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Volumn 74, Issue 4, 2008, Pages 941-951

Structural determinants for antagonist pharmacology that distinguish the ρ1 GABAC receptor from GABAA receptors

Author keywords

[No Author keywords available]

Indexed keywords

3 AMINO 2 (3 CARBOXYPROPYL) 6 (4 METHOXYPHENYL)PYRIDAZINIUM BROMIDE; 3 AMINOPROPANEPHOSPHONIC ACID; 3 AMINOPROPYL(METHYL)PHOSPHINIC ACID; 4 AMINOBUTYRIC ACID A RECEPTOR; 4 AMINOBUTYRIC ACID C RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR BLOCKING AGENT; BICUCULLINE; PHENYLALANINE; RECEPTOR SUBUNIT; TYROSINE; VALINE;

EID: 52949150747     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.108.048710     Document Type: Article
Times cited : (35)

References (37)
  • 1
    • 0027787023 scopus 로고
    • A receptor needs two homologous domains of the β subunit for activation by GABA, but not by pentobarbital
    • A receptor needs two homologous domains of the β subunit for activation by GABA, but not by pentobarbital. Nature 366:565-569.
    • (1993) Nature , vol.366 , pp. 565-569
    • Amin, J.1    Weiss, D.S.2
  • 2
    • 0028171915 scopus 로고
    • 1 GABA channels: Activation properties and domains
    • 1 GABA channels: activation properties and domains. Receptors Channels 2:227-236.
    • (1994) Receptors Channels , vol.2 , pp. 227-236
    • Amin, J.1    Weiss, D.S.2
  • 3
    • 0029944870 scopus 로고    scopus 로고
    • Insights into the activation mechanism of ρ1 GABA receptors obtained by coexpression of wild type and activation-impaired subunits
    • Amin J and Weiss DS (1996) Insights into the activation mechanism of ρ1 GABA receptors obtained by coexpression of wild type and activation-impaired subunits. Proc Biol Sci 263:273-282.
    • (1996) Proc Biol Sci , vol.263 , pp. 273-282
    • Amin, J.1    Weiss, D.S.2
  • 4
    • 0031799363 scopus 로고    scopus 로고
    • International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acidA receptors: Classification on the basis of subunit structure and receptor function
    • Barnard EA, Skolnick P, Olsen RW, Mohler H, Sieghart W, Biggio G, Braestrup C, Bateson AN, and Langer SZ (1998) International Union of Pharmacology. XV. Subtypes of γ-aminobutyric acidA receptors: classification on the basis of subunit structure and receptor function. Pharmacol Rev 50:291-313.
    • (1998) Pharmacol Rev , vol.50 , pp. 291-313
    • Barnard, E.A.1    Skolnick, P.2    Olsen, R.W.3    Mohler, H.4    Sieghart, W.5    Biggio, G.6    Braestrup, C.7    Bateson, A.N.8    Langer, S.Z.9
  • 5
    • 0028454828 scopus 로고
    • The development of a simple empirical scoring function to estimate the binding constant for a protein-ligand complex of known three-dimensional structure
    • Böhm HJ (1994) The development of a simple empirical scoring function to estimate the binding constant for a protein-ligand complex of known three-dimensional structure. J Comput Aided Mol Des 8:243-256.
    • (1994) J Comput Aided Mol Des , vol.8 , pp. 243-256
    • Böhm, H.J.1
  • 6
    • 0032112137 scopus 로고    scopus 로고
    • Prediction of binding constants of protein ligands: A fast method for the prioritization of hits obtained from the de novo design or 3D database search programs
    • Böhm HJ (1998) Prediction of binding constants of protein ligands: A fast method for the prioritization of hits obtained from the de novo design or 3D database search programs. J Comput Aided Mol Des 12:309-323.
    • (1998) J Comput Aided Mol Des , vol.12 , pp. 309-323
    • Böhm, H.J.1
  • 8
    • 0037169532 scopus 로고    scopus 로고
    • A receptor β2 Tyr97 and Leu99 line the GABA-binding site: Insights into mechanisms of agonist and antagonist actions
    • A receptor β2 Tyr97 and Leu99 line the GABA-binding site: Insights into mechanisms of agonist and antagonist actions. J Biol Chem 277:2931-2937.
    • (2002) J Biol Chem , vol.277 , pp. 2931-2937
    • Boileau, A.J.1    Newell, J.G.2    Czajkowski, C.3
  • 9
    • 0033669727 scopus 로고    scopus 로고
    • Correlation of the apparent affinities and efficacies of γ-aminobutyric acidC receptor agonists
    • Chang Y, Covey DF, and Weiss DS (2000) Correlation of the apparent affinities and efficacies of γ-aminobutyric acidC receptor agonists. Mol Pharmacol 58:1375-1380.
    • (2000) Mol Pharmacol , vol.58 , pp. 1375-1380
    • Chang, Y.1    Covey, D.F.2    Weiss, D.S.3
  • 10
    • 0029664746 scopus 로고    scopus 로고
    • Stoichiometry of a recombinant GABAA receptor
    • Chang Y, Wang R, Barot S, and Weiss DS (1996) Stoichiometry of a recombinant GABAA receptor. J Neurosci 16:5415-5424.
    • (1996) J Neurosci , vol.16 , pp. 5415-5424
    • Chang, Y.1    Wang, R.2    Barot, S.3    Weiss, D.S.4
  • 12
    • 0021691416 scopus 로고
    • Bicuculline-insensitive GABA receptors: Studies on the binding of ( -)-baclofen to rat cerebellar membranes
    • Drew CA, Johnston GA, and Weatherby RP (1984) Bicuculline-insensitive GABA receptors: studies on the binding of ( -)-baclofen to rat cerebellar membranes. Neurosci Lett 52:317-321.
    • (1984) Neurosci Lett , vol.52 , pp. 317-321
    • Drew, C.A.1    Johnston, G.A.2    Weatherby, R.P.3
  • 14
    • 0039012103 scopus 로고    scopus 로고
    • Reduced dimensionality in ligand-protein structure prediction: Covalent inhibitors of serine proteases and design of site-directed combinatorial libraries
    • Rational Drug Design: Novel Methodology and Practical Applications (, Parrill L and Rami Reddy M eds) pp, American Chemical Society, Washington, DC
    • Gehlhaar D, Bouzida D and Rejto P (1999) Reduced dimensionality in ligand-protein structure prediction: covalent inhibitors of serine proteases and design of site-directed combinatorial libraries, in Rational Drug Design: Novel Methodology and Practical Applications (ACS Symposium Series) (Parrill L and Rami Reddy M eds) pp 292-311, American Chemical Society, Washington, DC.
    • (1999) ACS Symposium Series , pp. 292-311
    • Gehlhaar, D.1    Bouzida, D.2    Rejto, P.3
  • 15
    • 0029294584 scopus 로고
    • Molecular recognition of the inhibitor AG-1343 by HIV-1 protease: Conformationally flexible docking by evolutionary programming
    • Gehlhaar DK, Verkhivker GM, Rejto PA, Sherman CJ, Fogel DB, Fogel LJ, and Freer ST (1995) Molecular recognition of the inhibitor AG-1343 by HIV-1 protease: conformationally flexible docking by evolutionary programming. Chem Biol 2:317-324.
    • (1995) Chem Biol , vol.2 , pp. 317-324
    • Gehlhaar, D.K.1    Verkhivker, G.M.2    Rejto, P.A.3    Sherman, C.J.4    Fogel, D.B.5    Fogel, L.J.6    Freer, S.T.7
  • 17
    • 0037166316 scopus 로고    scopus 로고
    • A receptor α1T60-α1K70 Region mediate GABA and SR-95531 actions
    • A receptor α1T60-α1K70 Region mediate GABA and SR-95531 actions. J Biol Chem 277:18785-18792.
    • (2002) J Biol Chem , vol.277 , pp. 18785-18792
    • Holden, J.H.1    Czajkowski, C.2
  • 18
    • 52949094365 scopus 로고    scopus 로고
    • A receptor that undergoes distinct conformational rearrangements during ligand binding and allosteric modulation. Soc Neurosci Abstr 29:50.10.
    • A receptor that undergoes distinct conformational rearrangements during ligand binding and allosteric modulation. Soc Neurosci Abstr 29:50.10.
  • 19
    • 0030255303 scopus 로고    scopus 로고
    • Scoring noncovalent protein-ligand interactions: A continuous differentiable function tuned to compute binding affinities
    • Jain AN (1996) Scoring noncovalent protein-ligand interactions: A continuous differentiable function tuned to compute binding affinities. J Comput Aided Mol Des 10:427-440.
    • (1996) J Comput Aided Mol Des , vol.10 , pp. 427-440
    • Jain, A.N.1
  • 20
    • 0030222776 scopus 로고    scopus 로고
    • C receptors: Relatively simple transmitter-gated ion channels?
    • C receptors: relatively simple transmitter-gated ion channels? Trends Pharmacol Sci 17:319-323.
    • (1996) Trends Pharmacol Sci , vol.17 , pp. 319-323
    • Johnston, G.A.1
  • 23
    • 25144465496 scopus 로고    scopus 로고
    • C Receptor. Chem Biol 12:993-997.
    • C Receptor. Chem Biol 12:993-997.
  • 24
    • 0033545622 scopus 로고    scopus 로고
    • A general and fast scoring function for protein-ligand interactions: A simplified potential approach
    • Muegge I and Martin YC (1999) A general and fast scoring function for protein-ligand interactions: a simplified potential approach. J Med Chem 42:791-804.
    • (1999) J Med Chem , vol.42 , pp. 791-804
    • Muegge, I.1    Martin, Y.C.2
  • 26
    • 0037969585 scopus 로고    scopus 로고
    • 191 segment is involved in GABA binding and channel gating
    • 191 segment is involved in GABA binding and channel gating. J Biol Chem 278:13166-13172.
    • (2003) J Biol Chem , vol.278 , pp. 13166-13172
    • Newell, J.G.1    Czajkowski, C.2
  • 27
    • 10644270878 scopus 로고    scopus 로고
    • A receptor β2 subunit produces a spontaneously open channel: A trigger for channel activation
    • A receptor β2 subunit produces a spontaneously open channel: a trigger for channel activation. J Neurosci 24:11226-11235.
    • (2004) J Neurosci , vol.24 , pp. 11226-11235
    • Newell, J.G.1    McDevitt, R.A.2    Czajkowski, C.3
  • 28
    • 0029859986 scopus 로고    scopus 로고
    • Design and in vitro pharmacology of a selective γ-aminobutyric acid C receptor antagonist
    • Ragozzino D, Woodward RM, Murata Y, Eusebi F, Overman LE, and Miledi R (1996) Design and in vitro pharmacology of a selective γ-aminobutyric acid C receptor antagonist. Mol Pharmacol 50:1024-1030.
    • (1996) Mol Pharmacol , vol.50 , pp. 1024-1030
    • Ragozzino, D.1    Woodward, R.M.2    Murata, Y.3    Eusebi, F.4    Overman, L.E.5    Miledi, R.6
  • 29
    • 0027136282 scopus 로고
    • Comparative protein modeling by satisfaction of spatial restraints
    • Sali A and Blundell TL (1993) Comparative protein modeling by satisfaction of spatial restraints. J Mol Biol 234:779-815.
    • (1993) J Mol Biol , vol.234 , pp. 779-815
    • Sali, A.1    Blundell, T.L.2
  • 32
    • 0028170429 scopus 로고
    • 3H]muscimol photoaffinity substrate in the bovine γ-aminobutyric acidA receptor α subunit
    • 3H]muscimol photoaffinity substrate in the bovine γ-aminobutyric acidA receptor α subunit. J Biol Chem 269:20380-20387.
    • (1994) J Biol Chem , vol.269 , pp. 20380-20387
    • Smith, G.B.1    Olsen, R.W.2
  • 33
    • 0037212102 scopus 로고    scopus 로고
    • LigandFit: A novel method for the shape-directed rapid docking of ligands to protein active sites
    • Venkatachalam CM, Jiang X, Oldfield T, and Waldman M (2003) LigandFit: a novel method for the shape-directed rapid docking of ligands to protein active sites. J Mol Graph Model 21:289-307.
    • (2003) J Mol Graph Model , vol.21 , pp. 289-307
    • Venkatachalam, C.M.1    Jiang, X.2    Oldfield, T.3    Waldman, M.4
  • 36
    • 0002923248 scopus 로고    scopus 로고
    • Pharmacological subtypes of GABAA receptors based on subunit composition
    • Martin D and Olsen R eds pp, Lippincott Williams & Wilkins, Philadelphia
    • Whiting P, Wafford K and McKernan R (2000) Pharmacological subtypes of GABAA receptors based on subunit composition, in GABA in the Nervous System: The View at Fifty Years (Martin D and Olsen R eds) pp 113-126, Lippincott Williams & Wilkins, Philadelphia.
    • (2000) GABA in the Nervous System: The View at Fifty Years , pp. 113-126
    • Whiting, P.1    Wafford, K.2    McKernan, R.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.