The E2.65A mutation disrupts dynamic binding poses of SB269652 at the dopamine D2 and D3 receptors.

The dopamine D2 and D3 receptors (D2R and D3R) are important targets for antipsychotics and for the treatment of drug abuse. SB269652, a bitopic ligand that simultaneously binds both the orthosteric binding site (OBS) and a secondary binding pocket (SBP) in both D2R and D3R, was found to be a negati...

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Bibliographic Details
Main Authors: Ravi Kumar Verma, Ara M Abramyan, Mayako Michino, R Benjamin Free, David R Sibley, Jonathan A Javitch, J Robert Lane, Lei Shi
Format: Article
Language:English
Published: Public Library of Science (PLoS) 2018-01-01
Series:PLoS Computational Biology
Online Access:http://europepmc.org/articles/PMC5786319?pdf=render