环磷酸鸟苷
磷酸二酯酶
鸟苷酸
效应器
一氧化氮
PDE10A型
磷酸二酯酶3
cGMP依赖性蛋白激酶
鸟苷
化学
激酶
鸟苷酸环化酶
药理学
蛋白激酶A
内科学
生物
医学
生物化学
酶
核苷酸
基因
细胞周期蛋白依赖激酶2
作者
Chien-Nien Chen,Geoffrey Watson,Lan Zhao
标识
DOI:10.1016/j.vph.2012.09.001
摘要
During the last decade, it emerged that cyclic guanosine monophosphate (cGMP) is a novel drug target for the treatment of pulmonary arterial hypertension (PAH). cGMP regulates many cellular functions, ranging from contractility to growth, of relevance to the disease. Generated from guanylyl cyclases in response to natriuretic peptides or nitric oxide (NO), cGMP transduces its effects through a number of cGMP effectors, including cGMP-regulated phosphodiesterases and protein kinases. Furthermore, the cGMP concentration is modulated by cGMP-degrading phosphodiesterases. Data to date demonstrate that increasing intracellular cGMP through stimulation of GCs, inhibition of PDEs, or both is a valid therapeutic strategy in drug development for PAH. New advances in understanding of cGMP are unravelled, as well as the pathobiology of PAH. cGMP remains an attractive future PAH drug target. This review makes a more detailed examination of cGMP signalling with particular reference to PAH.
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