A tight coupling between β 2Y97 and β 2F200 of the GABA A receptor mediates GABA binding

Journal of Neurochemistry

Volumn 119, Issue 2, 2011, Pages 283-293

  Tran, Phu N ^a   Laha, Kurt T ^a   Wagner, David A ^a  

^a Marquette University   (United States)

Author keywords

functional coupling; GABA binding; GABA A receptor

Indexed keywords

4 AMINOBUTYRIC ACID RECEPTOR; ARGININE ALPHA1R120; ARGININE ALPHA1R132; ARGININE ALPHA1R207; ARGININE ALPHA1R67; ARGININE DERIVATIVE; AROMATIC COMPOUND; BETA2F200; BETA2Y97; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CONTROLLED STUDY; EVOKED RESPONSE; HUMAN; HUMAN CELL; LIGAND BINDING; MUTATION; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN INTERACTION; RECEPTOR BINDING;

ALGORITHMS; ARGININE; CELLS, CULTURED; CHLORIDE CHANNELS; DNA, COMPLEMENTARY; ELECTROPHYSIOLOGICAL PHENOMENA; GABA ANTAGONISTS; GAMMA-AMINOBUTYRIC ACID; HEK293 CELLS; HUMANS; KINETICS; MODELS, MOLECULAR; MUTAGENESIS; PATCH-CLAMP TECHNIQUES; RECEPTORS, GABA-A; TRANSFECTION;

EID: 80053501223     PISSN: 00223042     EISSN: 14714159     Source Type: Journal    
DOI: 10.1111/j.1471-4159.2011.07409.x     Document Type: Article

References (35)

1. Amin J., and, Weiss D., (1993) GABAA receptor needs two homologous domains of the β subunit for activation by GABA, but not by pentobarbital. Nature 366, 565-569. (Pubitemid 24035996)
2. Beene D. L., Brandt G. S., Zhong W., Zacharias N. M., Lester H. A., and, Dougherty D. A., (2002) Cation-pi interactions in ligand recognition by serotonergic (5-HT3A) and nicotinic acetylcholine receptors: the anomalous binding properties of nicotine. Biochemistry 41, 10262-10269. (Pubitemid 34856451)
3. Boileau A. J., Evers A. R., Davis A. F., and, Czajkowski C., (1999) Mapping the agonist binding site of the GABAA receptor: evidence for a β-strand. J. Neurosci. 19, 4847-4854. (Pubitemid 29270121)
4. Boileau A. J., Newell J. G., and, Czajkowski C., (2002) GABAA receptor β2 Tyr97 and Leu99 line the GABA-binding site: insights into mechanisms of agonist and antagonist actions. J. Biol. Chem. 277, 2931-2937. (Pubitemid 34953327)
5. Bollan K., King D., Robertson L. A., Brown K., Taylor P. M., Moss S. J., and, Connolly C. N., (2003) GABA(A) receptor composition is determined by distinct assembly signals within alpha and beta subunits. J. Biol. Chem. 278, 4747-4755. (Pubitemid 36800976)
6. Bourne Y., Radic Z., Araoz R., Talley T. T., Benoit E., Servent D., Taylor P., Molgo J., and, Marchot P., (2010) Structural determinants in phycotoxins and AChBP conferring high affinity binding and nicotinic AChR antagonism. Proc. Natl Acad. Sci. USA 107, 6076-6081.
7. Brejc K., van Dijk W. J., Klaassen R. V., Schuurmans M., van Der Oost J., Smit A. B., and, Sixma T. K., (2001) Crystal structure of an ACh-binding protein reveals the ligand-binding domain of nicotinic receptors. Nature 411, 269-276. (Pubitemid 32467026)
8. Colquhoun D., (1998) Binding, gating, affinity and efficacy: the interpretation of structure-activity relationships for agonists and of the effects of mutating receptors. Br. J. Pharmacol. 125, 924-947.
9. Cromer B. A., Morton C. J., and, Parker M. W., (2002) Anxiety over GABA(A) receptor structure relieved by AChBP. Trends Biochem. Sci. 27, 280-287. (Pubitemid 34628667)
10. Crowley P. B., and, Golovin A., (2005) Cation-π interactions in protein-protein interfaces. Proteins 59, 231-239.
11. Ernst M., Brauchart D., Boresch S., and, Sieghart W., (2003) Comparative modeling of GABA(A) receptors: limits, insights, future developments. Neuroscience 119, 933-943. (Pubitemid 36776445)
12. Gallivan J. P., and, Dougherty D. A., (1999) Cation-n Interactions in Structural Biology. Am. Chem. Soc. 122, 870-874.
13. Gleitsman K. R., Kedrowski S. M., Lester H. A., and, Dougherty D. A., (2008) An intersubunit hydrogen bond in the nicotinic acetylcholine receptor that contributes to channel gating. J. Biol. Chem. 283, 35638-35643.
14. 1K70 region mediate GABA and SR-95531 actions. J. Biol. Chem. 277, 18785-18792. (Pubitemid 34952437)
15. Horovitz A., (1996) Double-mutant cycles: a powerful tool for analyzing protein structure and function. Fold Des. 1, 121-126.
16. Jones M. V., Sahara Y., Dzubay J. A., and, Westbrook G. L., (1998) Defining affinity with the GABAA receptor. J. Neurosci. 18, 8590-8604.
17. Jones M. V., Jonas P., Sahara Y., and, Westbrook G. L., (2001) Microscopic kinetics and energetics distinguish GABA(A) receptor agonists from antagonists. Biophys. J. 81, 2660-2670. (Pubitemid 33020053)
18. Kash T. L., Jenkins A., Kelley J. C., Trudell J. R., and, Harrison N. L., (2003) Coupling of agonist binding to channel gating in the GABA(A) receptor. Nature 421, 272-275. (Pubitemid 36139131)
19. Kash T. L., Trudell J. R., and, Harrison N. L., (2004) Structural elements involved in activation of the gamma-aminobutyric acid type A (GABAA) receptor. Biochem. Soc. Trans. 32, 540-546. (Pubitemid 38813557)
20. Laha K. T., and, Wagner D. A., (2011) A state-dependent salt-bridge interaction exists across the β/α intersubunit interface of the GABAA receptor. Mol. Pharm. 79, 662-671.
21. A receptor kinetics: evidence for slowed agonist unbinding. J. Neurosci. 20, 899-907. (Pubitemid 30220446)
22. Lummis S. C. R., (2009) Locating GABA in GABA receptor binding sites. Biochem. Soc. Trans. 37, 1343-1346.
23. Lummis S. C., Beene D., Harrison N. J., Lester H. A., and, Dougherty D. A., (2005) A cation-π interaction with a tyrosine in the binding site of the GABAC receptor. Chem. Biol. 12, 993-997. (Pubitemid 41338809)
24. O'Mara M., Cromer B., Parker M., and, Chung S. H., (2005) Homology model of the GABAA receptor examined using Brownian dynamics. Biophys. J. 88, 3286-3299. (Pubitemid 40586580)
25. Padgett C. L., Hanek A. P., Lester H. A., Dougherty D. A., and, Lummis S. C., (2007) Unnatural amino acid mutagenesis of the GABA(A) receptor binding site residues reveals a novel cation-pi interaction between GABA and beta2Tyr97. J. Neurosci. 27, 886-892. (Pubitemid 46174509)
26. Pless S. A., Millen K. S., Hanek A. P., Lynch J. W., Lester H. A., Lummis S. C. R., and, Dougherty D. A., (2008) A cation-π interaction in the binding site of the glycine receptor is mediated by a phenylalanine residue. J. Neurosci. 28, 10937-10942.
27. Price K. L., Millen K. S., and, Lummis S. C., (2007) Transducing agonist binding to channel gating involves different interactions in 5-HT3 and GABAC receptors. J. Biol. Chem. 282, 25623-25630. (Pubitemid 47372843)
28. A receptor channels. EMBO J. 11, 2017-2023.
29. Taylor P. M., Thomas P., Gorrie G. H., Connolly C. N., Smart T. G., and, Moss S. J., (1999) Identification of amino acid residues within GABA(A) receptor beta subunits that mediate both homomeric and heteromeric receptor expression. J. Neurosci. 19, 6360-6371. (Pubitemid 29347436)
30. Venkatachalan S. P., and, Czajkowski C., (2008) A conserved salt bridge critical for GABA(A) receptor function and loop C dynamics. Proc. Natl Acad. Sci. USA 105, 13604-13609.
31. Wagner D. A., and, Czajkowski C., (2001) Structure and dynamics of the GABA binding pocket: a narrowing cleft that constricts during activation. J. Neurosci. 21, 67-74. (Pubitemid 32098727)
32. Wagner D. A., Czajkowski C., and, Jones M. V., (2004) An arginine involved in GABA binding and unbinding but not gating of the GABA(A) receptor. J. Neurosci. 24, 2733-2741. (Pubitemid 38380950)
33. Westh-Hansen S. E., Witt M. R., Dekermendjian K., Liljefors T., Rasmussen P. B., and, Nielsen M., (1999) Arginine residue 120 of the human GABAA receptor alpha 1, subunit is essential for GABA binding and chloride ion current gating. Neuroreport 10, 2417-2421. (Pubitemid 29367949)
34. Zacharias N., and, Dougherty D. A., (2002) Cation-π interactions in ligand recognition and catalysis. Trends Pharmacol. Sci. 23, 281-287. (Pubitemid 34655734)
35. Zhong W., Gallivan J. P., Zhang Y., Li L., Lester H. A., and, Dougherty D. A., (1998) From ab initio quantum mechanics to molecular neurobiology: a cation-pi binding site in the nicotinic receptor. Proc. Natl Acad. Sci. USA 95, 12088-12093. (Pubitemid 28483723)