title: A photoswitchable neurotransmitter analogue bound to its receptor.
abstract: Incorporation of the azobenzene derivative gluazo, a synthetic photochromic ligand, into a kainate receptor allows for the optical control of neuronal activity. The crystal structure of gluazo bound to a dimeric GluK2 ligand-binding domain reveals one monomer in a closed conformation, occupied by gluazo, and the other in an open conformation, with a bound buffer molecule. The glutamate group of gluazo interacts like the natural glutamate ligand, while its trans-azobenzene moiety protrudes into a tunnel. This elongated cavity presumably cannot accommodate a cis-azobenzene, which explains the reversible activation of the receptor upon photoisomerization.
authors.affiliation: Munich Center for Integrated Protein Science (CIPS-M).
authors.forename: Alwin
authors.initials: A
authors.lastname: Reiter
authors.forename: Arne
authors.initials: A
authors.lastname: Skerra
authors.forename: Dirk
authors.initials: D
authors.lastname: Trauner
authors.forename: André
authors.initials: A
authors.lastname: Schiefner
mesh_terms: D001391:Azo Compounds / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D018360:Crystallography, X-Ray; D008024:Ligands; D008958:Models, Molecular; D015394:Molecular Structure; D018377:Neurotransmitter Agents / Q000737:chemistry* / Q000378:metabolism* / Q000494:pharmacology; D055668:Photochemical Processes; D018092:Kainic Acid Receptors / Q000819:agonists / Q000737:chemistry* / Q000378:metabolism*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001391:Azo Compounds; D008024:Ligands; D018377:Neurotransmitter Agents; D018092:Kainic Acid Receptors; C009850:azobenzene