Is the isolated ligand binding domain a good model of the domain in the native receptor?

被引:18
作者
Deming, D [1 ]
Cheng, Q [1 ]
Jayaraman, V [1 ]
机构
[1] Univ Texas, Hlth Sci Ctr, Dept Integrat Biol & Pharmacol, Houston, TX 77030 USA
关键词
SELECTIVE GLUTAMATE RECEPTORS; AMPA RECEPTOR; STABLE EXPRESSION; DESENSITIZATION; CORE;
D O I
10.1074/jbc.C300105200
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Numerous studies have used the atomic level structure of the isolated ligand binding domain of the glutamate receptor to elucidate the agonist-induced activation and desensitization processes in this group of proteins. However, no study has demonstrated the structural equivalence of the isolated ligand binding fragments and the protein in the native receptor. In this report, using visible absorption spectroscopy we show that the electronic environment of the antagonist 6-cyano-7-nitro-2,3-dihydroxyquinoxaline is identical for the isolated protein and the native glutamate receptors expressed in cells. Our results hence establish that the local structure of the ligand binding site is the same in the two proteins and validate the detailed structure-function relationships that have been developed based on a comparison of the structure of the isolated ligand binding domain and electrophysiological consequences in the native receptor.
引用
收藏
页码:17589 / 17592
页数:4
相关论文
共 16 条
[1]   Stable expression of homomeric AMPA-selective glutamate receptors in BHK cells [J].
Andersen, PH ;
Tygesen, CK ;
Rasmussen, JS ;
SoegaardNielsen, L ;
Hansen, A ;
Hansen, K ;
Kiemer, A ;
Stidsen, CE .
EUROPEAN JOURNAL OF PHARMACOLOGY, 1996, 311 (01) :95-100
[2]   Mechanisms for activation and antagonism of an AMPA-Sensitive glutamate receptor: Crystal structures of the GluR2 ligand binding core [J].
Armstrong, N ;
Gouaux, E .
NEURON, 2000, 28 (01) :165-181
[3]   Probing the ligand binding domain of the GluR2 receptor by proteolysis and deletion mutagenesis defines domain boundaries and yields a crystallizable construct [J].
Chen, GQ ;
Sun, Y ;
Jin, RS ;
Gouaux, E .
PROTEIN SCIENCE, 1998, 7 (12) :2623-2630
[4]   Overexpression of a glutamate receptor (GluR2) ligand binding domain in Escherichia coli: Application of a novel protein folding screen [J].
Chen, GQ ;
Gouaux, E .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1997, 94 (25) :13431-13436
[5]  
Hennegriff M, 1997, J NEUROCHEM, V68, P2424
[6]   CLONED GLUTAMATE RECEPTORS [J].
HOLLMANN, M ;
HEINEMANN, S .
ANNUAL REVIEW OF NEUROSCIENCE, 1994, 17 :31-108
[7]   Ligand-protein interactions in the glutamate receptor [J].
Jayaraman, V ;
Keesey, R ;
Madden, DR .
BIOCHEMISTRY, 2000, 39 (30) :8693-8697
[8]   A FAMILY OF AMPA-SELECTIVE GLUTAMATE RECEPTORS [J].
KEINANEN, K ;
WISDEN, W ;
SOMMER, B ;
WERNER, P ;
HERB, A ;
VERDOORN, TA ;
SAKMANN, B ;
SEEBURG, PH .
SCIENCE, 1990, 249 (4968) :556-560
[9]   Molecular dissection of the agonist binding site of an AMPA receptor [J].
Kuusinen, A ;
Arvola, M ;
Keinanen, K .
EMBO JOURNAL, 1995, 14 (24) :6327-6332
[10]   The structure and function of glutamate receptor ion channels [J].
Madden, DR .
NATURE REVIEWS NEUROSCIENCE, 2002, 3 (02) :91-101