3R7X

Crystal Structure Analysis of a Quinazolinedione sulfonamide bound to human GluR2: A Novel Class of Competitive AMPA Receptor Antagonists with Oral Activity

Summary for 3R7X

• Entry DOI: 10.2210/pdb3r7x/pdb
• Related: 2CMO
• Descriptor: Glutamate receptor 2, N-[6-(1H-imidazol-1-yl)-7-nitro-2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl]methanesulfonamide, GLUTAMIC ACID, ... (4 entities in total)
• Functional Keywords: ion channel, ionic channel, postsynaptic membrane, transmembrane, transport protein
• Biological source: Homo sapiens (human); More
• Cellular location: Cell membrane ; Multi-pass membrane protein : P42262
• Total number of polymer chains: 2
• Total formula weight: 59209.17

Authors

Kallen, J. (deposition date: 2011-03-23, release date: 2011-05-18, Last modification date: 2024-11-27)

Primary citation

Koller, M.,Lingenhoehl, K.,Schmutz, M.,Vranesic, I.T.,Kallen, J.,Auberson, Y.P.,Carcache, D.A.,Mattes, H.,Ofner, S.,Orain, D.,Urwyler, S.
Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity.
Bioorg.Med.Chem.Lett., 21:3358-3361, 2011

PubMed Abstract: Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the synthesized compounds, 28, shows nanomolar receptor affinity, whereas other examples of the series display oral anticonvulsant activity in animal models.

PubMed: 21531559
DOI: 10.1016/j.bmcl.2011.04.017

Experimental method

X-RAY DIFFRACTION (2.1 Å)