designation, additional variations linked in cis with the defining single-nucleotide polymorphism create N O N O CYP2D6 (CYP2B6, CYP2C9, Tamoxifen (TAM) CYP2C19, CYP3A) OH 4-hydroxyTAM SULT1A1 CYP3A4/5 (CYP2C9 + other CYP isoforms) N OH CYP2D6 CYP3A4/5 N ...
人CYP2C19和CYP2D6新变异体的体外酶活研究及CYP2C19等位基因分型
体外实验主要分别以咖啡因、咪哒唑仑、甲苯磺丁脲、氯唑沙宗、美托洛尔、美芬妥因为探针药,利用¨1)Lc方法测定探针药与相应代谢产物的浓度,研究葛根素在人肝微粒体孵化体系中对CYPlA2、CYP3A4、CYP2C9、CYP2El、CYP2D6、CYP2C19酶活性的影响。体内实验主要分别以咖啡因和美托洛尔为探针药研究临床剂量的葛根素...
Potential implications for CYP2D6 phenotyping studies and the clinical use of CYP2D6 substrate drugs in some African populations. Biochem Pharmacol 2002; 64: 1387–1398. Article CAS Google Scholar Yu A, Kneller DM, Rettie AE, Haining RL . Expression, purification, biochemical characterization, and...