[人细胞色素P450 2J2及其配体研究进展]。

药学学报 Pub Date : 2017-01-01
Hong-ying Ma, Jing Ning, Guang-bo Ge, Ling Yang, Da-cheng Hao
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引用次数: 0

摘要

细胞色素P4502J2 (CYP2J2)广泛分布于人体各种组织中,参与内源性化合物和药物的代谢。CYP2J2可将花生四烯酸(AA)转化为暴露型二十碳三烯酸(EETs), EETs具有多种生物学效应,提示CYP2J2在调节心血管系统、促进肿瘤进展转移等方面具有重要作用。此外,CYP2J2在多种药物的肠道代谢中起着不可缺少的作用,如阿司咪唑、特非那定、依巴斯汀等。本文结合国内外最新文献,对CYP2J2的代谢功能、催化特性及组织分布进行综述。强调了CYP2J2表征的最新方法和底物发现的当前趋势以及它与疾病的关系。本文就CYP2J2的功能及其在疾病进展中的作用作一综述。这些配体(底物和抑制剂)的信息将为CYP2J2新药的开发提供理论指导和参考。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
[Research progress of human cytochrome P450 2J2 and its ligands].

Cytochrome P4502J2 (CYP2J2) is widely distributed in various human tissues and takes a part in the metabolism of endogenous compounds and drugs. CYP2J2 can convert arachidonic acid (AA) to expoxyeicosatrienoic acids (EETs), which have various biological effects, implying the important role of CYP2J2 in the regulation of cardiovascular system and promotion of tumor progression and metastasis. Additionally, CYP2J2 plays an indispensable role in the intestinal metabolism of various drugs, such as astemizole, terfenadine and ebastine. In this review, the metabolic function, characteristic of catalysis and tissue distribution of CYP2J2 are discussed with the latest literatures both in China and abroad. The state-of-the-art methods for characterization of CYP2J2 and current trend of substrate discovery as well as its relationship with disease are highlighted. This review gives in-depth understanding of the function of CYP2J2 and its role in disease advance. The information of ligand (substrate and inhibitor) will provide the theoretical guidance and reference to the development of novel drugs for CYP2J2.

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来源期刊
药学学报
药学学报 Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.20
自引率
0.00%
发文量
0
期刊介绍: Acta Pharmaceutica Sinica B (APSB) is a bimonthly English peer-reviewed online journal in ScienceDirect, which publishes significant original research articles, communications and high quality reviews of recent advances. APSB encourages submissions from all areas of pharmaceutical sciences, including pharmacology, pharmaceutics, medicinal chemistry, natural products, pharmacognosy, pharmaceutical analysis and pharmacokinetics. APSB is a part of the series Acta Pharmaceutica Sinica, which was founded in 1953. The journal is co-published by Elsevier B.V., in association with the Institute of MateriaMedica, Chinese Academy of Medical Sciences and Chinese Pharmaceutical Association.
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