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CYP2D6 pharmacogenomics

机译:CYP2D6药物基因组学

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Cytochromes are proteins that catalyze electron transfer reactions of many metabolic pathways. They are involved in drug metabolism and thus determines the therapeutic safety and efficacy of drugs in patients. Cytochrome P450 in mitochondria accounts for 90% of the oxidative metabolism of clinically used drugs during phase 1 reaction. CYP2D6 is a major gene member of this superfamily as it carries out metabolism of 25% of drugs currently available in the market. Contrary to the concept of specificity of enzyme action these can metabolize substrates of different chemistry. Since its discovery, many have intensively studied this unique hemoprotein and contributed to the elucidation of its molecular properties and physiological functions and also the structure-activity relationships of its substrates and inhibitors. Its activity ranges considerably within a population due to genetic polymorphisms which lead to varied responses to drug intake. Studying such polymorphisms which cause a significant impact in the management of patients and helps to achieve the final target of personalizing medicine. This review briefs about history, structure, and function, molecular genetics, substrates, regulators and inhibitors of CYP2D6 and its clinical pharmacogenomics.
机译:细胞色素是催化许多代谢途径的电子转移反应的蛋白质。它们参与药物代谢,因此决定了药物在患者中的治疗安全性和功效。线粒体中的细胞色素P450占1期反应期间临床使用药物氧化代谢的90%。 CYP2D6是该超家族的主要基因成员,因为它能进行市场上现有药物的25%的代谢。与酶作用特异性的概念相反,这些酶可以代谢不同化学性质的底物。自发现以来,许多人都对这种独特的血红蛋白进行了深入研究,并有助于阐明其分子特性和生理功能,以及其底物和抑制剂的构效关系。由于遗传多态性,其活性在人群中的范围相当大,这导致对药物摄入的不同反应。研究此类多态性会对患者的治疗产生重大影响,并有助于实现个性化药物的最终目标。该综述简要介绍了CYP2D6的历史,结构和功能,分子遗传学,底物,调节剂和抑制剂及其临床药物基因组学。

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