title: 6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.
abstract: AMPA receptors mediate fast excitatory synaptic transmission and are essential for synaptic plasticity. ANQX, a photoreactive AMPA receptor antagonist, is an important biological probe used to irreversibly inactivate AMPA receptors. Here, using X-ray crystallography and mass spectroscopy, we report that ANQX forms two major products in the presence of the GluR2 AMPAR ligand-binding core (S1S2J). Upon photostimulation, ANQX reacts intramolecularly to form FQX or intermolecularly to form a covalent adduct with Glu705.
authors.affiliation: Graduate Program in Chemistry and Chemical Biology, University of California San Francisco, San Francisco, California 94158-2517, USA.
authors.forename: Leslie A
authors.initials: LA
authors.lastname: Cruz
authors.forename: Eva
authors.initials: E
authors.lastname: Estébanez-Perpiñá
authors.forename: Sam
authors.initials: S
authors.lastname: Pfaff
authors.forename: Sabine
authors.initials: S
authors.lastname: Borngraeber
authors.forename: Ning
authors.initials: N
authors.lastname: Bao
authors.forename: Justin
authors.initials: J
authors.lastname: Blethrow
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Fletterick
authors.forename: Pamela M
authors.initials: PM
authors.lastname: England