Photoaffinity Labeling of the Human A 2A Adenosine Receptor and Cross-link Position Analysis by Mass Spectrometry

ACS Med Chem Lett. 2017 May 17;8(6):660-665. doi: 10.1021/acsmedchemlett.7b00138. eCollection 2017 Jun 8.


Photoaffinity labeling (PAL) is widely used for the identification of ligand-binding proteins and elucidation of ligand-binding sites. PAL has also been employed for the characterization of G protein-coupled receptors (GPCRs); however, a limited number of reports has successfully identified their cross-linked amino acids. This report is the first of its kind to determine the cross-link position of the human A2A adenosine receptor by PAL with the novel diazirine-based photoaffinity probe 9.

Keywords: A2A adenosine receptor; GPCR; Mass spectrometry; Photoaffinity labeling.