Substrate-Dependent Functional Alterations of Seven CYP2C9 Variants Found in Japanese Subjects

• Published in: Drug metabolism and disposition Vol. 37; no. 9; pp. 1895 - 1903
• Main Authors: Maekawa, Keiko, Harakawa, Noriko, Sugiyama, Emiko, Tohkin, Masahiro, Kim, Su-Ryang, Kaniwa, Nahoko, Katori, Noriko, Hasegawa, Ryuichi, Yasuda, Kazuki, Kamide, Kei, Miyata, Toshiyuki, Saito, Yoshiro, Sawada, Jun-ichi
• Format: Journal Article
• Language: English
• Published: Bethesda, MD Elsevier Inc 01.09.2009; American Society for Pharmacology and Experimental Therapeutics
• Subjects: Alleles; Angiotensin II Type 1 Receptor Blockers - metabolism; Animals; Biological and medical sciences; Blotting, Western; Cytochrome P-450 Enzyme System - genetics; Cytochrome P-450 Enzyme System - metabolism; Diclofenac - metabolism; DNA, Complementary - biosynthesis; DNA, Complementary - genetics; Genetic Variation; Humans; Hypoglycemic Agents - metabolism; Insecta; Japan; Kinetics; Losartan - metabolism; Medical sciences; Microsomes - metabolism; Pharmacology. Drug treatments; Rats; Recombinant Proteins - metabolism; Substrate Specificity; Sulfonylurea Compounds - metabolism; Asia; Japan; Human; Substrate; Variant; Genetic variability; Enzyme; Isozyme; Cytochrome P450; Genotype; CYP2C9 gene

CYP2C9 is a polymorphic enzyme that metabolizes a number of clinically important drugs. In this study, catalytic activities of seven alleles found in Japanese individuals, CYP2C9*3 (I359L), *13 (L90P), *26 (T130R), *28 (Q214L), *30 (A477T), *33 (R132Q), and *34 (R335Q), were assessed using three sub...