4MF3

Crystal Structure of Human GRIK1 complexed with a 6-(tetrazolyl)aryl decahydroisoquinoline antagonist

Summary for 4MF3

• Entry DOI: 10.2210/pdb4mf3/pdb
• Descriptor: Glutamate receptor ionotropic, kainate 1, (3S,4aS,6S,8aR)-6-[3-chloro-2-(1H-tetrazol-5-yl)phenoxy]decahydroisoquinoline-3-carboxylic acid (3 entities in total)
• Functional Keywords: protein-ligand complex, ligand gated ion channel, glutamate receptor, glutamate binding, none, membrane, signaling protein
• Biological source: Homo sapiens (human); More
• Cellular location: Cell membrane; Multi-pass membrane protein: P39086
• Total number of polymer chains: 2
• Total formula weight: 59973.57

Authors

Martinez-Perez, J.A.,Iyengar, S.,Shannon, H.E.,Bleakman, D.,Alt, A.,Clawson, D.K.,Arnold, B.M.,Bell, M.G.,Bleisch, T.J.,Castano, A.M.,Del Prado, M.,Dominguez, E.,Escribano, A.M.,Filla, S.A.,Ho, K.H.,Hudziak, K.J.,Jones, C.K.,Katofiasc, M.A.,Mateo, A.,Mathes, B.M.,Mattiuz, E.L.,Ogden, A.M.L.,Phebus, L.A.,Simmons, R.M.A.,Stack, D.R.,Stratford, R.E.,Winter, M.A.,Wu, Z.,Ornstein, P.L. (deposition date: 2013-08-27, release date: 2014-05-07, Last modification date: 2017-11-15)

• Primary citation: Martinez-Perez, J.A.,Iyengar, S.,Shannon, H.E.,Bleakman, D.,Alt, A.,Clawson, D.K.,Arnold, B.M.,Bell, M.G.,Bleisch, T.J.,Castano, A.M.,Del Prado, M.,Dominguez, E.,Escribano, A.M.,Filla, S.A.,Ho, K.H.,Hudziak, K.J.,Jones, C.K.,Mateo, A.,Mathes, B.M.,Mattiuz, E.L.,Ogden, A.M.,Simmons, R.M.,Stack, D.R.,Stratford, R.E.,Winter, M.A.,Wu, Z.,Ornstein, P.L.; GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.; Bioorg.Med.Chem.Lett., 23:6463-6466, 2013; PubMed: 24140446; DOI: 10.1016/j.bmcl.2013.09.045

Experimental method

X-RAY DIFFRACTION (3 Å)