3UA8

Crystal Structure Analysis of a 6-Amino Quinazolinedione Sulfonamide bound to human GluR2

Summary for 3UA8

• Entry DOI: 10.2210/pdb3ua8/pdb
• Related: 3R7X
• Descriptor: Glutamate receptor 2, N-methyl-1-{3-[(methylsulfonyl)amino]-2,4-dioxo-7-(trifluoromethyl)-1,2,3,4-tetrahydroquinazolin-6-yl}-1H-imidazole-4-carboxamide (3 entities in total)
• Functional Keywords: ion channel, ionic channel, postsynaptic membrane, transmembrane, transport protein-antagonist complex, transport protein/antagonist
• Biological source: Homo sapiens (human); More
• Cellular location: Cell membrane ; Multi-pass membrane protein : P42262
• Total number of polymer chains: 1
• Total formula weight: 29794.23

Authors

Kallen, J. (deposition date: 2011-10-21, release date: 2012-01-11, Last modification date: 2024-11-20)

Primary citation

Orain, D.,Ofner, S.,Koller, M.,Carcache, D.A.,Froestl, W.,Allgeier, H.,Rasetti, V.,Nozulak, J.,Mattes, H.,Soldermann, N.,Floersheim, P.,Desrayaud, S.,Kallen, J.,Lingenhoehl, K.,Urwyler, S.
6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
Bioorg.Med.Chem.Lett., 22:996-999, 2012

PubMed Abstract: A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage.

PubMed: 22197388
DOI: 10.1016/j.bmcl.2011.12.009

Experimental method

X-RAY DIFFRACTION (1.9 Å)