TY - JOUR
T1 - Molecular basis for ligand modulation of the cannabinoid CB1 receptor
AU - Ramesh, Karthik
AU - Rosenbaum, Daniel M.
N1 - Funding Information:
We gratefully acknowledge the support of the Welch Foundation (I‐1770 to D.M.R.) and the Edward Mallinckrodt, Jr. Foundation (Scholar Award to D.M.R.)
Publisher Copyright:
© 2021 The British Pharmacological Society.
PY - 2022/7
Y1 - 2022/7
N2 - The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which mediates the functional response to endocannabinoids and Cannabis compounds. A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment of neurological disorders. New high-resolution structures of CB1 receptor in different functional states have significantly improved our molecular understanding of CB1 ligand interactions, selectivity, receptor activation and allosteric modulation. These advances have paved the way for development of novel ligands for different therapeutic applications. In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor. LINKED ARTICLES: This article is part of a themed issue on Structure Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.14/issuetoc.
AB - The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in the central nervous system, which mediates the functional response to endocannabinoids and Cannabis compounds. A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment of neurological disorders. New high-resolution structures of CB1 receptor in different functional states have significantly improved our molecular understanding of CB1 ligand interactions, selectivity, receptor activation and allosteric modulation. These advances have paved the way for development of novel ligands for different therapeutic applications. In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor. LINKED ARTICLES: This article is part of a themed issue on Structure Guided Pharmacology of Membrane Proteins (BJP 75th Anniversary). To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v179.14/issuetoc.
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U2 - 10.1111/bph.15627
DO - 10.1111/bph.15627
M3 - Article
C2 - 34265078
AN - SCOPUS:85112372312
SN - 0007-1188
VL - 179
SP - 3487
EP - 3495
JO - British Journal of Pharmacology
JF - British Journal of Pharmacology
IS - 14
ER -