6XSR

Crystal structure of GluA2 AMPA receptor in complex with trans-4-butylcyclohexane carboxylic acid (4-BCCA) inhibitor

Summary for 6XSR

Entry DOI	10.2210/pdb6xsr/pdb
Descriptor	Glutamate receptor 2, 2-acetamido-2-deoxy-beta-D-glucopyranose, trans-4-butylcyclohexane-1-carboxylic acid (3 entities in total)
Functional Keywords	ampa receptor, ion channels, synapse, bcca, transport protein
Biological source	Rattus norvegicus (Rat)
Total number of polymer chains	4
Total formula weight	363862.82
Authors	Yelshanskaya, M.V.,Singh, A.K.,Sobolevsky, A.I. (deposition date: 2020-07-16, release date: 2020-12-30, Last modification date: 2024-10-30)
Primary citation	Yelshanskaya, M.V.,Singh, A.K.,Narangoda, C.,Williams, R.S.B.,Kurnikova, M.G.,Sobolevsky, A.I. Structural basis of AMPA receptor inhibition by trans-4-butylcyclohexane carboxylic acid. Br.J.Pharmacol., 179:3628-3644, 2022 Cited by PubMed Abstract: AMPA receptors, which shape excitatory postsynaptic currents and are directly involved in overactivation of synaptic function during seizures, represent a well-accepted target for anti-epileptic drugs. Trans-4-butylcyclohexane carboxylic acid (4-BCCA) has emerged as a new promising anti-epileptic drug in several in vitro and in vivo seizure models, but the mechanism of its action remained unknown. The purpose of this study is to characterize structure and dynamics of 4-BCCA interaction with AMPA receptors. PubMed: 32959886 DOI: 10.1111/bph.15254 PDB entries with the same primary citation
Experimental method	X-RAY DIFFRACTION (4.25 Å)

Structure validation