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Volumn 473, Issue 6, 2016, Pages 779-787

A negative allosteric modulator modulates GABAB -receptor signalling through GB2 subunits

Author keywords

Cerebellar granular neurons; GabaB receptor; Heptahelical domain; Negative allosteric modulator.

Indexed keywords

2,6 DI TERT BUTYL 4 (3 HYDROXY 2,2 DIMETHYLPROPYL)PHENOL; 4 AMINOBUTYRIC ACID B RECEPTOR; 4 AMINOBUTYRIC ACID RECEPTOR STIMULATING AGENT; BACLOFEN; CLH 304A; CLH 391; CLH 393; GUANINE NUCLEOTIDE BINDING PROTEIN; MITOGEN ACTIVATED PROTEIN KINASE 1; PROTEIN KINASE B; UNCLASSIFIED DRUG; CLH304A; OXOACID; PHENOL DERIVATIVE; PROTEIN SUBUNIT;

EID: 84975311440     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20150979     Document Type: Article
Times cited : (20)

References (47)
  • 2
    • 0019395276 scopus 로고
    • B sites in rat brain
    • Hill, D.R. and Bowery, N.G. (1981) 3H-Baclofen and 3H-GABA bind to bicuculline-insensitive GABAB sites in rat brain. Nature 290, 149-152
    • (1981) Nature , vol.290 , pp. 149-152
    • Hill, D.R.1    Bowery, N.G.2
  • 3
    • 0035125654 scopus 로고    scopus 로고
    • B receptor autoradiography in hippocampal sclerosis associated with human temporal lobe epilepsy
    • Billinton, A., Baird, V.H., Thom, M., Duncan, J.S., Upton, N. and Bowery, N.G. (2001) GABAB receptor autoradiography in hippocampal sclerosis associated with human temporal lobe epilepsy. Br. J. Pharmacol. 132, 475-480
    • (2001) Br. J. Pharmacol. , vol.132 , pp. 475-480
    • Billinton, A.1    Baird, V.H.2    Thom, M.3    Duncan, J.S.4    Upton, N.5    Bowery, N.G.6
  • 4
    • 0024472082 scopus 로고
    • GABAB receptors and their significance in mammalian pharmacology
    • Bowery, N.G. (1989) GABAB receptors and their significance in mammalian pharmacology. Trends Pharmacol. Sci. 10, 401-407
    • (1989) Trends Pharmacol. Sci , vol.10 , pp. 401-407
    • Bowery, N.G.1
  • 6
    • 14944359484 scopus 로고    scopus 로고
    • Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits
    • Mombereau, C., Kaupmann, K., Gassmann, M., Bettler, B., van der Putten, H. and Cryan, J.F. (2005) Altered anxiety and depression-related behaviour in mice lacking GABAB(2) receptor subunits. NeuroReport 16, 307-310
    • (2005) NeuroReport , vol.16 , pp. 307-310
    • Mombereau, C.1    Kaupmann, K.2    Gassmann, M.3    Bettler, B.4    Van Der Putten, H.5    Cryan, J.F.6
  • 7
    • 84862068720 scopus 로고    scopus 로고
    • Regulation of neuronal GABAB receptor functions by subunit composition
    • Gassmann, M. and Bettler, B. (2012) Regulation of neuronal GABAB receptor functions by subunit composition. Nat. Rev. Neurosci. 13, 380-394
    • (2012) Nat. Rev. Neurosci. , vol.13 , pp. 380-394
    • Gassmann, M.1    Bettler, B.2
  • 8
    • 30844468174 scopus 로고    scopus 로고
    • GABAB receptor: A site of therapeutic benefit
    • Bowery, N.G. (2006) GABAB receptor: a site of therapeutic benefit. Curr. Opin. Pharmacol. 6, 37-43
    • (2006) Curr. Opin. Pharmacol. , vol.6 , pp. 37-43
    • Bowery, N.G.1
  • 9
    • 77955068362 scopus 로고    scopus 로고
    • Chemistry and pharmacology of GABAB receptor ligands
    • Froestl, W. (2010) Chemistry and pharmacology of GABAB receptor ligands. Adv. Pharmacol. 58, 19-62
    • (2010) Adv. Pharmacol. , vol.58 , pp. 19-62
    • Froestl, W.1
  • 14
    • 84890434896 scopus 로고    scopus 로고
    • B receptor
    • Geng, Y., Bush, M., Mosyak, L., Wang, F. and Fan, Q.R. (2013) Structural mechanism of ligand activation in human GABAB receptor. Nature 504, 254-259
    • (2013) Nature , vol.504 , pp. 254-259
    • Geng, Y.1    Bush, M.2    Mosyak, L.3    Wang, F.4    Fan, Q.R.5
  • 17
    • 77955273299 scopus 로고    scopus 로고
    • 2+ channel and GABAB receptor subunit 2
    • Park, H.W., Jung, H., Choi, K.H., Baik, J.H. and Rhim, H. (2010) Direct interaction and functional coupling between voltage-gated CaV1.3 Ca2+ channel and GABAB receptor subunit 2. FEBS Lett. 584, 3317-3322
    • (2010) FEBS Lett. , vol.584 , pp. 3317-3322
    • Park, H.W.1    Jung, H.2    Choi, K.H.3    Baik, J.H.4    Rhim, H.5
  • 19
    • 34447621270 scopus 로고    scopus 로고
    • Dominant role of GABAB2 and Gbetagamma for GABAB receptor-mediated-ERK1/2/CREB pathway in cerebellar neurons
    • Tu, H., Rondard, P., Xu, C., Bertaso, F., Cao, F., Zhang, X., Pin, J.P. and Liu, J. (2007) Dominant role of GABAB2 and Gbetagamma for GABAB receptor-mediated-ERK1/2/CREB pathway in cerebellar neurons. Cell Signal. 19, 1996-2002
    • (2007) Cell Signal , vol.19 , pp. 1996-2002
    • Tu, H.1    Rondard, P.2    Xu, C.3    Bertaso, F.4    Cao, F.5    Zhang, X.6    Pin, J.P.7    Liu, J.8
  • 20
    • 74949134498 scopus 로고    scopus 로고
    • GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation
    • Tu, H., Xu, C., Zhang, W., Liu, Q., Rondard, P., Pin, J. P. and Liu, J. (2010) GABAB receptor activation protects neurons from apoptosis via IGF-1 receptor transactivation. J. Neurosci. 30, 749-759
    • (2010) J. Neurosci. , vol.30 , pp. 749-759
    • Tu, H.1    Xu, C.2    Zhang, W.3    Liu, Q.4    Rondard, P.5    Pin, J.P.6    Liu, J.7
  • 21
    • 0034760504 scopus 로고    scopus 로고
    • Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501
    • Urwyler, S., Mosbacher, J., Lingenhoehl, K., Heid, J., Hofstetter, K., Froestl, W., Bettler, B. and Kaupmann, K. (2001) Positive allosteric modulation of native and recombinant gamma-aminobutyric acid(B) receptors by 2,6-di-tert-butyl-4-(3-hydroxy-2,2-dimethyl-propyl)-phenol (CGP7930) and its aldehyde analog CGP13501. Mol. Pharmacol. 60, 963-971
    • (2001) Mol. Pharmacol. , vol.60 , pp. 963-971
    • Urwyler, S.1    Mosbacher, J.2    Lingenhoehl, K.3    Heid, J.4    Hofstetter, K.5    Froestl, W.6    Bettler, B.7    Kaupmann, K.8
  • 22
    • 0141742370 scopus 로고    scopus 로고
    • N,N′ Dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine (GS39783) and structurally related compounds: Novel allosteric enhancers of gamma-aminobutyric acidB receptor function
    • Urwyler, S., Pozza, M.F., Lingenhoehl, K., Mosbacher, J., Lampert, C., Froestl, W., Koller, M. and Kaupmann, K. (2003) N,N′ -Dicyclopentyl-2-methylsulfanyl-5-nitropyrimidine-4,6-diamine (GS39783) and structurally related compounds: novel allosteric enhancers of gamma-aminobutyric acidB receptor function. J. Pharmacol. Exp. Ther. 307, 322-330
    • (2003) J. Pharmacol. Exp. Ther. , vol.307 , pp. 322-330
    • Urwyler, S.1    Pozza, M.F.2    Lingenhoehl, K.3    Mosbacher, J.4    Lampert, C.5    Froestl, W.6    Koller, M.7    Kaupmann, K.8
  • 24
    • 35148824487 scopus 로고    scopus 로고
    • Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors
    • Guery, S., Floersheim, P., Kaupmann, K. and Froestl, W. (2007) Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors. Bioorg. Med. Chem. Lett. 17, 6206-6211
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 6206-6211
    • Guery, S.1    Floersheim, P.2    Kaupmann, K.3    Froestl, W.4
  • 25
    • 33751082960 scopus 로고    scopus 로고
    • Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N′ dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit
    • Dupuis, D.S., Relkovic, D., Lhuillier, L., Mosbacher, J. and Kaupmann, K. (2006) Point mutations in the transmembrane region of GABAB2 facilitate activation by the positive modulator N,N′ -dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine (GS39783) in the absence of the GABAB1 subunit. Mol. Pharmacol. 70, 2027-2036
    • (2006) Mol. Pharmacol. , vol.70 , pp. 2027-2036
    • Dupuis, D.S.1    Relkovic, D.2    Lhuillier, L.3    Mosbacher, J.4    Kaupmann, K.5
  • 26
    • 3142685557 scopus 로고    scopus 로고
    • B receptor
    • Binet, V., Brajon, C., Le Corre, L., Acher, F., Pin, J.P. and Prezeau, L. (2004) The heptahelical domain of GABAB2 is activated directly by CGP7930, a positive allosteric modulator of the GABAB receptor. J. Biol. Chem. 279, 29085-29091
    • (2004) . Biol. Chem. , vol.279 , pp. 29085-29091
    • Binet, V.1    Brajon, C.2    Le Corre, L.3    Acher, F.4    Pin, J.P.5    Prezeau, L.6
  • 28
    • 0001014261 scopus 로고
    • Synthesis of γ aminopropylphosphonous acids using hypophosphorus acid synthons
    • Dingwall, J.G., Ehrenfreund, J., Hall, R.G. and Jack, J. (1987a) Synthesis of γ -aminopropylphosphonous acids using hypophosphorus acid synthons. Phosphorus Sulfur 30, 571-575
    • (1987) Phosphorus Sulfur , vol.30 , pp. 571-575
    • Dingwall, J.G.1    Ehrenfreund, J.2    Hall, R.G.3    Jack, J.4
  • 29
    • 84975246628 scopus 로고
    • Substituted propane-phosphonous acid compounds
    • United States Patent
    • Dingwall, J.G., Ehrenfreund, J., Hall, R.G. and Jack, J. (1987b) Substituted propane-phosphonous acid compounds. Chem. Abst. 106, 18814 (United States Patent No. 4,656,298)
    • (1987) Chem. Abst. , vol.106 , pp. 18814
    • Dingwall, J.G.1    Ehrenfreund, J.2    Hall, R.G.3    Jack, J.4
  • 30
    • 0031713304 scopus 로고    scopus 로고
    • Comparative effect of L-CCG-I, DCG-IV and gamma-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypes
    • Brabet, I., Parmentier, M.L., De Colle, C., Bockaert, J., Acher, F. and Pin, J.P. (1998) Comparative effect of L-CCG-I, DCG-IV and gamma-carboxy-L-glutamate on all cloned metabotropic glutamate receptor subtypes. Neuropharmacology 37, 1043-1051
    • (1998) Neuropharmacology , vol.37 , pp. 1043-1051
    • Brabet, I.1    Parmentier, M.L.2    De Colle, C.3    Bockaert, J.4    Acher, F.5    Pin, J.P.6
  • 31
    • 0032846317 scopus 로고    scopus 로고
    • The heteromeric GABA-B receptor recognizes G-protein alpha subunit C-termini
    • Franek, M., Pagano, A., Kaupmann, K., Bettler, B., Pin, J.P. and Blahos, J. (1999) The heteromeric GABA-B receptor recognizes G-protein alpha subunit C-termini. Neuropharmacology 38, 1657-1666
    • (1999) Neuropharmacology , vol.38 , pp. 1657-1666
    • Franek, M.1    Pagano, A.2    Kaupmann, K.3    Bettler, B.4    Pin, J.P.5    Blahos, J.6
  • 32
    • 84919704267 scopus 로고    scopus 로고
    • Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer
    • Xue, L., Rovira, X., Scholler, P., Zhao, H., Liu, J., Pin, J. P. and Rondard, P. (2015) Major ligand-induced rearrangement of the heptahelical domain interface in a GPCR dimer. Nat. Chem. Biol. 11, 134-140
    • (2015) Nat. Chem. Biol. , vol.11 , pp. 134-140
    • Xue, L.1    Rovira, X.2    Scholler, P.3    Zhao, H.4    Liu, J.5    Pin, J.P.6    Rondard, P.7
  • 33
    • 84932136451 scopus 로고    scopus 로고
    • A GPCR promotes its own surface expression by recruiting a Rap1-dependent signaling cascade
    • Zhang, Z., Zhang, W., Huang, S., Sun, Q., Wang, Y., Hu, Y., Sun, N., Zhang, Y., Jiang, Z., Minato, N. et al. (2015) A GPCR promotes its own surface expression by recruiting a Rap1-dependent signaling cascade. J. Cell Sci. 128, 2302-2313
    • (2015) J. Cell Sci. , vol.128 , pp. 2302-2313
    • Zhang, Z.1    Zhang, W.2    Huang, S.3    Sun, Q.4    Wang, Y.5    Hu, Y.6    Sun, N.7    Zhang, Y.8    Jiang, Z.9    Minato, N.10
  • 34
    • 44449096254 scopus 로고    scopus 로고
    • Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: Application to GPCR oligomerization
    • Maurel, D., Comps-Agrar, L., Brock, C., Rives, M.L., Bourrier, E., Ayoub, M.A., Bazin, H., Tinel, N., Durroux, T., Prezeau, L. et al. (2008) Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies: application to GPCR oligomerization. Nat. Methods 5, 561-567
    • (2008) Nat. Methods , vol.5 , pp. 561-567
    • Maurel, D.1    Comps-Agrar, L.2    Brock, C.3    Rives, M.L.4    Bourrier, E.5    Ayoub, M.A.6    Bazin, H.7    Tinel, N.8    Durroux, T.9    Prezeau, L.10
  • 35
    • 0032969936 scopus 로고    scopus 로고
    • A multi-well filtration assay for quantitation of inositol phosphates in biological samples
    • Chengalvala, M., Kostek, B. and Frail, D.E. (1999) A multi-well filtration assay for quantitation of inositol phosphates in biological samples. J. Biochem. Biophys. Methods 38, 163-170
    • (1999) J. Biochem. Biophys. Methods , vol.38 , pp. 163-170
    • Chengalvala, M.1    Kostek, B.2    Frail, D.E.3
  • 37
    • 18044396542 scopus 로고    scopus 로고
    • GABAB receptor antagonist SGS742 improves spatial memory and reduces protein binding to the cAMP response element (CRE) in the hippocampus
    • Helm, K.A., Haberman, R.P., Dean, S.L., Hoyt, E.C., Melcher, T., Lund, P.K. and Gallagher, M. (2005) GABAB receptor antagonist SGS742 improves spatial memory and reduces protein binding to the cAMP response element (CRE) in the hippocampus. Neuropharmacology 48, 956-964
    • (2005) Neuropharmacology , vol.48 , pp. 956-964
    • Helm, K.A.1    Haberman, R.P.2    Dean, S.L.3    Hoyt, E.C.4    Melcher, T.5    Lund, P.K.6    Gallagher, M.7
  • 38
    • 33846846369 scopus 로고    scopus 로고
    • Behavioral evaluation of mice deficient in GABAB1 receptor isoforms in tests of unconditioned anxiety
    • Jacobson, L.H., Bettler, B., Kaupmann, K. and Cryan, J.F. (2007) Behavioral evaluation of mice deficient in GABAB1 receptor isoforms in tests of unconditioned anxiety. Psychopharmacology (Berl.) 190, 541-553
    • (2007) Psychopharmacology (Berl. ) , vol.190 , pp. 541-553
    • Jacobson, L.H.1    Bettler, B.2    Kaupmann, K.3    Cryan, J.F.4
  • 39
    • 84880416279 scopus 로고    scopus 로고
    • Baclofen and other GABAB receptor agents are allosteric modulators of the CXCL12 chemokine receptor CXCR4
    • Guyon, A., Kussrow, A., Olmsted, I.R., Sandoz, G., Bornhop, D.J. and Nahon, J.L. (2013) Baclofen and other GABAB receptor agents are allosteric modulators of the CXCL12 chemokine receptor CXCR4. J. Neurosci. 33, 11643-11654
    • (2013) J. Neurosci. , vol.33 , pp. 11643-11654
    • Guyon, A.1    Kussrow, A.2    Olmsted, I.R.3    Sandoz, G.4    Bornhop, D.J.5    Nahon, J.L.6
  • 40
    • 78149496159 scopus 로고    scopus 로고
    • Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
    • Keov, P., Sexton, P.M. and Christopoulos, A. (2011) Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology 60, 24-35
    • (2011) Neuropharmacology , vol.60 , pp. 24-35
    • Keov, P.1    Sexton, P.M.2    Christopoulos, A.3
  • 43
    • 78650920787 scopus 로고    scopus 로고
    • Trans-activation between 7TM domains: Implication in heterodimeric GABAB receptor activation
    • Monnier, C., Tu, H., Bourrier, E., Vol, C., Lamarque, L., Trinquet, E., Pin, J.P. and Rondard, P. (2011) Trans-activation between 7TM domains: implication in heterodimeric GABAB receptor activation. EMBO J. 30, 32-42
    • (2011) EMBO J , vol.30 , pp. 32-42
    • Monnier, C.1    Tu, H.2    Bourrier, E.3    Vol, C.4    Lamarque, L.5    Trinquet, E.6    Pin, J.P.7    Rondard, P.8
  • 45
    • 8844263762 scopus 로고    scopus 로고
    • Positive and negative allosteric modulation of metabotropic glutamate receptors: Emerging therapeutic potential
    • Kew, J.N. (2004) Positive and negative allosteric modulation of metabotropic glutamate receptors: emerging therapeutic potential. Pharmacol. Ther. 104, 233-244
    • (2004) Pharmacol. Ther. , vol.104 , pp. 233-244
    • Kew, J.N.1
  • 47
    • 1942469528 scopus 로고    scopus 로고
    • Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit
    • Liu, J., Maurel, D., Etzol, S., Brabet, I., Ansanay, H., Pin, J.P. and Rondard, P. (2004) Molecular determinants involved in the allosteric control of agonist affinity in the GABAB receptor by the GABAB2 subunit. J. Biol. Chem. 279, 15824-15830
    • (2004) J. Biol. Chem. , vol.279 , pp. 15824-15830
    • Liu, J.1    Maurel, D.2    Etzol, S.3    Brabet, I.4    Ansanay, H.5    Pin, J.P.6    Rondard, P.7


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