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cyp2c19
鎖定
- 外文名
- cyp2c19
- 釋 義
- CYP2C19是CYP450酶第二亞家族中的重要成員,是人體重要的藥物代謝酶
- 類 型
- 藥物代謝酶
cyp2c19重要性
Drugs and other agents whose metabolic pathway cosegregates with the activity ofcytochrome P450 2C19invitroand/orin vivo
Proton pump inhibitors Omeprazole 5-hydroxylation;Lansoprazole 5-hydroxylation; PantoprazoleO-demethylation;RabeprazoleN-demethylation Anticonvulsants, hypnosedatives, muscle relaxants Phenytoin 3’- and 4’-hydroxylation;(S)-Mephenytoin and nirvanol 4′-hydroxylation;Methylphenytoin 4′-hydroxylation;DiazepamN-demethylation (activation);Desmethyldiazepam hydroxylation;FlunitrazepamN-demethylation; Phenobarbitalp-hydroxylation;(R)-Hexobarbital 3′-hydroxylation; (R)-Mephobarbital 4-hydroxylation;CarisoprodolN-demethylation Anti-infectives Proguanil cyclisation (activation); Chlorproguanil cyclisation (activation); Nelfinavir hydroxylation (activation) Antidepressants CitalopramN-demethylation; FluoxetineN-demethylation; SertralineN-demethylation; VenlafaxineO-demethylation (activation); ImipramineN-demethylation; ClomipramineN-demethylation; Trimipramine; AmitriptylineN-demethylation; Nortriptyline demethylation; MoclobemideC-hydroxylation Others (mainlyin vitroevidence) Thioridazine Propranolol side-chain oxidation Tolbutamide 4-hydroxylation (R)-Warfarin 8-hydroxylation Progesterone 21-hydroxylation Testosterone oxidation at 17-position Desogestrel 3α-hydroxylation (activation) Cyclophosphamide 4-hydroxylation (active) Ifosfamide 4-hydroxylation (active) MethoxychlorO-demethylation (activation) |
cyp2c19多態性
CYP2C19具有很多SNP位點,在人類細胞色素P450等位基因命名法委員會(HumanCYPAllele NomenclatureCommittee)有詳盡的總結。最常見的是CYP2C19*2和CYP2C19*3。CYP2C19*2會導致轉錄蛋白的剪切突變失活,而CYP2C19*3能構成一個終止子,破壞轉錄蛋白的活性。據統計,CYP2C19*2和CYP2C19*3兩個突變位點能解釋幾乎100%的東亞人和85%的高加索人種的相關弱代謝遺傳缺陷,而其他兩種等位基因CYP2C19*4和CYP2C19*5主要在高加索人種中分佈。大量證據證實,不同人種在CYP2C19的底物的代謝能力有很大差異;2–5%高加索人是弱代謝者,而13–23%的亞洲人是弱代謝者。這是一由於在亞洲人口中CYP2C19*2和CYP2C19*3等位基因的高頻率造成的。
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