尿苷二磷酸葡萄糖醛酸转移酶介导的药物相互作用的研究进展

摘要/Abstract

摘要： 葡萄糖醛酸结合反应是生物体内重要的Ⅱ相代谢途径,由尿苷二磷酸葡萄糖醛酸转移酶(UGT)催化完成,是多种内源性物质和外源性化合物清除与解毒的机制。在新药研发过程中,研究UGT介导的药物代谢以及评估潜在的药物相互作用是非常重要的,吸引了很多研究人员的关注。但目前的研究偏重于由细胞色素P450酶(CYP450)介导的药物相互作用,对UGT的关注相对较少。鉴于UGT在药物代谢中的重要性,有必要对其导致的药物相互作用进行更深入的研究。本文综述了由UGT的抑制引起的药物相互作用的相关研究进展。

关键词: 葡萄糖醛酸转移酶, 抑制, 相互作用

Abstract: Glucuronidation catalyzed by UDP-glucuronosyltransferase (UGT) is often recognized as the main pathway of conjugative metabolism for a variety of endogenous substances and exogenous compounds. For the development of new drugs, the investigation of drug metabolism mediated by UGT and the evaluation of potential drug-drug interaction are essential. Drug-drug interactions have been extensively studied and attracted much attention from researchers worldwide. However, the area of drug-drug interaction mediated by UGTs has received less attention than CYPs. Therefore, it is important to enhance our understanding of the role UGTs play in metabolic drug interactions in light of the fact that many drugs and their metabolites undergo UGT-mediated conjugation reactions. This review summarizes latest studies of the drug-drug interaction mediated by UGT inhibition.

Key words: UGT, Inhibition, Interaction

中图分类号:

R969

张艳, 郝海平, 王广基. 尿苷二磷酸葡萄糖醛酸转移酶介导的药物相互作用的研究进展[J]. 中国临床药理学与治疗学, 2011, 16(4): 447-454.

ZHANG Yan, HAO Hai-ping, WANG Guang-ji. Drug-drug interaction mediated by UGT[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2011, 16(4): 447-454.

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