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Dawn of a New RAMPage.
Trends in Pharmacological Sciences ( IF 13.9 ) Pub Date : 2020-02-27 , DOI: 10.1016/j.tips.2020.01.009
D Stephen Serafin 1 , Natalie R Harris 1 , Natalie R Nielsen 1 , Duncan I Mackie 1 , Kathleen M Caron 1
Affiliation  

Receptor activity-modifying proteins (RAMPs) interact with G-protein-coupled receptors (GPCRs) to modify their functions, imparting significant implications upon their physiological and therapeutic potentials. Resurging interest in identifying RAMP-GPCR interactions has recently been fueled by coevolution studies and orthogonal technological screening platforms. These new studies reveal previously unrecognized RAMP-interacting GPCRs, many of which expand beyond Class B GPCRs. The consequences of these interactions on GPCR function and physiology lays the foundation for new molecular therapeutic targets, as evidenced by the recent success of erenumab. Here, we highlight recent papers that uncovered novel RAMP-GPCR interactions, human RAMP-GPCR disease-causing mutations, and RAMP-related human pathologies, paving the way for a new era of RAMP-targeted drug development.

中文翻译:


新 RAMPage 的黎明。



受体活性修饰蛋白 (RAMP) 与 G 蛋白偶联受体 (GPCR) 相互作用以改变其功能,对其生理和治疗潜力产生重大影响。最近,协同进化研究和正交技术筛选平台激发了人们对识别 RAMP-GPCR 相互作用的兴趣。这些新研究揭示了以前未被识别的 RAMP 相互作用 GPCR,其中许多超出了 B 类 GPCR 的范围。这些相互作用对 GPCR 功能和生理学的影响为新的分子治疗靶点奠定了基础,erenumab 最近的成功证明了这一点。在这里,我们重点介绍最近的论文,这些论文揭示了新的 RAMP-GPCR 相互作用、人类 RAMP-GPCR 致病突变以及 RAMP 相关的人类病理学,为 RAMP 靶向药物开发的新时代铺平了道路。
更新日期:2020-02-27
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