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Does divergent binding pocket closure drive ligand bias for class A GPCRs?

Item Type:Editorial
Title:Does divergent binding pocket closure drive ligand bias for class A GPCRs?
Creators Name:Bermudez, M. and Bock, A.
Abstract:GPCRs couple to intracellular transducer proteins, which reciprocally closes the extracellular ligand binding pocket, a process called allosteric coupling. Biased agonists preferentially stimulate receptor coupling to specific signaling pathways. Here, we postulate that agonists with extended binding modes selectively interfere with binding pocket closure, which results in divergent allosteric coupling, eventually leading to ligand bias.
Keywords:GPCR, Biased Signaling, Ligand Bias, Allosteric Coupling, Extended Binding Mode, Drug Design
Source:Trends in Pharmacological Sciences
ISSN:0165-6147
Publisher:Elsevier (U.K.)
Volume:40
Number:4
Page Range:236-239
Date:April 2019
Official Publication:https://doi.org/10.1016/j.tips.2019.02.005
PubMed:View item in PubMed

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