An epilepsy-related region in the GABAA receptor mediates long-distance effects on GABA and benzodiazepine binding sites

Molecular Pharmacology

Volumn 77, Issue 1, 2010, Pages 35-45

  Goldschen Ohm, Marcel P ^a   Wagner, David A ^b   Petrou, Steven ^c   Jones, Mathew V ^a  

^a UNIVERSITY OF WISCONSIN MADISON   (United States)

^b Marquette University   (United States)

^c UNIVERSITY OF MELBOURNE   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

4 AMINOBUTYRIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; ARGININE; DIAZEPAM; GLUTAMIC ACID;

ARTICLE; BINDING SITE; CELL MEMBRANE; CONTROLLED STUDY; DESENSITIZATION; DISSOCIATION; DRUG BINDING; DRUG POTENTIATION; EMBRYO; EPILEPSY; EVOKED RESPONSE; GENE MUTATION; HUMAN; HUMAN CELL; KINETICS; NOISE; PRIORITY JOURNAL; PROTEIN INTERACTION; RECEPTOR BINDING;

BENZODIAZEPINES; BINDING SITES; CELL LINE; EPILEPSY; GAMMA-AMINOBUTYRIC ACID; HUMANS; KINETICS; MUTATION; PROTEIN BINDING; PROTEIN STABILITY; PROTEIN SUBUNITS; RECEPTORS, GABA-A;

EID: 73549095175     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.109.058289     Document Type: Article

References (40)

1. A receptor needs two homologous domains of the β-subunit for activation by GABA but not by pentobarbital. Nature 366: 565-569.
2. A receptors. Insight into the absolute arrangement. J Biol Chem 277: 46020-46025.
3. A receptors. J Neurosci 23: 11158-11166.
4. A receptor isoforms by a diazepam analogue provides evidence for a novel benzodiazepine binding site that prevents modulation by these drugs. J Neurochem 106: 2353-2363.
5. A receptor mutations linked to epilepsy in humans. J Neurosci 22: 5321-5327.
6. A receptor subunits. Mol Pharmacol 53: 295-303.
7. 2(R43Q)] found in human epilepsy. Proc Natl Acad Sci U S A 99: 15170-15175.
8. Campo-Soria C, Chang Y, and Weiss DS (2006) Mechanism of action of benzodiazepines on GABA(A) receptors. Br J Pharmacol 148: 984-990.
9. Carter PJ, Winter G, Wilkinson AJ, and Fersht AR (1984) The use of double mutants to detect structural changes in the active site of tyrosyl-tRNA synthetase (Bacillus stearothermophilus). Cell 38: 835-840.
10. Colquhoun D and Hawkes AG (1995) A Q-matrix cookbook. How to write only one program to calculate the single-channel and macroscopic predictions for any kinetic mechanism, in Single-Channel Recording (Sakmann B, Neher E eds) pp 589-633, 2nd ed. Plenum Press, New York.
11. Colquhoun D, Dowsland KA, Beato M, and Plested AJ (2004) How to impose microscopic reversibility in complex reaction mechanisms. Biophys J 86: 3510-3518.
12. A receptor structure relieved by AChBP. Trends Biochem Sci 27: 89-96.
13. A receptors supports an allosteric model of modulation. Br J Pharmacol 145: 894-906.
14. 2 subunit mutations linked to human epileptic syndromes differentially affect phasic and tonic inhibition. J Neurosci 27: 14108-14116.
15. 2 or δp subtypes expressed with α1 and β3 subtypes in mouse L929 cells. J Physiol 505: 283-297.
16. A receptor assembly and modifies subunit composition on the cell surface. J Biol Chem 282: 3819-3828.
17. A receptors. Mol Cell Neurosci 29: 120-127.
18. A receptor. J Neurosci 28: 3490-3499.
19. A receptors: discrete binding sites underlie subtype specificity. Nat Neurosci 6: 362-369.
20. A receptor. J Neurosci 18: 8590-8604.
21. A receptor γ2 subunit R43Q mutation linked to childhood absence epilepsy and febrile seizures causes retention of α1β2γ2S receptors in the endoplasmic reticulum. J Neurosci 24: 8672-8677.
22. A receptors. J Gen Physiol 131: 163-181.
23. A receptor microscopic affinity. Neuropharmacology 35: 1383-1392.
24. A-receptor subtypes really occur in the brain? Trends Neurol Sci 19: 139-143.
25. A receptors in cultured murine cerebellar granule cells. J Physiol 503: 353-369.
26. Mercik K, Piast M, and Mozrzymas JW (2007) Benzodiazepine receptor agonists affect both binding and gating of recombinant α1β2γ2 gamma-aminobutyric acid-A receptors. Neuroreport 18: 781-785.
27. Mozrzymas JW, Barberis A, Mercik K, and Zarnowska ED (2003) Binding sties, singly bound states, and conformation coupling shape GABA-evoked currents. J Neurophysiol 89: 871-883.
28. A receptors in central synapses. J Neurosci 19: 578-588.
29. Revah F, Bertrand D, Galzi JL, Devillers-Thiéry A, Mulle C, Hussy N, Bertrand S, Ballivet M, and Changeux JP (1991) Mutations in the channel domain alter desensitization of a neuronal nicotinic receptor. Nature 353:846-849.
30. A receptor channels of mouse spinal neurons in culture. J Physiol 475: 69-82.
31. 2L γ-aminobutyric acid type A receptors. Anesthesiology 102: 783-792.
32. 2R43Q) impairs cell surface expression of αβγ receptors. J Biol Chem 279: 47034-47039.
33. A receptor subtypes. Pharmacol Rev 47: 181-234.
34. A receptors. Trends Pharmacol Sci 18: 425-429.
35. Sigworth FJ (1980) The variance of sodium current fluctuations at the node of Ranvier. J Physiol 307: 97-129.
36. Tan HO, Reid CA, Single FN, Davies PJ, Chiu C, Murphy S, Clarke AL, Dibbens L, Krestel H, Mulley JC, et al. (2007) Reduced cortical inhibition in a mouse model of familial childhood absence epilepsy. Proc Natl Acad Sci U S A 104: 17536-17541.
37. - channels recorded from membrane patches of neonatal rat cortical neurons in culture. J Pharmacol Exp Ther 243: 1195-1201.
38. Wagner DA and Czajkowski C (2001) Structure and dynamics of the GABA binding pocket: a narrowing cleft that constricts during activation. J Neurosci 21: 67-74.
39. A receptor. J Neurosci 24: 2733-2741.
40. 2-subunit in childhood absence epilepsy and febrile seizures. Nat Genet 28: 49-52.