Site-selective labeling and electron paramagnetic resonance studies of human cannabinoid receptor CB₂.

ABSTRACT: Integral membrane G protein-coupled receptors (GPCR) regulate multiple physiological processes by transmitting signals from extracellular milieu to intracellular proteins and are major targets of pharmaceutical drug development. Since GPCR are inherently flexible proteins, their conformational dynamics can be studied by spectroscopic techniques such as electron paramagnetic resonance (EPR) which requires selective chemical labeling of the protein. Here, we developed protocols for selective chemical labeling of the recombinant human cannabinoid receptor CB₂ by judiciously replacing naturally occurring reactive cysteine residues and introducing a new single cysteine residue in selected positions. The majority of the 47 newly generated single cysteine constructs expressed well in E

SUBMITTER: Yeliseev AA 

PROVIDER: S-EPMC8154700 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature