Discovery and development of macrocyclic peptide modulators of the cannabinoid 2 receptor.

ABSTRACT: The cannabinoid type 2 receptor (CB₂R), a G protein-coupled receptor, is an important regulator of immune cell function and a promising target to treat chronic inflammation and fibrosis. While CB₂R is typically targeted by small molecules, including endo-, phyto-, and synthetic cannabinoids, peptides-owing to their size-may offer a different interaction space to facilitate differential interactions with the receptor. Here, we explore plant-derived cyclic cystine-knot peptides as ligands of the CB₂R. Cyclotides are known for their exceptional biochemical stability. Recently, they gained attention as G protein-coupled receptor modulators and as templates for designing peptide ligands with improved pharmacokinetic properties over linear peptides. Cyclotide-bas

SUBMITTER: Tomasevic N 

PROVIDER: S-EPMC11154713 | biostudies-literature | 2024 Jun

REPOSITORIES: biostudies-literature