The F-loop of the GABAa receptor γ2 subunit contributes to benzodiazepine modulation

Journal of Biological Chemistry

Volumn 283, Issue 5, 2008, Pages 2702-2708

  Padgett, Claire L ^a,b   Lummis, Sarah C R ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b SALK INSTITUTE FOR BIOLOGICAL STUDIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION ANALYSIS; BINDING ENERGY; CHEMICAL PROPERTIES; HYDROGEN; HYDROPHOBICITY; MODULATION;

BENZODIAZEPINES; BINDING AFFINITIES; BINDING CHARACTERISTICS; CONFORMATIONAL CHANGES; HOMOLOGY MODELING; HOMOLOGY MODELS; HYDROPHOBIC INTERACTIONS; LOOP RESIDUES; RADIOLIGAND BINDINGS; RECEPTOR ACTIVATIONS; RECEPTOR BINDINGS; TWO STATES; UNBOUND STATES; VOLTAGE CLAMPS; WILD TYPES;

HYDROGEN BONDS;

4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID A RECEPTOR GAMMA 2; ALANINE; ARGININE; ASPARAGINE; BENZODIAZEPINE; DIAZEPAM; FLUMAZENIL; RADIOLIGAND; TRITIUM; UNCLASSIFIED DRUG; BENZODIAZEPINE RECEPTOR AFFECTING AGENT; GAMMA2 SUBUNIT, GABA A RECEPTOR; GAMMA2 SUBUNIT, GABA-A RECEPTOR; RECOMBINANT PROTEIN;

ANIMAL CELL; ARTICLE; CONFORMATIONAL TRANSITION; DRUG BINDING; ELECTROPHYSIOLOGY; EMBRYO; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; HYDROPHOBICITY; LIGAND BINDING; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; RECEPTOR UPREGULATION; REGULATORY MECHANISM; SEQUENCE HOMOLOGY; SITE DIRECTED MUTAGENESIS; VOLTAGE CLAMP; AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMAL; CELL LINE; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECT; GENETICS; IN VITRO STUDY; METABOLISM; MOLECULAR GENETICS; OOCYTE; PATCH CLAMP; PROTEIN CONFORMATION; RADIOASSAY; XENOPUS LAEVIS;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ANIMALS; CELL LINE; DIAZEPAM; FEMALE; GABA MODULATORS; HUMANS; HYDROGEN BONDING; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; MUTAGENESIS, SITE-DIRECTED; OOCYTES; PATCH-CLAMP TECHNIQUES; PROTEIN CONFORMATION; RADIOLIGAND ASSAY; RECEPTORS, GABA-A; RECOMBINANT PROTEINS; SEQUENCE HOMOLOGY, AMINO ACID; XENOPUS LAEVIS;

EID: 41449090845     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M705699200     Document Type: Article

References (30)

1. Olsen, R. W. (1982) Annu. Rev. Pharmacol. Toxicol. 22, 245-277
2. Rusch, D., and Forman, S. A. (2005) Anesthesiology 102, 783-792
3. Campo-Soria, C., Chang, Y., and Weiss, D. S. (2006) Br. J. Pharmacol. 148, 984-990
4. Downing, S. S., Lee, Y. T., Farb, D. H., and Gibbs, T. T. (2005) Br. J. Pharmacol. 145, 894-906
5. Kloda, J. H., and Czajkowski, C. (2007) Mol. Pharmacol. 71, 483-493
6. Sancar, F., Ericksen, S. S., Kucken, A. M., Teissere, J. A., and Czajkowski, C. (2007) Mol. Pharmacol. 71, 38-46
7. Brejc, K., van Dijk, W. J., Klaassen, R. V., Schuurmans, M., van Der Oost, J., Smit, A. B., and Sixma, T. K. (2001) Nature 411, 269-276
8. Kash, T. L., Jenkins, A., Kelley, J. C., Trudell, J. R., and Harrison, N. L. (2003) Nature 421, 272-275
9. Lummis, S. C., Beene, D. L., Lee, L. W., Lester, H. A., Broadhurst, R. W., and Dougherty, D. A. (2005) Nature 438, 248-252
10. Mercado, J., and Czajkowski, C. (2006) J. Neurosci. 26, 2031-2040
11. Unwin, N. (2005) J. Mol. Biol. 346, 967-989
12. Boileau, A. J., and Czajkowski, C. (1999) J. Neurosci. 19, 10213-10220
13. Jordan, M., Schallhorn, A., and Wurm, F. M. (1996) Nucleic Acids Res. 24, 596-601
14. Kunkel, T. A. (1985) Proc. Natl. Acad. Sci. U. S. A. 82, 488-492
15. Sambrook, J., Fritsch, E. F., and Maniatis, T. (1989) Molecular Cloning: A Laboratory Manual, 2nd Ed., pp. 15.54-15.56, Cold Spring Harbor Laboratory Press, Cold Spring Harbor, NY
16. Turchin, A., and Lawler, J. F., Jr. (1999) BioTechniques 26, 672-676
17. Lummis, S. C., Sepulveda, M. I., Kilpatrick, G. J., and Baker, J. (1993) Eur. J. Pharmacol. 243, 7-11
18. Klein, R. L., Whiting, P. J., and Harris, R. A. (1994) J. Neurochem. 63, 2349-2352
19. Liman, E. R., Tytgat, J., and Hess, P. (1992) Neuron 9, 861-871
20. Reeves, D. C., Sayed, M. F., Chau, P. L., Price, K. L., and Lummis, S. C. (2003) Biophys. J. 84, 2338-2344
21. Thompson, A. J., Padgett, C. L., and Lummis, S. C. (2006) J. Biol. Chem. 281, 16576-16582
22. Shi, J., Blundell, T. L., and Mizuguchi, K. (2001) J. Mol. Biol. 310, 243-257
23. Sali, A., and Blundell, T. L. (1993) J. Mol. Biol. 234, 779-815
24. Buhr, A., Baur, R., Malherbe, P., and Sigel, E. (1996) Mol. Pharmacol. 49, 1080-1084
25. Czajkowski, C., and Karlin, A. (1995) J. Biol. Chem. 270, 3160-3164
26. Newell, J. G., and Czajkowski, C. (2003) J. Biol. Chem. 278, 13166-13172
27. Celie, P. H., van Rossum-Fikkert, S. E., van Dijk, W. J., Brejc, K., Smit, A. B., and Sixma, T. K. (2004) Neuron 41, 907-914
28. Corringer, P. J., Le Novere, N., and Changeux, J. P. (2000) Annu. Rev. Pharmacol. Toxicol. 40, 431-458
29. Karobath, M., Supavilai, P., and Borea, P. A. (1983) Adv. Biochem. Psychopharmacol. 38, 37-45
30. Jones-Davis, D. M., Song, L., Gallagher, M. J., and Macdonald, R. L. (2005) J. Neurosci. 25, 8056-8065