Mechanism of partial agonism at NMDA receptors for a conformationally restricted glutamate analog

Journal of Neuroscience

Volumn 25, Issue 34, 2005, Pages 7858-7866

  Erreger, Kevin ^a,d   Geballe, Matthew T ^b   Dravid, Shashank M ^a   Snyder, James P ^b   Wyllie, David J A ^c   Traynelis, Stephen F ^a  

^a EMORY UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b EMORY UNIVERSITY   (United States)

^c UNIVERSITY OF EDINBURGH   (United Kingdom)

^d VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Gating; Glutamate; Ion channel; Molecular dynamics; NMDA; Structure

Indexed keywords

COMPLEMENTARY RNA; GLUTAMATE RECEPTOR AGONIST; GLUTAMIC ACID; HOMOQUINOLINATE; ION CHANNEL; N METHYL DEXTRO ASPARTIC ACID; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR STIMULATING AGENT; PARTIAL AGONIST; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL STRAIN HEK293; CHANNEL GATING; CONFORMATIONAL TRANSITION; EMBRYO; HUMAN; HUMAN CELL; MOLECULAR DYNAMICS; MOLECULAR INTERACTION; NEUROTRANSMISSION; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PATCH CLAMP; PRIORITY JOURNAL; RECEPTOR BINDING; SITE DIRECTED MUTAGENESIS; VOLTAGE CLAMP; XENOPUS LAEVIS;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; EXCITATORY AMINO ACID AGONISTS; FEMALE; GLUTAMIC ACID; HUMANS; MOLECULAR SEQUENCE DATA; PROTEIN CONFORMATION; QUINOLINIC ACIDS; RECEPTORS, N-METHYL-D-ASPARTATE; XENOPUS LAEVIS;

EID: 23944453392     PISSN: 02706474     EISSN: None     Source Type: Journal    
DOI: 10.1523/JNEUROSCI.1613-05.2005     Document Type: Article

References (32)

1. Ariens EJ (1954) Affinity and intrinsic activity in the theory of competitive inhibition. I. Problems and theory. Arch Int Pharmacodyn Ther 99:32-49.
2. Armstrong N, 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.
3. Armstrong N, Sun Y, Chen GQ, Gouaux E (1998) Structure of a glutamate-receptor ligand-binding core in complex with kainate. Nature 395:913-917.
4. Banke TG, Traynelis SF (2003) Activation of NR1/NR2B NMDA receptors. Nat Neurosci 6:144-152.
5. Banke TG, Dravid SM, Traynelis SF (2005) Protons trap NR1/NR2B NMDA receptors in a nonconducting state. J Neurosci 25:42-51.
6. Berendsen HJC, van der Spoelvan D, Drunen R (1995) GROMACS: a message-passing parallel molecular dynamics implementation. Comp Phys Commun 91:43-56.
7. Chen PE, Geballe MT, Stansfeld PJ, Johnston AR, Yuan H, Jacob AL, Snyder JP, Traynelis SF, Wyllie DJ (2005) Structural features of the glutamate binding site in recombinant NR1/NR2A N-methyl-D-aspartate receptors determined by site-directed mutagenesis and molecular modeling. Mol Pharmacol
8. Del Castillo J, Katz B (1957) Interaction at end-plate receptors between different choline derivatives. Proc R Soc Lond B Biol Sci 146:369-381.
9. Dingledine R, Borges K, Bowie D, Traynelis SF (1999) The glutamate receptor ion channels. Pharmacol Rev 51:7-61.
10. Erreger K, Chen PE, Wyllie DJ, Traynelis SF (2004) Glutamate receptor gating. Grit Rev Neurobiol 16:187-224.
11. Erreger K, Dravid SM, Banke TG, Wyllie DJ, Traynelis SF (2005) Subunit-specific gating controls rat NR1/NR2A and NR1/NR2B NMDA channel kinetics and synaptic signalling profiles. J Physiol (Lond) 563:345-358.
12. Furukawa H, Gouaux E (2003) Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core. EMBO J 22:2873-2885.
13. Gibb AJ, Colquhoun D (1991) Glutamate activation of a single NMDA receptor-channel produces a cluster of channel openings. Proc Biol Sci 243:39-45.
14. Gouaux E (2004) Structure and function of AMPA receptors. J Physiol (Lond) 554:249-253.
15. Inanobe A, Furukawa H, Gouaux E (2005) Mechanism of partial agonist action at the NR1 subunit of NMDA receptors. Neuron 47:71-84.
16. Jackson MB, Wong BS, Morris CE, Lecar H, Christian CN (1983) Successive openings of the same acetylcholine receptor channel are correlated in open time. Biophys J 42:109-114.
17. Jin R, Gouaux E (2003) Probing the function, conformational plasticity, and dimer-dimer contacts of the GluR2 ligand-binding core: studies of 5-substituted willardiines and GluR2 S1S2 in the crystal. Biochemistry 42:5201-5213.
18. Jin R, Horning M, Mayer ML, Gouaux E (2002) Mechanism of activation and selectivity in a ligand-gated ion channel: structural and functional studies of GluR2 and quisqualate. Biochemistry 41:15635-15643.
19. Jin R, Banke TG, Mayer ML, Traynelis SF, Gouaux E (2003) Structural basis for partial agonist action at ionotropic glutamate receptors. Nat Neurosci 6:803-810.
20. Lindahl E, Hess B, van der Spoelvan D (2001) GROMACS 3.0: a package for molecular simulation and trajectory analysis. J Mol Mod 7:306-317.
21. Mayer ML, Armstrong N (2004) Structure and function of glutamate receptor ion channels. Annu Rev Physiol 66:161-181.
22. Popescu G, Auerbach A (2003) Modal gating of NMDA receptors and the shape of their synoptic response. Nat Neurosci 6:476-483.
23. Popescu G, Robert A, Howe JR, Auerbach A (2004) Reaction mechanism determines NMDA receptor response to repetitive stimulation. Nature 430:790-793.
24. Qin F (2004) Restoration of single-channel currents using the segmental k-means method based on hidden Markov modeling. Biophys J 86:1488-1501.
25. Qin F, Auerbach A, Sachs F (1996) Estimating single-channel kinetic parameters from idealized patch-clamp data containing missed events. Biophys J 70:264-280.
26. Rosenmund C, Stern-Bach Y, Stevens CF (1998) The tetrameric structure of a glutamate receptor channel. Science 280:1596-1599.
27. Smith TC, Wang LY, Howe JR (2000) Heterogeneous conductance levels of native AMPA receptors. J Neurosci 20:2073-2085.
28. Stephenson RP (1956) A modification of receptor theory. Br J Pharmacol 11:379-393.
29. Traynelis SF, Burgess MF, Zheng F, Lyuboslavsky P, Powers JL (1998) Control of voltage-independent zinc inhibition of NMDA receptors by the NR1 subunit. J Neurosci 18:6163-6175.
30. Wyllic DJ, Behe P, Colquhoun D (1998) Single-channel activations and concentration jumps: comparison of recombinant NR1a/NR2A and NRla/NR2D NMDA receptors. J Physiol (Lond) 510:1-18.
31. Zheng F, Gingrich MB, Traynelis SF, Conn PJ (1998) Tyrosine kinase potentiates NMDA receptor currents by reducing tonic zinc inhibition. Nat Neurosci 1:185-191.
32. Zheng F, Erreger K, Low CM, Banke T, Lee CJ, Conn PJ, Traynelis SF (2001) Allosteric interaction between the amino terminal domain and the ligand binding domain of NR2A. Nat Neurosci 4:894-901.