Issue 5, 2022

Covalent cannabinoid receptor ligands – structural insight and selectivity challenges

Abstract

X-ray crystallography and cryogenic electronic microscopy have provided significant advancement in the knowledge of GPCR structure and have allowed the rational design of GPCR ligands. The class A GPCRs cannabinoid receptor type 1 and type 2 are implicated in many pathophysiological processes and thus rational design of drug and tool compounds is of great interest. Recent structural insight into cannabinoid receptors has already led to a greater understanding of ligand binding sites and receptor residues that likely contribute to ligand selectivity. Herein, classes of heterocyclic covalent cannabinoid receptor ligands are reviewed in light of the recent advances in structural knowledge of cannabinoid receptors, with particular discussion regarding covalent ligand selectivity and rationale design.

Graphical abstract: Covalent cannabinoid receptor ligands – structural insight and selectivity challenges

Supplementary files

Article information

Article type
Review Article
Submitted
10 Jan 2022
Accepted
31 Mar 2022
First published
04 Apr 2022

RSC Med. Chem., 2022,13, 497-510

Covalent cannabinoid receptor ligands – structural insight and selectivity challenges

I. Liddle, M. Glass, J. D. A. Tyndall and A. J. Vernall, RSC Med. Chem., 2022, 13, 497 DOI: 10.1039/D2MD00006G

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