Crystal Structure of the Human Cannabinoid Receptor CB1
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- 作者：Tian Hua1 ; 2 ; Kiran Vemuri3 ; Mengchen Pu2 ; Lu Qu1 ; 2 ; Gye Won Han4 ; Yiran Wu1 ; Suwen Zhao1 ; Wenqing Shui1 ; Shanshan Li1 ; Anisha Korde3 ; Robert B. Laprairie5 ; Edward L. Stahl5 ; Jo-Hao Ho5 ; Nikolai Zvonok3 ; Han Zhou3 ; Irina Kufareva6 ; Beili Wu7 ; Qiang Zhao7 ; Michael A. Hanson8 ; Laura M. Bohn5 ; lbohn@scripps.edu" class="auth_mail" title="E-mail the corresponding author ; Alexandros Makriyannis3 ; a.makriyannis@northeastern.edu" class="auth_mail" title="E-mail the corresponding author ; Raymond C. Stevens1 ; 4 ; 9 ; stevens@shanghaitech.edu.cn" class="auth_mail" title="E-mail the corresponding author ; Zhi-Jie Liu1 ; 2 ; liuzhj@shanghaitech.edu.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：G protein-coupled receptor ; cannabinoid receptor CB1 ; crystal structure ; marijuana ; THC ; stabilizing antagonist ; cell signalling ; AM6538 ; rimonabant
- 刊名：Cell
- 出版年：2016
- 出版时间：20 October 2016
- 年：2016
- 卷：167
- 期：3
- 页码：750-762.e14
- 全文大小：6832 K
文摘
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AM6538 is presented as a stabilizing, tight binding antagonist of CB1
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Crystal structure of human CB1 in complex with AM6538 is determined
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Molecular docking predicts CB1 binding modes of THC and synthetic cannabinoids
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Resolution of the binding pocket provides path for rational CB1 drug design
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