细胞色素P450的结构，功能和临床意义：综述。,Current Drug Targets

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细胞色素P450的结构，功能和临床意义：综述。
Current Drug Targets ( IF 3.0 ) Pub Date : 2017-01-27 , DOI: 10.2174/1389450118666170125144557
Palrasu Manikandan ₁ , Siddavaram Nagini ₂

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背景技术细胞色素P450（CYP）酶是与膜结合的血蛋白，在异生物素的解毒，细胞代谢和体内平衡中起关键作用。CYP酶的诱导或抑制是药物相互作用的主要机制。CYP酶可以通过各种依赖受体的机制被各种异种生物和内源性底物转录激活。CYP酶抑制是基于代谢的药物-药物相互作用的主要机制。由于其抑制或诱导CYP酶系统的能力，许多化疗药物可引起药物相互作用。基于计算机分析和验证的预测已经确定了几种调节CYP的microRNA。CYP基因的遗传多态性和表观遗传变化可能是造成个体间和种族间疾病易感性和药物治疗效果的差异的原因。目的本综述是对细胞色素P450的结构，功能，药物遗传学，药物表观遗传学和临床意义的全面综述。结论有关CYP亚型的底物，诱导物和抑制剂以及CYP酶多态性的知识可被临床医生用于确定治疗策略以及被CYP基因产物代谢的药物的治疗剂量。药物表观遗传学和临床意义。结论有关CYP亚型的底物，诱导物和抑制剂以及CYP酶多态性的知识可被临床医生用于确定治疗策略以及被CYP基因产物代谢的药物的治疗剂量。药物表观遗传学和临床意义。结论有关CYP亚型的底物，诱导物和抑制剂以及CYP酶多态性的知识可被临床医生用于确定治疗策略以及被CYP基因产物代谢的药物的治疗剂量。

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Cytochrome P450 Structure, Function and Clinical Significance: A Review.

BACKGROUND The cytochrome P450 (CYP) enzymes are membrane-bound hemoproteins that play a pivotal role in the detoxification of xenobiotics, cellular metabolism and homeostasis. Induction or inhibition of CYP enzymes is a major mechanism that underlies drug-drug interactions. CYP enzymes can be transcriptionally activated by various xenobiotics and endogenous substrates through receptor-dependent mechanisms. CYP enzyme inhibition is a principal mechanism for metabolism- based drug-drug interactions. Many chemotherapeutic drugs can cause drug interactions due to their ability to either inhibit or induce the CYP enzyme system. Predictions based on in silico analyses followed by validation have identified several microRNAs that regulate CYPs. Genetic polymorphisms and epigenetic changes in CYP genes may be responsible for inter-individual and interethnic variations in disease susceptibility and the therapeutic efficacy of drugs. OBJECTIVE The present review is a comprehensive compilation of cytochrome P450 structure, function, pharmacogenetics, pharmacoepigenetics and clinical significance. CONCLUSION Knowledge about the substrates, inducers, and inhibitors of CYP isoforms, as well as the polymorphisms of CYP enzymes may be used as an aid by clinicians to determine therapeutic strategy, and treatment doses for drugs that are metabolized by CYP gene products.

更新日期：2019-11-01

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