A novel photoaffinity ligand for the phencyclidine site of the N-methyl-D-aspartate receptor labels a Mr 120,000 polypeptide.
作者： M S Sonders , P Barmettler , J A Lee , Y Kitahara , J F Keana
DOI: 10.1016/S0021-9258(19)39216-6
关键词: Chemistry 、 Phencyclidine 、 Aspartic acid 、 Ligand (biochemistry) 、 Amino acid 、 Biochemistry 、 Stereochemistry 、 Receptor complex 、 NMDA receptor 、 Binding site 、 Affinity label
摘要: A radiolabeled photoaffinity ligand has been developed for the N-methyl-D-aspartate (NMDA)-preferring excitatory amino acid receptor complex. [3H]3-Azido-(5S, 10R)(+)-5-methyl-10,11-dihydro-5H- dibenzo[a,d]cyclohepten-5,10-imine [3H]3-azido-MK-801 demonstrated nearly identical affinity, density of binding sites, selectivity, pH sensitivity, and pharmacological profile in reversible assays with guinea pig brain homogenates to those displayed by its parent compound, MK-801. When employed a photo-labeling protocol designed optimize specific incorporation, labeled single protein band which migrated sodium dodecyl sulfate-polyacrylamide gels Mr = 120,000. Incorporation tritium into this was completely inhibited when were coincubated 10 microM phencyclidine. These data suggest that phencyclidine site NMDA complex is at least part comprised 120,000 polypeptide.
sci-hub.st 参考文章(45)
M M Gottesman, I Pastan, The multidrug transporter, a double-edged sword. Journal of Biological Chemistry. ,vol. 263, pp. 12163- 12166 ,(1988) , 10.1016/S0021-9258(18)37730-5
A. Bar-Sinai, Y. Aldouby, M. Chorev, A. Levitzki, Association of turkey erythrocyte beta-adrenoceptors with a specific lipid component. The EMBO Journal. ,vol. 5, pp. 1175- 1180 ,(1986) , 10.1002/J.1460-2075.1986.TB04343.X
P G Strange, The structure and mechanism of neurotransmitter receptors. Implications for the structure and function of the central nervous system. Biochemical Journal. ,vol. 249, pp. 309- 318 ,(1988) , 10.1042/BJ2490309
J W Chen, M D Cunningham, N Galton, E K Michaelis, Immune labeling and purification of a 71-kDa glutamate-binding protein from brain synaptic membranes. Possible relationship of this protein to physiologic glutamate receptors. Journal of Biological Chemistry. ,vol. 263, pp. 417- 426 ,(1988) , 10.1016/S0021-9258(19)57409-9
RG Sorensen, MP Blaustein, m-Azido-phencyclidine covalently labels the rat brain PCP receptor, a putative K channel The Journal of Neuroscience. ,vol. 6, pp. 3676- 3681 ,(1986) , 10.1523/JNEUROSCI.06-12-03676.1986
D R Hampson, K D Wheaton, C J Dechesne, R J Wenthold, Identification and characterization of the ligand binding subunit of a kainic acid receptor using monoclonal antibodies and peptide mapping. Journal of Biological Chemistry. ,vol. 264, pp. 13329- 13335 ,(1989) , 10.1016/S0021-9258(18)51632-X
Guy Beauregard, Arlette Maret, Robert Salvayre, Michel Potier, The Radiation Inactivation Method as a Tool to Study Structure-Function Relationships in Proteins Methods of Biochemical Analysis. ,vol. 32, pp. 313- 343 ,(1987) , 10.1002/9780470110539.CH6
E S Deneris, J Boulter, J Connolly, E Wada, K Wada, D Goldman, L W Swanson, J Patrick, S Heinemann, Genes encoding neuronal nicotinic acetylcholine receptors. Clinical Chemistry. ,vol. 35, pp. 731- 737 ,(1989) , 10.1093/CLINCHEM/35.5.731
Richard W. Ransom, Nancy L. Stec, Cooperative modulation of [3H]MK-801 binding to the N-methyl-D-aspartate receptor-ion channel complex by L-glutamate, glycine, and polyamines. Journal of Neurochemistry. ,vol. 51, pp. 830- 836 ,(1988) , 10.1111/J.1471-4159.1988.TB01818.X
Rachel Haring, Yoel Kloog, Na-ava harshak-Felixbrodt, Mordechai Sokolovsky, Multiple mode of binding of phencyclidines: High affinity association between phencyclidine receptors in rat brain and a monovalent ion-sensitive polypeptide Biochemical and Biophysical Research Communications. ,vol. 142, pp. 501- 510 ,(1987) , 10.1016/0006-291X(87)90303-2