Identification of Critical Residues in the Amino Terminal Domain of the Human NR2B Subunit Involved in the RO 25-6981 Binding Pocket

Journal of Pharmacology and Experimental Therapeutics

Volumn 307, Issue 3, 2003, Pages 897-905

  Malherbe, Pari ^a,f   Mutel, Vincent ^a,c   Broger, Clemens ^a   Perin Dureau, Florent ^b   Kemp, John A ^a,d   Neyton, Jacques ^b   Paoletti, Pierre ^b   Kew, James N C ^a,e  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b CNRS   (France)

^c ADDEX PHARMACEUTICALS   (Switzerland)

^d Evotec Neurosciences GmbH   (Germany)

^e GLAXOSMITHKLINE   (United Kingdom)

^f F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4 CHLOROPHENYL) 2 METHYL 6 METHOXY 7 HYDROXY 1,2,3,4 TETRAHYDROISOQUINOLINE; 2 AMINO 5 PHOSPHONOVALERIC ACID; 4 BENZYL ALPHA (4 HYDROXYPHENYL) BETA METHYL 1 PIPERIDINEPROPANOL; ALPHA (4 HYDROXYPHENYL) BETA METHYL 4 (PHENYLMETHYL) 1 PIPERIDINE PROPANOL; BINDING PROTEIN; COMPLEMENTARY DNA; GLUTAMIC ACID; GLYCINE; IFENPRODIL; N METHYL DEXTRO ASPARTIC ACID; N METHYL DEXTRO ASPARTIC ACID RECEPTOR; N METHYL DEXTRO ASPARTIC ACID RECEPTOR BLOCKING AGENT; RECEPTOR SUBUNIT; RO 04 5595; TRITIUM; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CENTRAL NERVOUS SYSTEM; CONTROLLED STUDY; EMBRYO; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; KIDNEY CELL; MOLECULAR MODEL; NERVE CELL PLASTICITY; NEUROTRANSMISSION; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; POINT MUTATION; PRIORITY JOURNAL; PROTEIN DOMAIN; SITE DIRECTED MUTAGENESIS; VOLTAGE CLAMP; WESTERN BLOTTING; XENOPUS;

ANIMALS; BINDING SITES; BLOTTING, WESTERN; CELL MEMBRANE; CELLS, CULTURED; DNA, COMPLEMENTARY; EXCITATORY AMINO ACID ANTAGONISTS; HUMANS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; PATCH-CLAMP TECHNIQUES; PHENOLS; PIPERIDINES; POINT MUTATION; RECEPTORS, N-METHYL-D-ASPARTATE; TRANSFECTION; XENOPUS;

EID: 0344304828     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: 10.1124/jpet.103.056291     Document Type: Article

References (40)

1. Anson LC, Chen PE, Wyllie DJ, Colquhoun D, and Schoepfer R (1998) Identification of amino acid residues of the NR2A subunit that control glutamate potency in recombinant NR1/NR2A NMDA receptors. J Neurosci 18:581-589.
2. Armstrong N, Sun Y, Chen GQ, and Gouaux E (1998) Structure of a glutamate-receptor ligand-binding core in complex with kainate. Nature (Lond) 395:913-917.
3. Brimecombe JC, Gallagher MJ, Lynch DR, and Aizenman E (1998) An NR2B point mutation affecting haloperidol and CP101, 606 sensitivity of single recombinant N-methyl-D-aspartate receptors. J Pharmacol Exp Ther 286:627-634.
4. Carter CJ, Lloyd KG, Zivkovic B, and Scatton B (1990) Ifenprodil and SL 82.0715 as cerebral antiischemic agents. III. Evidence for antagonistic effects at the polyamine modulatory site within the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther 253:475-482.
5. Choi DW (1988) Glutamate neurotoxicity and diseases of the nervous system. Neuron 1:623-634.
6. 2+ inhibition of the NMDA receptor. Neuron 23:171-180.
7. Dingledine R, Borges K, Bowie D, and Traynelis SF (1999) The glutamate receptor ion channels. Pharmacol Rev 51:7-61.
8. 2+ binding to NMDA receptors. Neuron 25:683-694.
9. Fischer G, Mutel V, Trube G, Malherbe P, Kew JN, Mohacsi E, Heitz MP, and Kemp JA (1997) Ro 25-6981, a highly potent and selective blocker of N-methyl-D-aspartate receptors containing the NR2B subunit. Characterization in vitro. J Pharmacol Exp Ther 283:1285-1292.
10. Furukawa H and Gouaux E (2003) Mechanisms of activation, inhibition and specificity: crystal structures of the NMDA receptor NR1 ligand-binding core. EMBO (Eur Mol Biol Organ) J 22:2873-2885.
11. Gallagher MJ, Huang H, Grant ER, and Lynch DR (1997) The NR2B-specific interactions of polyamines and protons with the N-methyl-D-aspartate receptor. J Biol Chem 272:24971-24979.
12. Gallagher MJ, Huang H, Pritchett DB, and Lynch DR (1996) Interactions between ifenprodil and the NR2B subunit of the N-methyl-D-aspartate receptor. J Biol Chem 271:9603-9611.
13. Gerber PR and Muller K (1995) MAB, a generally applicable molecular force field for structure modelling in medicinal chemistry. J Comput Aided Mol Des 9:251-268.
14. Gotti B, Duverger D, Bertin J, Carter C, Dupont R, Frost J, Gaudilliere B, MacKenzie ET, Rousseau J, Scatton B, et al. (1988) Ifenprodil and SL 82.0715 as cerebral anti-ischemic agents. I. Evidence for efficacy in models of focal cerebral ischemia. J Pharmacol Exp Ther 247:1211-1221.
15. Graham D, Darles G, and Langer SZ (1992) The neuroprotective properties of ifenprodil, a novel NMDA receptor antagonist, in neuronal cell culture toxicity studies. Eur J Pharmacol 226:373-376.
16. Johnson JW and Ascher P (1987) Glycine potentiates the NMDA response in cultured mouse brain neurons. Nature (Lond) 325:529-531.
17. Kemp JA and Kew JN (1998) NMDA receptor antagonists, in Receptor-Based Drug Design (Leff P ed) pp 297-321, Marcel Dekker, Inc., New York.
18. Kew JN and Kemp JA (1998) An allosteric interaction between the NMDA receptor polyamine and ifenprodil sites in rat cultured cortical neurones. J Physiol (Lond)l 512:17-28.
19. Kew JN, Koester A, Moreau JL, Jenck F, Ouagazzal AM, Mutel V, Richards JG, Trube G, Fischer G, Montkowski A, et al. (2000) Functional consequences of reduction in NMDA receptor glycine affinity in mice carrying targeted point mutations in the glycine binding site. J Neurosci 20:4037-4049.
20. Kew JN, Trube G, and Kemp JA (1996) A novel mechanism of activity-dependent NMDA receptor antagonism describes the effect of ifenprodil in rat cultured cortical neurones. J Physiol (Lond) 497:761-772.
21. Kleckner NW and Dingledine R (1988) Requirement for glycine in activation of NMDA-receptors expressed in Xenopus oocytes. Science (Wash DC) 241:835-837.
22. Kunishima N, Shimada Y, Tsuji Y, Sato T, Yamamoto M, Kumasaka T, Nakanishi S, Jingami H, and Morikawa K (2000) Structural basis of glutamate recognition by a dimeric metabotropic glutamate receptor. Nature (Lond) 407:971-977.
23. Kuryatov A, Laube B, Betz H, and Kuhse J (1994) Mutational analysis of the glycine-binding site of the NMDA receptor: structural similarity with bacterial amino acid-binding proteins. Neuron 12:1291-1300.
24. Laube B, Hirai H, Sturgess M, Betz H, and Kuhse J (1997) Molecu]ar determinants of agonist discrimination by NMDA receptor subunits: analysis of the glutamate binding site on the NR2B subunit. Neuron 18:493-503.
25. Low CM, Zheng F, Lyuboslavsky P, and Traynelis SF (2000) Molecular determinants of coordinated proton and zinc inhibition of N-methyl-D-aspartate NR1/NR2A receptors. Proc Natl Acad Sci USA 97:11062-11067.
26. Malherbe P, Knoflach F, Broger C, Ohresser S, Kratzeisen C, Adam G, Stadler H, Kemp JA, and Mutel V (2001) Identification of essential residues involved in the glutamate binding pocket of the group II metabotropic glutamate receptor. Mol Pharmacol 60:944-954.
27. McBain CJ and Mayer ML (1994) N-Methyl-D-aspartic acid receptor structure and function. Physiol Rev 74:723-760.
28. Mutel V, Buchy D, Klingelschmidt A, Messer J, Bleuel Z, Kemp JA, and Richards JG (1998) In vitro binding properties in rat brain of [3H]Ro 25-6981, a potent and selective antagonist of NMDA receptors containing NR2B subunits. J Neurochem 70:2147-2155.
29. O'Hara PJ, Sheppard PO, Thogersen H, Venezia D, Haldeman BA, McGrane V, Houamed KM, Thomsen C, Gilbert TL, and Mulvihill ER (1993) The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins. Neuron 11:41-52.
30. Paoletti P, Ascher P, and Neyton J (1997) High-affinity zinc inhibition of NMDA NR1-NR2A receptors. J Neurosci 17:5711-5725.
31. 2+. Neuron 15:1109-1120.
32. Paoletti P, Perin-Dureau F, Fayyazuddin A, Le Goff A, Callebaut I, and Neyton J (2000) Molecular organization of a zinc binding N-terminal modulatory domain in a NMDA receptor subunit. Neuron 28:911-925.
33. Perin-Dureau F, Rachline J, Neyton J, and Paoletti P (2002) Mapping the binding site of the neuroprotectant ifenprodil on NMDA receptors. J Neurosci 22:5955-5965.
34. Reynolds IJ and Miller RJ (1989) Ifenprodil is a novel type of N-methyl-D-aspartate receptor antagonist: interaction with polyamines. Mol Pharmacol 36:758-765.
35. Sack JS, Saper MA, and Quiocho FA (1989) Periplasmic binding protein structure and function. Refined X-ray structures of the leucine/isoleucine/valine-binding protein and its complex with leucine. J Mol Biol 206:171-191.
36. Sigel E, Baur R, and Malherbe P (1994) Protein kinase C transiently activated heteromeric N-methyl-D-aspartate receptor channels independent of the phosphorylatable C-terminal splice domain and of consensus phosphorylation sites. J Biol Chem 269:8204-8208.
37. Stern-Bach Y, Bettler B, Hartley M, Sheppard PO, O'Hara PJ, and Heinemann SF (1994) Agonist selectivity of glutamate receptors is specified by two domains structurally related to bacterial amino acid-binding proteins. Neuron 13:1345-1357.
38. Tamiz AP, Whittemore ER, Zhou ZL, Huang JC, Drewe JA, Chen JC, Cai SX, Weber E, Woodward RM, and Keana JF (1998) Structure-activity relationships for a series of bis(phenylalkyl)amines: potent subtype-selective inhibitors of N-methyl-D-aspartate receptors. J Med Chem 41:3499-3506.
39. Wafford KA, Kathoria M, Bain CJ, Marshall G, Le Bourdelles B, Kemp JA, and Whiting PJ (1995) Identification of amino acids in the N-methyl-D-aspartate receptor NR1 subunit that contribute to the glycine binding site. Mol Pharmacol 47:374-380.
40. Williams K (1993) Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol Pharmacol 44:851-859.