Point mutations of the α1β2γ2 γ-aminobutyric acidA receptor affecting modulation of the channel by ligands of the benzodiazepine binding site

Molecular Pharmacology

Volumn 49, Issue 6, 1996, Pages 1080-1084

  Buhr, Andreas ^a   Baur, Roland ^a   Malherbe, Pari ^b   Sigel, Erwin ^a  

^a UNIVERSITY OF BERN   (Switzerland)

^b F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; 4 ETHYL 6,7 DIMETHOXY BETA CARBOLINE 3 CARBOXYLIC ACID METHYL ESTER; DIAZEPAM; RECEPTOR SUBUNIT; ZOLPIDEM;

AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; CHLORIDE CURRENT; CONFORMATIONAL TRANSITION; DRUG BINDING SITE; DRUG EFFECT; DRUG RECEPTOR BINDING; NEUROTRANSMISSION; NONHUMAN; OOCYTE; POINT MUTATION; PRIORITY JOURNAL; PROTEIN CONFORMATION; RECEPTOR AFFINITY; XENOPUS LAEVIS;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; CHLORIDE CHANNELS; DIAZEPAM; LIGANDS; MOLECULAR SEQUENCE DATA; POINT MUTATION; PYRIDINES; RATS; RECEPTORS, GABA-A; STRUCTURE-ACTIVITY RELATIONSHIP; XENOPUS LAEVIS;

EID: 0029998387     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (28)

1. Sigel, E., F. A. Stephenson, C. Mamalaki, and E. A. Barnard, A γ-aminobutyric acid/benzodiazepine receptor complex of bovine cerebral cortex: purification and partial characterization. J. Biol. Chem. 258:6965-6971 (1983).
2. Schofield, P. R., M. G. Darlison, N. Fujita, D. R. Burt, F. A. Stephenson, H. Rodriguez, L. M. Rhee, J. Ramachandran, V. Reale, T. A. Glencorse, P. H. Seeburg, and E. A. Barnard. Sequence and functional expression of the GABA-A receptor shows a ligand-gated receptor superfamily. Nature (Lond.) 328:221-227 (1987).
3. A receptor subtypes: from pharmacology to molecular biology. FASEB J. 5:2916-2923 (1991).
4. A receptor channels. Annu. Rev. Neurosci. 17:569-602 (1994).
5. A receptor. Int. Rev. Neurobiol. 36:51-96 (1994).
6. A receptor determined by electron microscope image analysis. J. Neurochem. 62:815-818 (1994).
7. Galzi, J. L., and J. P Changeas. Neurotransmitter-gated ion channels as unconventional allosteric proteins. Curr. Opin. Struc. Biol. 4:554-565 (1994).
8. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature (Lond.) 366:565-569 (1993).
9. A receptor channels. EMBO J. 11:2017-2023 (1992).
10. A receptor α-subunit. J. Biol. Chem. 269:20380-20387 (1994).
11. A receptor subunit for benzodiazepine pharmacology. Nature (Lond.) 338:582-585 (1989).
12. A receptors on channel function. Neuron 5:703-711 (1990).
13. A receptor α5-subunit creates novel type II benzodiazepine receptor pharmacology. J. Neurochem. 54:1802-1804 (1990).
14. A chloride channels and benzodiazepine binding sites in baculovirus infected insect cells. Biotechnol. 10:79-681 (1992).
15. A receptor. Eur. J. Pharmacol. 246:283-287 (1993).
16. A receptors. Mol. Pharmacol. 44:1211-1218 (1993).
17. Lüddens, H., P. H. Seeburg, and E. R. Korpi. Impact of β and γ variants on ligand-binding properties of γ-aminobutyric acid type A receptors. Mol. Pharmacol. 45:810-814 (1994).
18. Mihic, S. J., P. J. Whiting, R. L. Klein, K. A. Wafford, and R. A. Harris. A single amino acid of the human γ-aminobutyric acid type A receptor γ2 subunit determines benzodiazepine efficacy. J. Biol. Chem. 269:32768-32773 (1994).
19. A receptor channels of mouse spinal neurones in culture. J. Physiol. 475:69-82 (1994).
20. A receptor. FEBS Lett. 246:145-148 (1998).
21. A-receptor expressed from rat brain α- and β-subunit cDNAs display potentiation by benzodiazepine receptor ligands. Mol. Brain Res. 8:199-208 (1990).
22. Malherbe, P., E. Sigel, R. Baur, E. Persohn, J. G. Richards, and H. Mohler. Functional characteristics and sites of gene expression of the α1β1γ2-isoform of the rat GABAA receptor. J. Neurosci. 10:2330-2337 (1990).
23. A receptor subtypes. Pharmacol. Rev. 47:181-233 (1995).
24. A receptor but the α1 polypeptide is the principal site of the agonist benzodiazepine photoaffinity labelling reaction. J. Biol. Chem. 265:21160-21165 (1990).
25. Pritchett, D. B., and P. H. Seeburg. γ-Aminobutyric acid type A receptor point mutation increases the affinity of compounds for the benzodiazepine site. Proc. Natl. Acad. Sci. USA 88:1421-1425 (1991).
26. A receptors is essential for benzodiazepine agonist binding. J. Biol. Chem. 267:1426-1429 (1992).
27. A receptor. Nature (Lond) 361:356-359 (1993).
28. A receptor J. Med. Chem. 37:4576-4580 (1994).