p63RhoGEF: a new switch for G(q)-mediated activation of smooth muscle.

p63RhoGEF: a new switch for G(q)-mediated activation of smooth muscle.
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DOI:
10.1016/j.tcm.2012.07.007
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发表时间:
2012-07
影响因子:
9.3
通讯作者:
Somlyo, Avril V.
Somlyo, Avril V.
中科院分区:
医学2区
文献类型:
--
作者:
Momotani, Ko;Somlyo, Avril V.

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在正常和患病的血管平滑肌(SM)中,RhoA通路在调节基础张力和外周阻力中起着中心作用,该通路通过G蛋白偶联受体(GPCR)被多种激动剂激活。SM中表达多种RhoA GTP交换因子(GEF),这增加了与特定GPCR偶联的特定激动剂可能与不同的RhoGEF偶联并提供新的治疗靶点的可能性。本文就近年来在SM中发现的p63 RhoGEF(Arhgef 25; GEFT)的功能和激活机制,以及通过Gαq/11偶联的激动剂在选择性靶向RhoA介导的基础血压调节中的作用进行综述。
In normal and diseased vascular smooth muscle (SM), the RhoA pathway, which is activated by multiple agonists through G protein-coupled receptors (GPCRs), plays a central role in regulating basal tone and peripheral resistance. Multiple RhoA GTP exchange factors (GEFs) are expressed in SM raising the possibility that specific agonists coupled to specific GPCRs may couple to distinct RhoGEFs and provide novel therapeutic targets. This review will focus on the function and mechanisms of activation of p63RhoGEF (Arhgef 25; GEFT) recently identified in SM and its possible role in selective targeting of RhoA-mediated regulation of basal blood pressure through agonists that couple through Gαq/11.
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