Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

Controlling receptor functional selectivity profiles for opioid receptors is a promising approach for discovering safer analgesics; however, the structural determinants conferring functional selectivity are not well understood. Here, we used crystal structures of opioid receptors, including the rece...

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Bibliographic Details
Main Authors: Rajendra Uprety, Tao Che, Saheem A Zaidi, Steven G Grinnell, Balázs R Varga, Abdelfattah Faouzi, Samuel T Slocum, Abdullah Allaoa, András Varadi, Melissa Nelson, Sarah M Bernhard, Elizaveta Kulko, Valerie Le Rouzic, Shainnel O Eans, Chloe A Simons, Amanda Hunkele, Joan Subrath, Ying Xian Pan, Jonathan A Javitch, Jay P McLaughlin, Bryan L Roth, Gavril W Pasternak, Vsevolod Katritch, Susruta Majumdar
Format: Article
Language:English
Published: eLife Sciences Publications Ltd 2021-02-01
Series:eLife
Subjects:
safer opioids
GPCR bias
structure-based drug design
functional selectivity
boat/chair
Online Access:https://elifesciences.org/articles/56519

Internet

https://elifesciences.org/articles/56519

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