6-Azido-7-nitro-1,4-dihydroquinoxaline-2,3-dione (ANQX) forms an irreversible bond to the active site of the GluR2 AMPA receptor.
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.
Cruz
Leslie A
LA
Graduate Program in Chemistry and Chemical Biology, University of California San Francisco, San Francisco, California 94158-2517, USA.
Estébanez-Perpiñá
Eva
E
Pfaff
Sam
S
Borngraeber
Sabine
S
Bao
Ning
N
Blethrow
Justin
J
Fletterick
Robert J
RJ
England
Pamela M
PM