创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

可溶性鸟苷酸环化酶激动剂与激活剂的研究进展

Research Progress of Soluble Guanylate Cyclase Stimulators and Activators

  • 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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