Neurosteroid binding sites on GABAA receptors

Pharmacology and Therapeutics

Volumn 116, Issue 1, 2007, Pages 7-19

  Hosie, Alastair M ^a   Wilkins, Megan E ^a   Smart, Trevor G ^a  

^a UNIVERSITY COLLEGE LONDON   (United Kingdom)

Author keywords

Binding site; GABAA receptor; Neurosteroid binding site; Transmembrane domains

Indexed keywords

3ALPHA HYDROXY 5ALPHA PREGNAN 20 ONE; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID C RECEPTOR; ALFAXALONE; ELTANOLONE; GLYCINE RECEPTOR; MUSCIMOL; N METHYL DEXTRO ASPARTIC ACID RECEPTOR 2B; NEUROSTEROID; PENTOBARBITAL; PICROTOXIN; PRASTERONE SULFATE; PREGNENOLONE SULFATE; PROGESTERONE; PROPOFOL; RECEPTOR SUBUNIT; TERT BUTYLBICYCLOPHOSPHOROTHIOATE; TETRAHYDRODEOXYCORTICOSTERONE;

CENTRAL NERVOUS SYSTEM; DRUG BINDING SITE; DRUG POTENCY; DRUG RECEPTOR BINDING; GABAERGIC SYSTEM; HUMAN; NERVE CELL EXCITABILITY; NERVE CELL PLASTICITY; PATHOPHYSIOLOGY; PRIORITY JOURNAL; RECEPTOR SENSITIVITY; REVIEW; STRUCTURE ACTIVITY RELATION;

ANIMALS; BINDING SITES; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; RECEPTORS, GABA-A; STEROIDS; SYNAPTIC TRANSMISSION;

EID: 34548639993     PISSN: 01637258     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.pharmthera.2007.03.011     Document Type: Review

References (129)

1. A receptors: mechanism and involvement of a residue in the M2 region of the α subunit. J Physiol 532 (2001) 673-684
2. A receptors. J Physiol 558 (2004) 59-74
3. A receptor. J Neurosci 25 (2005) 11605-11613
4. Alakoskela J.M., Covey D.F., and Kinnunen P.K. Lack of enantiomeric specificity in the effects of anesthetic steroids on lipid bilayers. Biochim Biophys Acta 1768 (2007) 131-145
5. A receptors by redox reagents. J Physiol 517 (1999) 35-50
6. A receptors. J Med Chem 43 (2000) 4118-4125
7. Backstrom T., Andersson A., Andree L., Birzniece V., Bixo M., Bjorn I., et al. Pathogenesis in menstrual cycle-linked CNS disorders. Ann N Y Acad Sci 1007 (2003) 42-53
8. Barbaccia M.L. Neurosteroidogenesis: relevance to neurosteroid actions in brain and modulation by psychotropic drugs. Crit Rev Neurobiol 16 (2004) 67-74
9. A receptor-mediated inhibitory neurotransmission in the rat hippocampus: evidence for endogenous neurosteroids?. J Neurosci 23 (2003) 10013-10020
10. A receptor. Nat Rev Neurosci 6 (2005) 565-575
11. Belelli D., Lambert J.J., Peters J.A., Wafford K., and Whiting P.J. The interaction of the general anesthetic etomidate with the γ-aminobutyric acid type A receptor is influenced by a single amino acid. Proc Natl Acad Sci U S A 94 (1997) 11031-11036
12. Belelli D., Pau D., Cabras G., Peters J.A., and Lambert J.J. A single amino acid confers barbiturate sensitivity upon the GABA γ1 receptor. Br J Pharmacol 127 (1999) 601-604
13. A and glycine receptors. Neurochem Int 34 (1999) 447-452
14. A receptors. Neuropharmacology 43 (2002) 651-661
15. Ben Ari Y. Excitatory actions of GABA during development: the nature of the nurture. Nat Rev Neurosci 3 (2002) 728-739
16. A receptor channels from low- to high-efficacy gating patterns. J Neurosci 23 (2003) 10934-10943
17. A receptors. J Neuroendocrinol 7 (1995) 171-177
18. Brambilla F., Biggio G., Pisu M.G., Bellodi L., Perna G., Bogdanovich-Djukic V., et al. Neurosteroid secretion in panic disorder. Psychiatry Res 118 (2003) 107-116
19. A receptor function and cell surface expression. Pharmacol Ther 94 (2002) 113-122
20. Buhr A., Wagner C., Fuchs K., Sieghart W., and Sigel E. Two novel residues in M2 of the gamma-aminobutyric acid type A receptor affecting gating by GABA and picrotoxin affinity. J Biol Chem 276 (2001) 7775-7781
21. A receptor by progesterone metabolites. Proc R Soc Lond B Biol Sci 231 (1987) 359-369
22. A receptor in anesthetic modulation and direct activation. J Biol Chem 278 (2003) 42821-42828
23. Chen R., Belelli D., Lambert J.J., Peters J.A., Reyes A., and Lan N.C. Cloning and functional expression of a Drosophila γ-aminobutyric acid receptor. Proc Natl Acad Sci U S A 91 (1994) 6069-6073
24. A receptor plasticity by progesterone metabolites. Eur J Pharmacol 375 (1999) 225-235
25. Cossart R., Bernard C., and Ben Ari Y. Multiple facets of GABAergic neurons and synapses: multiple fates of GABA signalling in epilepsies. Trends Neurosci 28 (2005) 108-115
26. A receptor activity by alphaxalone. Br J Pharmacol 90 (1987) 491-500
27. Couture J.F., Legrand P., Cantin L., Luu-The V., Labrie F., and Breton R. Human 20α-hydroxysteroid dehydrogenase: crystallographic and site-directed mutagenesis studies lead to the identification of an alternative binding site for C21-steroids. J Mol Biol 331 (2003) 593-604
28. A receptors. Brain Res Brain Res Rev 37 (2001) 91-97
29. A receptor modulation and anesthesia. J Pharmacol Exp Ther 293 (2000) 1009-1016
30. Darbandi-Tonkabon R., Hastings W.R., Zeng C.M., Akk G., Manion B.D., Bracamontes J.R., et al. Photoaffinity labeling with a neuroactive steroid analogue. 6-azi-pregnanolone labels voltage-dependent anion channel-1 in rat brain. J Biol Chem 278 (2003) 13196-13206
31. A receptor-mediated current. J Physiol 550 (2003) 679-691
32. Enz R., and Bormann J. A single point mutation decreases picrotoxinin sensitivity of the human GABA receptor ρ1 subunit. NeuroReport 6 (1995) 1569-1572
33. Eser D., Schule C., Baghai T.C., Romeo E., Uzunov D.P., and Rupprecht R. Neuroactive steroids and affective disorders. Pharmacol Biochem Behav 84 (2006) 656-666
34. Fancsik A., Linn D.M., and Tasker J.G. Neurosteroid modulation of GABA IPSCs is phosphorylation dependent. J Neurosci 20 (2000) 3067-3075
35. A receptors. Nat Rev Neurosci 6 (2005) 215-229
36. Ffrench-Constant R.H., Rocheleau T.A., Steichen J.C., and Chalmers A.E. A point mutation in a Drosophila GABA receptor confers insecticide resistance. Nature 363 (1993) 449-451
37. Finn D.A., Beadles-Bohling A.S., Beckley E.H., Ford M.M., Gililland K.R., Gorin-Meyer R.E., et al. A new look at the 5alpha-reductase inhibitor finasteride. CNS Drug Rev 12 (2006) 53-76
38. Fritschy J.M., and Brunig I. Formation and plasticity of GABAergic synapses: physiological mechanisms and pathophysiological implications. Pharmacol Ther 98 (2003) 299-323
39. Gaiarsa J.L., Caillard O., and Ben Ari Y. Long-term plasticity at GABAergic and glycinergic synapses: mechanisms and functional significance. Trends Neurosci 25 (2002) 564-570
40. Gao W., Bohl C.E., and Dalton J.T. Chemistry and structural biology of androgen receptor. Chem Rev 105 (2005) 3352-3370
41. Germain P., Staels B., Dacquet C., Spedding M., and Laudet V. Overview of nomenclature of nuclear receptors. Pharmacol Rev 58 (2006) 685-704
42. Grishkovskaya I., Avvakumov G.V., Sklenar G., Dales D., Hammond G.L., and Muller Y.A. Crystal structure of human sex hormone-binding globulin: steroid transport by a laminin G-like domain. EMBO J 19 (2000) 504-512
43. A channel that abolish block by picrotoxin. Receptors Channels 3 (1995) 13-20
44. A receptors by the non-steroidal anti-inflammatory agent, mefenamic acid. Eur J Neurosci 11 (1999) 2897-2905
45. A receptors in rat CA1 and dentate gyrus neurones. Neuropharmacology 45 (2003) 873-883
46. 2+: an endogenous modulator of ligand- and voltage-gated ion channels. Neuropharmacology 33 (1994) 935-952
47. Harrison N.L., and Simmonds M.A. Modulation of the GABA receptor complex by a steroid anaesthetic. Brain Res 323 (1984) 287-292
48. Hemmings Jr. H.C., Akabas M.H., Goldstein P.A., Trudell J.R., Orser B.A., and Harrison N.L. Emerging molecular mechanisms of general anesthetic action. Trends Pharmacol Sci 26 (2005) 503-510
49. Hosie A.M., and Sattelle D.B. Allosteric modulation of an expressed homo-oligomeric GABA-gated chloride channel of Drosophila melanogaster. Br J Pharmacol 117 (1996) 1229-1237
50. A receptors: discrete binding sites underlie subtype specificity. Nat Neurosci 6 (2003) 362-369
51. A receptors through two discrete transmembrane sites. Nature 444 (2006) 486-489
52. Huang R.Q., and Dillon G.H. Effect of extracellular pH on GABA-activated current in rat recombinant receptors and thin hypothalamic slices. J Neurophysiol 82 (1999) 1233-1243
53. Jang M.K., Mierke D.F., Russek S.J., and Farb D.H. A steroid modulatory domain on NR2B controls N-methyl-d-aspartate receptor proton sensitivity. Proc Natl Acad Sci U S A 101 (2004) 8198-8203
54. Jiang X., Manion B.D., Benz A., Rath N.P., Evers A.S., Zorumski C.F., et al. Neurosteroid analogues: 9. Conformationally constrained pregnanes: structure-activity studies of 13,24-cyclo-18,21-dinorcholane analogues of the GABA modulatory and anesthetic steroids (3α,5α)- and (3α,5β)-3-hydroxypregnan-20-one. J Med Chem 46 (2003) 5334-5348
55. Jin Y., Stayrook S.E., Albert R.H., Palackal N.T., Penning T.M., and Lewis M. Crystal structure of human type III 3α-hydroxysteroid dehydrogenase/bile acid binding protein complexed with NADPand ursodeoxycholate. Biochemistry 40 (2001) 10161-10168
56. Krasowski M.D., Koltchine V.V., Rick C.E., Ye Q., Finn S.E., and Harrison N.L. Propofol and other intravenous anaesthetics have sites of action on the γ-aminobutyric acid type A receptor distinct from that for isoflurane. Mol Pharmacol 53 (1998) 530-538
57. A receptor is associated with the receptor subunit composition. J Physiol 492 (1996) 431-443
58. Kumar S., Fleming R.L., and Morrow A.L. Ethanol regulation of gamma-aminobutyric acid A receptors: genomic and nongenomic mechanisms. Pharmacol Ther 101 (2004) 211-226
59. A receptors. Prog Neurobiol 71 (2003) 67-80
60. A receptors. Mol Pharmacol 69 (2006) 2015-2026
61. C receptor as the mechanism of steroid action. Mol Pharmacol 69 (2006) 1779-1782
62. A receptors mediating tonic inhibition alter seizure susceptibility and anxiety. Nat Neurosci 8 (2005) 797-804
63. Majewska M.D., and Schwartz R.D. Pregnenolone-sulfate: an endogenous antagonist of the gamma-aminobutyric acid receptor complex in brain?. Brain Res 404 (1987) 355-360
64. Majewska M.D., Harrison N.L., Schwartz R.D., Barker J.L., and Paul S.M. Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 232 (1986) 1004-1007
65. Majewska M.D., Mienville J.M., and Vicini S. Neurosteroid pregnenolone sulfate antagonizes electrophysiological responses to GABA in neurons. Neurosci Lett 90 (1988) 279-284
66. A receptor. Eur J Pharmacol 189 (1990) 307-315
67. A receptor. Brain Res 526 (1990) 143-146
68. Maksay G., Laube B., and Betz H. Subunit-specific modulation of glycine receptors by neurosteroids. Neuropharmacology 41 (2001) 369-376
69. Marx C.E., Stevens R.D., Shampine L.J., Uzunova V., Trost W.T., Butterfield M.I., et al. Neuroactive steroids are altered in schizophrenia and bipolar disorder: relevance to pathophysiology and therapeutics. Neuropsychopharmacology 31 (2006) 1249-1263
70. A receptors. Mol Pharmacol 65 (2004) 1191-1197
71. A and glycine receptors. Nature 389 (1997) 385-389
72. Miyazawa A., Fujiyoshi Y., and Unwin N. Structure and gating mechanism of the acetylcholine receptor pore. Nature 424 (2003) 949-955
73. A receptors responsible for tonic and phasic conductances. Neurochem Res 26 (2001) 907-913
74. Morris K.D., and Amin J. Insight into the mechanism of action of neuroactive steroids. Mol Pharmacol 66 (2004) 56-69
75. Morris K.D., Moorefield C.N., and Amin J. Differential modulation of the γ-aminobutyric acid type C receptor by neuroactive steroids. Mol Pharmacol 56 (1999) 752-759
76. Morrow A.L., Suzdak P.D., and Paul S.M. Steroid hormone metabolites potentiate GABA receptor-mediated chloride ion flux with nanomolar potency. Eur J Pharmacol 142 (1987) 483-485
77. Nahoum V., Gangloff A., Legrand P., Zhu D.W., Cantin L., Zhorov B.S., et al. Structure of the human 3α-hydroxysteroid dehydrogenase type 3 in complex with testosterone and NADP at 1.25-A resolution. J Biol Chem 276 (2001) 42091-42098
78. Newland C.F., and Cull-Candy S.G. On the mechanism of action of picrotoxin on GABA receptor channels in dissociated sympathetic neurones of the rat. J Physiol (Lond) 447 (1992) 191-213
79. A receptor pharmacology of enantiomers of dehydroepiandrosterone sulfate, pregnenolone sulfate, and (3α,5β)-3-hydroxypregnan-20-one sulfate. J Med Chem 41 (1998) 2604-2613
80. A receptors underlies potentiation at hippocampal inhibitory synapses. Nature 395 (1998) 172-177
81. Pan Z.H., Bahring R., Grantyn R., and Lipton S.A. Differential modulation by sulfhydryl redox agents and glutathione of GABA- and glycine-evoked currents in rat retinal ganglion cells. J Neurosci 15 (1995) 1384-1391
82. A receptors. Neuroscience 98 (2000) 333-338
83. A receptor function through distinct sites. Brain Res 830 (1999) 72-87
84. A receptors. Biochem Pharmacol 68 (2004) 819-831
85. A receptor subunit composition?. Receptors Channels 1 (1993) 135-142
86. Purdy R.H., Morrow A.L., Moore Jr. P.H., and Paul S.M. Stress-induced elevations of γ-aminobutyric acid type A receptor-active steroids in the rat brain. Proc Natl Acad Sci U S A 88 (1991) 4553-4557
87. A receptors in Xenopus oocyte. Eur J Pharmacol 547 (2006) 37-44
88. A receptor at sites on the N-terminal side of the middle of TM2. NeuroReport 9 (1998) 379-383
89. Rupprecht R., and Holsboer F. Neuroactive steroids: mechanisms of action and neuropsychopharmacological perspectives. Trends Neurosci 22 (1999) 410-416
90. Schwabe J.W.R., and Teichmann S.A. Nuclear receptors: the evolution of diversity. Sci STKE (2004) E4
91. A receptor. J Physiol 577 (2006) 569-577
92. A receptors: modulating gain and maintaining the tone. Trends Neurosci 27 (2004) 262-269
93. A receptors. Neuropharmacology 38 (1999) 267-271
94. A receptor desensitization. J Neurosci 20 (2000) 3571-3579
95. A receptor subtypes. Curr Top Med Chem 2 (2002) 795-816
96. A receptor by steroids. Neurosciences 3 (1991) 231-239
97. Smart T.G., Xie X., and Krishek B.J. Modulation of inhibitory and excitatory amino acid receptor ion channels by zinc. Prog Neurobiol 42 (1994) 393-441
98. A receptor complex reveals that it may act via the picrotoxin site. J Pharmacol Exp Ther 282 (1997) 827-833
99. A receptor d subunit. J Neurophysiol 90 (2003) 903-910
100. Spivak V., Lin A., Beebe P., Stoll L., and Gentile L. Identification of a neurosteroid binding site contained within the GluR2-S1S2 domain. Lipids 39 (2004) 811-819
101. A receptors. Proc Natl Acad Sci U S A 100 (2003) 14439-14444
102. Stoffel-Wagner B. Neurosteroid biosynthesis in the human brain and its clinical implications. Ann N Y Acad Sci 1007 (2003) 64-78
103. A receptor in primary neuronal cultures. J Med Chem 49 (2006) 3225-3234
104. Tasker J. Coregulation of ion channels by neurosteroids and phosphorylation. Sci STKE (2000) E1
105. Thompson S.A., Arden S.A., Marshall G., Wingrove P.B., Whiting P.J., and Wafford K.A. Residues in transmembrane domains I and II determine γ-aminobutyric acid type AA receptor subtype-selective antagonism by furosemide. Mol Pharmacol 55 (1999) 993-999
106. A α1 receptor using three crystal structures as templates. J Mol Graph Model 23 (2004) 39-49
107. Tsutsui K. Biosynthesis, mode of action and functional significance of neurosteroids in the developing Purkinje cell. J Steroid Biochem Mol Biol 102 (2006) 187-194
108. A receptors expressed in Xenopus oocytes. Br J Pharmacol 127 (1999) 377-382
109. Ueno S., Tsutsui M., Toyohira Y., Minami K., and Yanagihara N. Sites of positive allosteric modulation by neurosteroids on ionotropic γ-aminobutyric acid receptor subunits. FEBS Lett 566 (2004) 213-217
110. Uzunova V., Sampson L., and Uzunov D.P. Relevance of endogenous 3α-reduced neurosteroids to depression and antidepressant action. Psychopharmacology 186 (2006) 351-361
111. Wang T.L., Hackam A.S., Guggino W.B., and Cutting G.R. A single amino acid in gamma-aminobutyric acid rho 1 receptors affects competitive and noncompetitive components of picrotoxin inhibition. Proc Natl Acad Sci U S A 92 (1995) 11751-11755
112. A receptor antagonists. J Neurosci 22 (2002) 3366-3375
113. A receptor through different channel property. Acta Physiol (Oxf) 188 (2006) 153-162
114. A receptor confer sensitivity to the neurosteroid pregnenolone sulfate. Br J Pharmacol 148 (2006) 162-172
115. Weatherman R.V., Fletterick R.J., and Scanlan T.S. Nuclear-receptor ligands and ligand-binding domains. Annu Rev Biochem 68 (1999) 559-581
116. A receptors. Br J Anaesth 92 (2004) 704-711
117. 2+ complexation. Neuropharmacology 43 (2002) 938-944
118. Wilkins M.E., Hosie A.M., and Smart T.G. Identification of a β subunit TM2 residue mediating proton modulation of GABA type A receptors. J Neurosci 22 (2002) 5328-5333
119. A receptors: influence of GABA concentration and the β subunit TM2-TM3 domain. J Physiol 567 (2005) 365-377
120. Williams D.B., and Akabas M.H. γ-aminobutyric acid increases the water accessibility of M3 membrane-spanning segment residues in γ-aminobutyric acid type A receptors. Biophys J 77 (1999) 2563-2574
121. Wingrove P.B., Wafford K.A., Bain C., and Whiting P.J. The modulatory action of loreclezole at the γ-aminobutyric acid type A receptor is determined by a single amino acid in the β2 and β3 subunit. Proc Natl Acad Sci U S A 91 (1994) 4569-4573
122. A receptor modulation and anesthesia. Mol Pharmacol 50 (1996) 1581-1586
123. A receptors containing the delta subunit. J Neurosci 22 (2002) 1541-1549
124. Woodward R.M., Polenzani L., and Miledi R. Effects of steroids on γ-aminobutyric acid receptors expressed in Xenopus oocytes by poly(A)+ RNA from mammalian brain and retina. Mol Pharmacol 41 (1992) 89-103
125. Wurtz J.M., Bourguet W., Renaud J.P., Vivat V., Chambon P., Moras D., et al. A canonical structure for the ligand-binding domain of nuclear receptors. Nat Struct Biol 3 (1996) 206
126. A receptor channel-lining residues probed in cysteine mutants. Biophys J 69 (1995) 1858-1867
127. A receptor neurosteroid site. J Pharmacol Exp Ther 281 (1997) 1095-1101
128. Yoon K.W., Covey D.F., and Rothman S.M. Multiple mechanisms of picrotoxin block of GABA-induced currents in rat hippocampal neurons. J Physiol 464 (1993) 423-439
129. A channel deactivation by altering kinetics of desensitized states. J Neurosci 17 (1997) 4022-4031