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探索人类 CYP4 酶:生理作用、在疾病中的功能及抑制剂的关注焦点。

Exploring human CYP4 enzymes: Physiological roles, function in diseases and focus on inhibitors.

机构信息

Department of Medicinal Chemistry, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.

School of Life Science and Technology, China Pharmaceutical University, 639 Longmian Avenue, Nanjing 211198, China.

出版信息

Drug Discov Today. 2023 May;28(5):103560. doi: 10.1016/j.drudis.2023.103560. Epub 2023 Mar 22.

Abstract

The cytochrome P450 (CYP)4 family of enzymes are monooxygenases responsible for the ω-oxidation of endogenous fatty acids and eicosanoids and play a crucial part in regulating numerous eicosanoid signaling pathways. Recently, CYP4 gained attention as a potential therapeutic target for several human diseases, including cancer, cardiovascular diseases and inflammation. Small-molecule inhibitors of CYP4 could provide promising treatments for these diseases. The aim of the present review is to highlight the advances in the field of CYP4, discussing the physiology and pathology of the CYP4 family and compiling CYP4 inhibitors into groups based on their chemical classes to provide clues for the future discovery of drug candidates targeting CYP4.

摘要

细胞色素 P450(CYP)4 酶家族是单加氧酶,负责内源性脂肪酸和类二十烷酸的ω-氧化,在调节众多类二十烷酸信号通路中起着至关重要的作用。最近,CYP4 作为治疗包括癌症、心血管疾病和炎症在内的多种人类疾病的潜在治疗靶点引起了关注。CYP4 的小分子抑制剂可能为这些疾病提供有前途的治疗方法。本综述的目的是强调 CYP4 领域的进展,讨论 CYP4 家族的生理学和病理学,并根据其化学类别将 CYP4 抑制剂进行分组,为未来发现针对 CYP4 的药物候选物提供线索。

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