Regulation of GPCR Trafficking by Ubiquitin.
Regulation of GPCR Trafficking by Ubiquitin.
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DOI：
10.1016/bs.pmbts.2015.02.005
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发表时间：
2015
影响因子：
--
通讯作者：
Marchese A
中科院分区：
文献类型：
--
作者：
Kennedy JE;Marchese A
G蛋白偶联受体（GPCR）促进的信号转导介导细胞对各种刺激的反应，参与各种生理过程。此外，GPCR也是用于治疗各种疾病的许多药物的最大一类靶标。尽管GPCR信号在健康和疾病中发挥着重要作用，但人们对GPCR信号的分子机制仍然知之甚少。经典地，GPCR信号传导受GPCR激酶和β-抑制蛋白的严格调节，其以协调一致的方式起作用以控制GPCR脱敏以及GPCR运输。泛素化现在已经成为一种重要的翻译后修饰，在控制GPCR贩运方面具有直接或间接的多种作用。最近的研究揭示了GPCR磷酸化、β-抑制蛋白和泛素化之间的机制联系。在这里，我们回顾了最近的发展，我们的理解如何泛素调节GPCR内吞途径的贩运。
G protein-coupled receptor (GPCR)-promoted signaling mediates cellular responses to a variety of stimuli involved in diverse physiological processes. In addition, GPCRs are also the largest class of target for many drugs used to treat a variety of diseases. Despite the role of GPCR signaling in health and disease, the molecular mechanisms governing GPCR signaling remain poorly understanding. Classically, GPCR signaling is tightly regulated by GPCR kinases and β-arrestins, which act in a concerted fashion to govern GPCR desensitization and also GPCR trafficking. Ubiquitination has now emerged as an important posttranslational modification that has multiple roles, either directly or indirectly, in governing GPCR trafficking. Recent studies have revealed a mechanistic link between GPCR phosphorylation, β-arrestins, and ubiquitination. Here, we review recent developments in our understanding of how ubiquitin regulates GPCR trafficking within the endocytic pathway.