孕烷X受体
雄激素受体
生物
CYP3A型
背景(考古学)
糖皮质激素受体
基因表达调控
基因表达
计算生物学
基因
遗传学
核受体
亚科
细胞色素P450
CYP3A4型
受体
细胞生物学
转录因子
生物化学
酶
古生物学
作者
G. Gordon Gibson,Nick Plant,KE Swales,Andrew D. Ayrton,Wafaa El-Sankary
出处
期刊:Xenobiotica
[Informa]
日期:2002-01-01
卷期号:32 (3): 165-206
被引量:202
标识
DOI:10.1080/00498250110102674
摘要
1. The importance of CYP3A enzymes in drug metabolism and toxicology has yielded a wealth of information on the structure, function and regulation of this subfamily and recent research emphasis has been placed on the human forms, namely CYP3A4, CYP3A5, CYP3A7 and CYP3A43. 2. The current review will focus on the receptor-dependency of CYP3A regulation and includes consideration of the regulatory roles of the glucocorticoid (GR), pregnane X (PXR) and constitutive androstane (CAR) receptors. 3. Emphasis has been placed on the topics of expression and substrate specificity, assessment of induction, species differences in induction, CYP3A promoter sequences and regulation of gene expression, structural and functional aspects of receptor-mediated, CYP3A gene activation, receptor variants and interindividual variation in human CYP3A expression, the latter encompassing environmental, physiological and genetic aspects. 4. An outline of future research needs will be discussed in the context of receptor-mediated molecular mechanisms of CYP3A gene regulation and the impact on interindividual variations in CYP3A expression. 5. Taken collectively, this review highlights the importance of understanding the molecular mechanisms of CYP3A induction as a means of rationalizing human responses to many clinically used drugs, in addition to providing a mechanistically coherent platform to understand and predict interindividual variations in response and drug-drug interactions.
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