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Structure paper

タイトル	Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes.
ジャーナル・号・ページ	Science, Vol. 364, Issue 6440, Page 552-557, Year 2019
掲載日	2019年5月10日
著者	Shoji Maeda / Qianhui Qu / Michael J Robertson / Georgios Skiniotis / Brian K Kobilka /
PubMed 要旨	Muscarinic acetylcholine receptors are G protein-coupled receptors that respond to acetylcholine and play important signaling roles in the nervous system. There are five muscarinic receptor subtypes ...Muscarinic acetylcholine receptors are G protein-coupled receptors that respond to acetylcholine and play important signaling roles in the nervous system. There are five muscarinic receptor subtypes (M1R to M5R), which, despite sharing a high degree of sequence identity in the transmembrane region, couple to different heterotrimeric GTP-binding proteins (G proteins) to transmit signals. M1R, M3R, and M5R couple to the G family, whereas M2R and M4R couple to the G family. Here, we present and compare the cryo-electron microscopy structures of M1R in complex with G and M2R in complex with G The M1R-G complex exhibits distinct features, including an extended transmembrane helix 5 and carboxyl-terminal receptor tail that interacts with G protein. Detailed analysis of these structures provides a framework for understanding the molecular determinants of G-protein coupling selectivity.
リンク	Science / PubMed:31073061 / PubMed Central
手法	EM (単粒子)
解像度	3.3 - 3.6 Å
構造データ	20078 6oij EMDB-20078, PDB-6oij: Muscarinic acetylcholine receptor 1-G11 protein complex 手法: EM (単粒子) / 解像度: 3.3 Å 20079 6oik EMDB-20079, PDB-6oik: Muscarinic acetylcholine receptor 2-Go complex 手法: EM (単粒子) / 解像度: 3.6 Å
化合物	ChemComp-IXO: 4-(4,5-dihydro-1,2-oxazol-3-yloxy)-N,N,N-trimethylbut-2-yn-1-aminium / [4-(2-イソオキサゾリン-3-イルオキシ)-2-ブチニル]トリメチルアミニウム ChemComp-Y01: CHOLESTEROL HEMISUCCINATE / コレステリルヘミスクシナ-ト ChemComp-2CU: 3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide
由来	homo sapiens (ヒト) mus musculus (ハツカネズミ)
キーワード	SIGNALING PROTEIN / G-protein coupled receptor-G-protein complex / neurotransmitter receptor