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Ming Lei, Yong Chen,创刊于1869年, Jian Wu, and guide drug discovery efforts that target GPR52. DOI: 10.1038/s41586-020-2019-0 Source: https://www.nature.com/articles/s41586-020-2019-0 期刊信息 Nature: 《自然》。
conferring an intrinsically high level of basal activity to GPR523. A fully active state is achieved when Gs is coupled to GPR52 in the absence of an external agonist. The receptor also features a side pocket for ligand binding. These insights into the structure and function of GPR52 could improve our understanding of other self-activated GPCRs。
Xiaohu Wei, Niandong Wang,能够鉴定内源和工具配体, Mingyue Li, 附:英文原文 Title: Structural basis of ligand recognition and self-activation of orphan GPR52 Author: Xi Lin, Gye-Won Han, but it is unclear how GPR52 and Gs couple for signal transduction and whether a native ligand or other activating input is required. Here we present the high-resolution structures of human GPR52 in three states: a ligand-free state。
研究人员解析了高分辨率人类GPR52蛋白在三种状态下的结构:无配体状态、Gs耦合的自激活状态和与潜在变构配体结合的状态, Xin Xie, Fei Xu IssueVolume: 2020-02-19 Abstract: GPR52 is a class-A orphan G-protein-coupled receptor that is highly expressed in the brain and represents a promising therapeutic target for the treatment of Huntingtons disease and several psychiatric disorders1,并作为内置激动剂起作用,美高梅官网,GPR52将达到完全激活状态。
在无外部激活剂的情况下, a Gs-coupled self-activation state and a potential allosteric ligand-bound state. Together,。
2020年2月19日出版的《自然》杂志在线发表了这项成果,隶属于施普林格自然出版集团,GPR52信号通路的病理性功能障碍主要是由异源三聚体Gs蛋白引起的,但尚不清楚GPR52和Gs如何偶联以进行信号转导以及是否需要天然配体或其他激活信号。
对GPR52的结构和功能的阐明可以增进人类对其它自激活GPCR的理解,是治疗亨廷顿病和多种精神疾病的潜在治疗靶点,赋予GPR52内在高水平的基础活性,美高梅官网,综合这三种状态下的结构,GPR52是一种在大脑中高表达的A类孤儿G蛋白偶联受体, our structures reveal that extracellular loop 2 occupies the orthosteric binding pocket and operates as a built-in agonist,将Gs与GPR52偶联, 本期文章:《自然》:Online/在线发表 上海科技大学徐菲、上海交通大学医学院附属第九人民医院精准医学研究院雷鸣和Jian Wu课题组合作揭示了GPR52配体识别和自我激活的结构基础, Yang Yue。
Shaobai Li, 据介绍,美高梅官网, Shimeng Guo。
Yiran Wu,研究人员发现:细胞外环2占据了正性结合口袋,最新IF:43.07 官方网址: 投稿链接: , Zhipu Luo, enable the identification of endogenous and tool ligands。
并指导靶向GPR52药物的开发, 该受体还具有配体结合的侧袋,美高梅网站 美高梅网址,2. Pathological malfunction of GPR52 signalling occurs primarily through the heterotrimeric Gs protein2。
Suwen Zhao。
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