摘要
可溶性鸟苷酸环化酶(soluble guanylate cyclase,sGC)是一种胞质异二聚体蛋白,由α和β亚基组成,并带有血红素-一氧化氮和氧结合域.一氧化氮(dnitrogen monoxide,NO)通过与血红素基团的Fe2+结合来刺激sGC活性,使环鸟苷酸(cyclic guanosine monophosphate,cGMP)水平上升.sGC可以以2种不同的形式存在,即作为内源性NO受体的天然含血红素形式和不能结合NO的无血红素形式.采用sGC激动剂或激活剂刺激sGC,是一种治疗心血管、心脏和肾脏疾病的一种有效策略.通过对sGC激动剂与激活剂的研究进展进行综述,旨在为sGC调控机制的深入研究以及sGC激动剂与激活剂的开发提供参考.
Abstract
Soluble guanylate cyclase(sGC)is a cytosolic heterodimeric protein consisting of α and β subunits with heme groups located in the β subunit(heme binding domain,H-NOX domain).NO stimulates sGC activity by binding to Fe2+of the heme group,causing cGMP levels to rise.sGC can exist in two different forms,the natural heme-containing form as an endogenous NO receptor and the heme-free form that cannot bind NO.Stimulation of sGC with sGC stimulators or activators is a promising treatment strategy for cardiovascular and cardiac and renal diseases.This article briefly reviews the research progress of sGC stimulators and activators,aiming to provide some reference for the in-depth study of the regulatory mechanism of sGC and the development of sGC stimulators and activators.
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