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Emerging roles for Regulator of G Protein Signaling 2 in (patho)physiology.
Molecular Pharmacology ( IF 3.6 ) Pub Date : 2020-12-01 , DOI: 10.1124/molpharm.120.000111
Harrison J McNabb 1 , Qian Zhang 1 , Benita Sjögren 2
Affiliation  

Since their discovery in the mid-1990s, regulator of G protein signaling (RGS) proteins have emerged as key regulators of signaling through G protein–coupled receptors. Among the over 20 known RGS proteins, RGS2 has received increasing interest as a potential therapeutic drug target with broad clinical implications. RGS2 is a member of the R4 subfamily of RGS proteins and is unique in that it is selective for Gαq. Despite only having an RGS domain, responsible for the canonical GTPase activating protein activity, RGS2 can regulate additional processes, such as protein synthesis and adenylate cyclase activity, through protein-protein interactions. Here we provide an update of the current knowledge of RGS2 function as it relates to molecular mechanisms of regulation as well as its potential role in regulating a number of physiologic systems and pathologies, including cardiovascular disease and central nervous system disorders, as well as various forms of cancer.

中文翻译:

G蛋白信号传导2调节剂在(病理)生理学中的新兴作用。

自1990年代中期发现以来,G蛋白信号转导(RGS)蛋白的调节剂已成为通过G蛋白偶联受体的信号转导的关键调节剂。在20多种已知的RGS蛋白中,RGS2作为具有潜在临床意义的潜在治疗药物靶标越来越受到关注。RGS2是RGS蛋白的R4亚家族的成员,并且在它是选择性对于G独特α q。尽管仅具有负责经典GTPase激活蛋白活性的RGS域,RGS2仍可以通过蛋白-蛋白相互作用来调节其他过程,例如蛋白合成和腺苷酸环化酶活性。在这里,我们提供有关RGS2功能的最新知识的最新信息,因为它涉及调控的分子机制,以及其在调控许多生理系统和病理学(包括心血管疾病和中枢神经系统疾病)以及各种形式中的潜在作用癌症。
更新日期:2020-11-12
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