title: Probing G protein-coupled receptor-ligand interactions with targeted photoactivatable cross-linkers.
abstract: It has been 50 years since F. H. Westheimer and colleagues reported the first use of a photoactivatable cross-linking reagent to study the active site of chymotrypsin. In studies of seven transmembrane helical receptors, also known as G protein-coupled receptors (GPCRs), recent simultaneous advances in structural biology, molecular dynamics simulations, and amber codon suppression methods have allowed the development of a targeted photo-cross-linking strategy to probe receptor-ligand interactions in cell membranes. We review here recent advances in targeted photo-cross-linking of GPCR-ligand complexes in the context of extensive earlier work that primarily relied upon the use of ligand analogues with photoactivatable constituents.
authors.affiliation: Laboratory of Chemical Biology and Signal Transduction, The Rockefeller University , 1230 York Avenue, New York , New York 10065, United States.
authors.forename: Amy
authors.initials: A
authors.lastname: Grunbeck
authors.forename: Thomas P
authors.initials: TP
authors.lastname: Sakmar
mesh_terms: D001665:Binding Sites / Q000187:drug effects / Q000528:radiation effects; D003432:Cross-Linking Reagents / Q000737:chemistry*; D006801:Humans; D008024:Ligands; D019920:Photoaffinity Labels / Q000737:chemistry*; D055668:Photochemical Processes; D011485:Protein Binding / Q000187:drug effects / Q000528:radiation effects; D025941:Protein Interaction Mapping / Q000379:methods*; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D003432:Cross-Linking Reagents; D008024:Ligands; D019920:Photoaffinity Labels; D043562:Receptors, G-Protein-Coupled