Unraveling GPCRs Allosteric Modulation. Cannabinoid 1 Receptor as a Case Study.

ABSTRACT: G-protein-coupled receptors (GPCRs) constitute one of the most prominent families of integral membrane receptor proteins that mediate most transmembrane signaling processes. Malfunction of these signal transduction processes is one of the underlying causes of many human pathologies (Parkinson's, Huntington's, heart diseases, etc), provoking that GPCRs are the largest family of druggable proteins. However, these receptors have been targeted traditionally by orthosteric ligands, which usually causes side effects due to the simultaneous targeting of homologous receptor subtypes. Allosteric modulation offers a promising alternative approach to circumvent this problematic and, thus, comprehending its details is a most important task. Here we use the Cannabinoid type-1 receptor (CB1R) in trying

SUBMITTER: Cruz A 

PROVIDER: S-EPMC11879764 | biostudies-literature | 2025 Apr

REPOSITORIES: biostudies-literature