Structure-Based Rational Design of Chemical Ligands for AMPA-Subtype Glutamate Receptors

Journal of Molecular Neuroscience

Volumn 20, Issue 3, 2003, Pages 345-348

  Zeng, Lei ^a   Chen, Can Hao ^a   Muller, Michaela ^a   Zhou, Ming Ming ^a  

^a NEW YORK UNIVERSITY   (United States)

Author keywords

GluR2; Glutamate receptor; Nuclear magnetic resonance (NMR); Rational ligand design

Indexed keywords

ALPHA AMINO 3 HYDROXY 5 METHYL 4 ISOXAZOLEPROPIONIC ACID; DIMER; GLUTAMATE RECEPTOR 2; LIGAND; PROTEIN SUBUNIT; AMINO ACID RECEPTOR BLOCKING AGENT; AMINO ACID RECEPTOR STIMULATING AGENT; AMPA RECEPTOR; DIAGNOSTIC AGENT; DRUG DERIVATIVE; GLUTAMATE RECEPTOR IONOTROPIC, AMPA 2; GLUTAMIC ACID; RADIOISOTOPE;

ARTICLE; BINDING SITE; DESENSITIZATION; DIMERIZATION; EXTRACELLULAR SPACE; LIGAND BINDING; NUCLEAR MAGNETIC RESONANCE; PROTEIN ANALYSIS; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN FUNCTION; PROTEIN INTERACTION; PROTEIN STRUCTURE; REGULATORY MECHANISM; ALZHEIMER DISEASE; BRAIN; CHEMICAL STRUCTURE; CHEMISTRY; CONFORMATION; DRUG DESIGN; DRUG EFFECT; DRUG SCREENING; HUMAN; METABOLISM; NUCLEAR MAGNETIC RESONANCE SPECTROSCOPY; PATHOPHYSIOLOGY; PHYSIOLOGY; SYNAPTIC TRANSMISSION;

ALZHEIMER DISEASE; BINDING SITES; BRAIN; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; EXCITATORY AMINO ACID AGONISTS; EXCITATORY AMINO ACID ANTAGONISTS; GLUTAMIC ACID; HUMANS; LIGANDS; MAGNETIC RESONANCE SPECTROSCOPY; MODELS, MOLECULAR; MOLECULAR CONFORMATION; MOLECULAR STRUCTURE; RADIOISOTOPES; RECEPTORS, AMPA; SYNAPTIC TRANSMISSION;

EID: 0642370862     PISSN: 08958696     EISSN: None     Source Type: Journal    
DOI: 10.1385/JMN:20:3:345     Document Type: Article

References (13)

1. Armstrong N. and Gouaux E. (2000) Mechanisms for activation and antagonism of an AMPA-sensitive glutamate receptor: crystal structures of the GluR2 ligand binding core. Neuron 28, 165-181.
2. Armstrong N., Sun Y., Chen G. Q., and Gouaux E. (1998) Structure of a glutamate-receptor ligand-binding core in complex with kainate. Nature 395, 913-917.
3. Burnashev N., Monyer H., Seeberg P. H., and Sakmann B. (1992) Divalent ion permeability of AMPA receptor channels is dominated by the edited form of a single subunit. Neuron 8, 189-198.
4. Hajduk P. J., Measdows R. P., and Fesik S. W. (1999) NMR-based screening in drug discovery. Q. Rev. Biophys. 32, 211-240.
5. Hollmann M. and Heibemann S. (1994) Cloned glutamate receptors. Annu. Rev. Neurosci. 17, 31-108.
6. Kuusinen A., Arvola M., and Keinanen K. (1995) Molecular dissection of the agonist binding site of an AMPA receptor. EMBO J. 14, 6327-6332.
7. Lee J.-M., Zipfel G. J., and Choi D. W. (1999) The changing landscape of ischaemic brain injury mechanisms. Nature 399, A7-A14.
8. Moore J. M. (1999) NMR screening in drug discovery. Curr. Opin. Biotechnol. 10, 54-58.
9. Morrison J. H. and Hof P. R. (1997) Life and death of neurons in the aging brain. Science 278, 412-419.
10. 2+-permeable AMPA receptors in neurological disorders. Trends Neurosci. 20, 464-470.
11. Seeburg P. H. (1993) The TINS/TiPS lecture. The moecular biology of mammalian glutamte receptor channels. Trends Neurosci. 16, 359-365.
12. Sun Y., Olson R., Horning M., Armstrong N., Mayer M., and Gouaux E. (2002) Mechanism of glutamate receptor desensitization. Nature 417, 245-253.
13. Weinstein H. and Osman R. (1989) Interaction mechanisms at biological targets: Implications for design of serotonin receptor ligands, in Computer-Aided Molecular Design (IBC Technical Services, London, UK).