Mass spectrometry-based GPCR proteomics: comprehensive characterization of the human cannabinoid 1 receptor.

ABSTRACT: The human cannabinoid 1 receptor (hCB1), a ubiquitous G protein-coupled receptor (GPCR), transmits cannabinergic signals that participate in diverse (patho)physiological processes. Pharmacotherapeutic hCB1 targeting is considered a tractable approach for treating such prevalent diseases as obesity, mood disorders, and drug addiction. The hydrophobic nature of the transmembrane helices of hCB1 presents a formidable difficulty to its direct structural analysis. Comprehensive experimental characterization of functional hCB1 by mass spectrometry (MS) is essential to the targeting of affinity probes that can be used to define directly hCB1 binding domains using a ligand-assisted experimental approach. Such information would greatly facilitate the rational design of hCB1-selective agonists/antag

SUBMITTER: Zvonok N 

PROVIDER: S-EPMC3697753 | biostudies-literature | 2010 Apr

REPOSITORIES: biostudies-literature