Advances in the structural understanding of opioid allostery.

Authors :: Ramos-Gonzalez N
Varga BR
Majumdar S
Source :: Trends in pharmacological sciences [Trends Pharmacol Sci] 2025 Jan 17. Date of Electronic Publication: 2025 Jan 17.
Publication Year :: 2025
Publisher :: Ahead of Print
Abstract: Activation of the μ opioid receptor (MOR) can give analgesia, but also has dangerous side effects. Drugs that target MOR through an allosteric site, meaning they bind outside of the usual pocket, present a novel mode of receptor activation with different pharmacology relative to orthosteric drugs. Recent structural studies give valuable new information on how allosteric modulators interact with MOR.<br />Competing Interests: Declaration of interests S.M. is a cofounder of Sparian biosciences and has provisional patents filed on negative allosteric modulators of the mu opioid receptor. No interests are declared by N.R-G. and B.R.V.<br /> (Copyright © 2024 The Author(s). Published by Elsevier Ltd.. All rights reserved.)