可溶性环氧化物水解酶

Pooja M. Sontakke, Suraj G. Malpani, Pooja R. Tange, MD Rayees Ahmad, Vishweshwar M. Dharashive
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引用次数: 0

摘要

环二十碳三烯酸(EETs)对心血管有诸多益处,包括扩张血管、抗炎作用以及对血管平滑肌细胞的抗迁移作用。然而,将 EET 分解成二元醇的酶 sEH 限制了这些益处。sEH 抑制剂(sEHIs)的开发,尤其是基于 1,3-二取代脲的抑制剂的开发,已显示出增强 EETs 治疗特性的前景。这些抑制剂具有降压和抗炎作用,可保护心脏、大脑和肾脏免受损伤。虽然仍有一些挑战需要克服,如改进 sEHIs 的类药物特性和找到针对特定组织的更好方法,但 sEHIs 临床试验的启动凸显了它们作为治疗剂的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Soluble Epoxide Hydrolase
Epoxyeicosatrienoic acids (EETs) have numerous cardiovascular benefits, including vasodilation, anti-inflammatory actions, and anti-migratory effects on vascular smooth muscle cells. However, sEH, an enzyme that breaks down EETs into diols, limits these benefits. The development of sEH inhibitors (sEHIs), particularly those based on 1,3-disubstituted urea, has shown promise in enhancing the therapeutic properties of EETs. These inhibitors are antihypertensive and anti-inflammatory and can protect the heart, brain, and kidneys from damage. While there are still challenges to overcome, such as improving the drug-like properties of sEHIs and finding better ways to target specific tissues, the initiation of clinical trials for sEHIs highlights their potential as therapeutic agents.  
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