Structural insights into G-protein- coupled receptor allostery

Thal David M.; Glukhova Alisa; Sexton Patrick M.; Christopoulos Arthur

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Structural insights into G-protein- coupled receptor allostery

机译：对G蛋白偶联受体变构的结构见解

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G-protein-coupled receptors (GPCRs) are key cell-surface proteins that transduce external environmental cues into biochemical signals across the membrane. GPCRs are intrinsically allosteric proteins; they interact via spatially distinct yet conformationally linked domains with both endogenous and exogenous proteins, nutrients, metabolites, hormones, small molecules and biological agents. Here we explore recent high-resolution structural studies, which are beginning to unravel the atomic details of allosteric transitions that govern GPCR biology, as well as highlighting how the wide diversity of druggable allosteric sites across these receptors present opportunities for developing new classes of therapeutics.

机译：G蛋白偶联受体（GPCR）是关键的细胞表面蛋白，可将外部环境线索转化为跨膜的生化信号。 GPCR是内在的变构蛋白。它们通过空间上不同但构象相连的结构域与内源性和外源性蛋白质，营养素，代谢产物，激素，小分子和生物因子相互作用。在这里，我们探索了最近的高分辨率结构研究，这些研究开始揭示支配GPCR生物学的变构转变的原子细节，并强调这些受体上可药用变构位点的广泛多样性如何为开发新型疗法提供了机会。

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来源
《Nature》 |2018年第7712期|45-53|共9页
作者
Thal David M.; Glukhova Alisa; Sexton Patrick M.; Christopoulos Arthur;
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作者单位

Monash Univ, Monash Inst Pharmaceut Sci, Drug Discovery Biol, Melbourne, Vic, Australia;

Monash Univ, Monash Inst Pharmaceut Sci, Drug Discovery Biol, Melbourne, Vic, Australia;

Monash Univ, Monash Inst Pharmaceut Sci, Drug Discovery Biol, Melbourne, Vic, Australia;

Monash Univ, Monash Inst Pharmaceut Sci, Drug Discovery Biol, Melbourne, Vic, Australia;

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收录信息美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);美国《化学文摘》(CA);
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3. Molecular cloning, tissue-specific expression, and chromosomal localization of a novel nerve growth factor-regulated G-protein- coupled receptor, nrg-1. [J] . Glickman M, Malek RL, Kwitek Black-AE, Molecular and cellular neurosciences . 1999,第2期

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Structural insights into G-protein- coupled receptor allostery

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