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-Structure paper
タイトル | Structure and dynamics of the CGRP receptor in apo and peptide-bound forms. |
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ジャーナル・号・ページ | Science, Vol. 372, Issue 6538, Year 2021 |
掲載日 | 2021年4月9日 |
著者 | Tracy M Josephs / Matthew J Belousoff / Yi-Lynn Liang / Sarah J Piper / Jianjun Cao / Daniel J Garama / Katie Leach / Karen J Gregory / Arthur Christopoulos / Debbie L Hay / Radostin Danev / Denise Wootten / Patrick M Sexton / |
PubMed 要旨 | G protein-coupled receptors (GPCRs) are key regulators of information transmission between cells and organs. Despite this, we have only a limited understanding of the behavior of GPCRs in the apo ...G protein-coupled receptors (GPCRs) are key regulators of information transmission between cells and organs. Despite this, we have only a limited understanding of the behavior of GPCRs in the apo state and the conformational changes upon agonist binding that lead to G protein recruitment and activation. We expressed and purified unmodified apo and peptide-bound calcitonin gene-related peptide (CGRP) receptors from insect cells to determine their cryo-electron microscopy (cryo-EM) structures, and we complemented these with analysis of protein conformational dynamics using hydrogen-deuterium exchange mass spectrometry and three-dimensional variance analysis of the cryo-EM data. Together with our previously published structure of the active, Gs-bound CGRP receptor complex, our work provides insight into the mechanisms of class B1 GPCR activation. |
リンク | Science / PubMed:33602864 |
手法 | EM (単粒子) |
解像度 | 3.15 - 3.49 Å |
構造データ | EMDB-22962, PDB-7knt: EMDB-22963, PDB-7knu: |
由来 |
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キーワード | SIGNALING PROTEIN / GPCR (Gタンパク質共役受容体) / CGRP receptor / apo receptor / MEMBRANE PROTEIN (膜タンパク質) |