Functional asymmetry of the conserved cystine loops in αβγ GABAA receptors revealed by the response to GABA activation and drug potentiation

International Journal of Biochemistry and Cell Biology

Volumn 40, Issue 5, 2008, Pages 968-979

  Tierney, M Louise ^a   Luu, Tien ^a   Gage, Peter W ^a  

^a Biology and Environment   (Australia)

Author keywords

Cys loop; Diazepam; Electrophysiology; GABAA receptor; Gating

Indexed keywords

4 AMINOBUTYRIC ACID A RECEPTOR; ALIPHATIC CARBOXYLIC ACID; AROMATIC CARBOXYLIC ACID; CYSTINE; DIAZEPAM; ETOMIDATE; LIGAND; PENTOBARBITAL; PROLINE;

ARTICLE; CELL STRAIN L 929; CHANNEL GATING; CYS LOOP; DRUG ACTIVATION; DRUG POTENTIATION; ELECTROPHYSIOLOGY; LIGAND BINDING; MUTATION; PATCH CLAMP; WHOLE CELL;

AMINO ACID MOTIFS; AMINO ACID SEQUENCE; CELL LINE; CYSTINE; DIAZEPAM; DRUG SYNERGISM; ETOMIDATE; GABA MODULATORS; GAMMA-AMINOBUTYRIC ACID; HUMANS; ION CHANNEL GATING; MOLECULAR SEQUENCE DATA; PATCH-CLAMP TECHNIQUES; PENTOBARBITAL; PROLINE; PROTEIN CONFORMATION; RECEPTORS, GABA-A; RECEPTORS, GABA-B;

EID: 40149087048     PISSN: 13572725     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.biocel.2007.10.029     Document Type: Article

References (35)

1. Absalom N.L., Lewis T.M., Kaplan W., Pierce K.D., and Schofield P.R. Role of charged residues in coupling ligand binding and channel activation in the extracellular domain of the glycine receptor. J Biol Chem 278 (2003) 50151-50157
2. A receptor needs 2 homologous domains of the beta-subunit for activation by GABA but not by pentobarbital. Nature 366 (1993) 565-569
3. A receptor channel superfamily. Trends Neurosci 10 (1987) 502-509
4. Belelli D., Lambert J.J., Peters J.A., Wafford K.A., and Whiting P.J. The interaction of the general anesthetic etomidate with the gamma-aminobutyric acid type A receptor is influenced by a single amino acid. Proc Natl Acad Sci USA 94 (1997) 11031-11036
5. Blount P., and Merlie J.P. Mutational analysis of muscle nicotinic acetylcholine receptor subunit assembly. J Cell Biol 111 (1990) 2613-2622
6. Brejc K., van Dijk W.J., Klaassen R.V., Schuurmans M., van Der Oost J., Smit A.B., et al. Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature 411 (2001) 269-276
7. Brown N., Kerby J., Bonnert T.P., Whiting P.J., and Wafford K.A. Pharmacological characterization of a novel cell line expressing human alpha(4)beta(3)delta GABA(A) receptors. Br J Pharmacol 136 (2002) 965-974
8. Celie P.H., van Rossum-Fikkert S.E., van Dijk W.J., Brejc K., Smit A.B., and Sixma T.K. Nicotine and carbamylcholine binding to nicotinic acetylcholine receptors as studied in AChBP crystal structures. Neuron 41 (2004) 907-914
9. Cromer B.A., Morton C.J., and Parker M.W. Anxiety over GABA(A) receptor structure relieved by AChBP. Trends Biochem Sci 27 (2002) 280-287
10. A receptors are directly activated but not modulated by pentobarbital. Eur J Pharmacol 385 (1999) 283-286
11. Dellisanti C.D., Yao Y., Stroud J.C., Wang Z.-Z., and Chen L. Crystal structure of the extracellular domain of nAChR α1 bound to α-bungarotoxin at 1.94 Å resolution. Nat Neurosci 10 (2007) 953-962
12. Fu D.-X., and Sine S.M. Assymmetrical contribution of the conserved disulfide loop to subunit oligomerization and assembly of the nicotinic acetylcholine receptor. J Biol Chem 271 (1996) 31479-31484
13. Hamill O.P., Marty A., Neher E., Sakmann B., and Sigworth F.J. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches. Pflugers Arch 391 (1981) 85-100
14. Hill-Venning C., Belelli D., Peters J.A., and Lambert J.J. Subunit-dependent interaction of the general anaesthetic etomidate with the gamma-aminobutyric acid type A receptor. Br J Pharmacol 120 (1997) 749-756
15. A receptor. Nature 421 (2003) 272-275
16. A receptor activation. J Biol Chem 279 (2004) 4887-4893
17. A receptor anesthetic binding site at subunit interfaces by photolabeling with an etomidate analog. J Neurosci 26 (2006) 11599-11605
18. Lummis S.C., Beene D.L., Lee L.W., Lester H.A., Broadhurst R.W., and Dougherty D.A. Cis-trans isomerization at a proline opens the pore of a neurotransmitter-gated ion channel. Nature 438 (2005) 248-252
19. A channels co-expressed with GABARAP. J Biol Chem 281 (2006) 35699-35708
20. Mathers D.A., and Barker J.L. (-)Pentobarbital opens ion channels of long duration in cultured mouse spinal neurons. Science 209 (1980) 507-509
21. Mihic S.J., Whiting P.J., Klein R.L., Wafford K.A., and Harris R.A. A single amino acid of the human gamma-aminobutyric acid type A receptor gamma(2) subunit determines benzodiazepine efficacy. J Biol Chem 269 (1994) 32768-32773
22. Miyazawa A., Fujiyoshi Y., and Unwin N. Structure and gating mechanism of the acetylcholine receptor pore. Nature 423 (2003) 949-955
23. Ortells M.O., and Lunt G.G. Evolutionary history of the ligand-gated ion-channel superfamily of receptors. Trends Neurosci 18 (1995) 121-127
24. R Development Core Team. R: A language and environment for statistical computing (2006), R Foundation for Statistical Computing, Vienna, Austria
25. A receptors by barbiturates in cultured rat hippocampal neurons. J Physiol 497 (1996) 509-522
26. A receptor shows a ligand-gated receptor super-family. Nature 328 (1987) 221-227
27. Schofield C.M., Trudell J.R., and Harrison N.L. Alanine-scanning mutagenesis in the signature disulfide loop of the glycine receptor alpha 1 subunit: Critical residues for activation and modulation. Biochemistry 43 (2004) 10058-10063
28. Shen X.M., Ohno K., Sine S.M., and Engel A.G. Subunit-specific contribution to agonist binding and channel gating revealed by inherited mutation in muscle acetylcholine receptor M3-M4 linker. Brain 128 (2005) 345-355
29. A receptors. Trends Pharmacol Sci 18 (1997) 425-429
30. Sigel E., Schaerer M.T., Buhr A., and Baur R. The benzodiazepine binding pocket of recombinant alpha1beta2gamma2 gamma-aminobutyric acid A receptors: Relative orientation of ligands and amino acid side chains. Mol Pharmacol 54 (1998) 1097-1105
31. Unwin N. Refined structure of the nicotinic acetylcholine receptor at 4 Å resolution. J Mol Biol 346 (2005) 967-989
32. Unwin N., Miyazawa A., Li J., and Fujiyoshi Y. Activation of the nicotinic acetylcholine receptor involves a switch in conformation of the alpha subunits. J Mol Biol 319 (2002) 1165-1176
33. A receptors depend upon subunit composition. Neuron 4 (1990) 919-928
34. Xiu X., Hanek A.P., Wang J., Lester H.A., and Dougherty D.A. A unified view of the role of electrostatic interactions in modulating the gating of Cys loop receptors. J Biol Chem 280 (2005) 41655-41666
35. A receptor-gated currents in cultured postnatal hippocampal neurons. Neuroscience 73 (1996) 69-78