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Discovery of Soluble Epoxide Hydrolase Inhibitors from Chemical Synthesis and Natural Products
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-12-28 , DOI: 10.1021/acs.jmedchem.0c01507
Cheng-Peng Sun 1 , Xin-Yue Zhang 1 , Christophe Morisseau 2 , Sung Hee Hwang 2 , Zhan-Jun Zhang 3 , Bruce D Hammock 2 , Xiao-Chi Ma 1, 4
Affiliation  

Soluble epoxide hydrolase (sEH) is an α/β hydrolase fold protein and widely distributed in numerous organs including the liver, kidney, and brain. The inhibition of sEH can effectively maintain endogenous epoxyeicosatrienoic acids (EETs) levels and reduce dihydroxyeicosatrienoic acids (DHETs) levels, resulting in therapeutic potentials for cardiovascular, central nervous system, and metabolic diseases. Therefore, since the beginning of this century, the development of sEH inhibitors is a hot research topic. A variety of potent sEH inhibitors have been developed by chemical synthesis or isolated from natural sources. In this review, we mainly summarized the interconnected aspects of sEH with cardiovascular, central nervous system, and metabolic diseases and then focus on representative inhibitors, which would provide some useful guidance for the future development of potential sEH inhibitors.

中文翻译:

从化学合成和天然产物中发现可溶性环氧化物水解酶抑制剂

可溶性环氧化物水解酶 (sEH) 是一种 α/β 水解酶折叠蛋白,广泛分布于肝脏、肾脏和大脑等众多器官中。抑制 sEH 可有效维持内源性环氧二十碳三烯酸 (EETs) 水平并降低二羟基二十碳三烯酸 (DHETs) 水平,从而对心血管、中枢神经系统和代谢疾病具有治疗潜力。因此,本世纪初以来,sEH抑制剂的开发一直是研究热点。通过化学合成或从天然来源中分离出多种有效的 sEH 抑制剂。在这篇综述中,我们主要总结了 sEH 与心血管、中枢神经系统和代谢疾病的相互关联的方面,然后重点介绍了具有代表性的抑制剂,
更新日期:2021-01-14
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