메뉴 건너뛰기




Volumn 39, Issue 10, 2014, Pages 1862-1875

mGluR5: Exploration of Orthosteric and Allosteric Ligand Binding Pockets and Their Applications to Drug Discovery

Author keywords

Allosteric; Homology modelling; Ligand recognition; Metabotropic glutamate receptor subtype 5; Mutagenesis; Orthosteric

Indexed keywords

ARGININE; ASPARAGINE; GLUTAMIC ACID; GLUTAMINE; LYSINE; MAVOGLURANT; METABOTROPIC RECEPTOR 1; METABOTROPIC RECEPTOR 2; METABOTROPIC RECEPTOR 3; METABOTROPIC RECEPTOR 4; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR 6; METABOTROPIC RECEPTOR 7; METABOTROPIC RECEPTOR 8; QUISQUALIC ACID; LIGAND;

EID: 84918777709     PISSN: 03643190     EISSN: 15736903     Source Type: Journal    
DOI: 10.1007/s11064-014-1248-8     Document Type: Review
Times cited : (27)

References (92)
  • 2
    • 0022516186 scopus 로고
    • The activation of inositol phospholipid metabolism as a signal-transducing system for excitatory amino acids in primary cultures of cerebellar granule cells
    • PID: 3016212, COI: 1:CAS:528:DyaL28XltV2hsLw%3D
    • Nicoletti F, Wroblewski JT, Novelli A, Alho H, Guidotti A, Costa E (1986) The activation of inositol phospholipid metabolism as a signal-transducing system for excitatory amino acids in primary cultures of cerebellar granule cells. J Neurosci 6:1905–1911
    • (1986) J Neurosci , vol.6 , pp. 1905-1911
    • Nicoletti, F.1    Wroblewski, J.T.2    Novelli, A.3    Alho, H.4    Guidotti, A.5    Costa, E.6
  • 3
    • 0023092256 scopus 로고
    • A new type of glutamate receptor linked to inositol phospholipid metabolism
    • PID: 2880300, COI: 1:CAS:528:DyaL2sXhtFCisr4%3D
    • Sugiyama H, Ito I, Hirono C (1987) A new type of glutamate receptor linked to inositol phospholipid metabolism. Nature 325:531–533
    • (1987) Nature , vol.325 , pp. 531-533
    • Sugiyama, H.1    Ito, I.2    Hirono, C.3
  • 5
    • 0026093312 scopus 로고
    • Sequence and expression of a metabotropic glutamate receptor
    • PID: 1847995, COI: 1:CAS:528:DyaK3MXltVOntrs%3D
    • Masu M, Tanabe Y, Tsuchida K, Shigemoto R, Nakanishi S (1991) Sequence and expression of a metabotropic glutamate receptor. Nature 349:760–765
    • (1991) Nature , vol.349 , pp. 760-765
    • Masu, M.1    Tanabe, Y.2    Tsuchida, K.3    Shigemoto, R.4    Nakanishi, S.5
  • 6
    • 0032834028 scopus 로고    scopus 로고
    • Pharmacological agents acting at subtypes of metabotropic glutamate receptors
    • PID: 10530808, COI: 1:CAS:528:DyaK1MXlvVWnsLc%3D
    • Schoepp DD, Jane DE, Monn JA (1999) Pharmacological agents acting at subtypes of metabotropic glutamate receptors. Neuropharmacology 38:1431–1476
    • (1999) Neuropharmacology , vol.38 , pp. 1431-1476
    • Schoepp, D.D.1    Jane, D.E.2    Monn, J.A.3
  • 7
    • 33845973375 scopus 로고    scopus 로고
    • Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors
    • PID: 17266540
    • Bräuner-Osborne H, Wellendorph P, Jensen AA (2007) Structure, pharmacology and therapeutic prospects of family C G-protein coupled receptors. Curr Drug Targets 8:169–184
    • (2007) Curr Drug Targets , vol.8 , pp. 169-184
    • Bräuner-Osborne, H.1    Wellendorph, P.2    Jensen, A.A.3
  • 8
    • 0030995878 scopus 로고    scopus 로고
    • Pharmacology and functions of metabotropic glutamate receptors
    • PID: 9131252, COI: 1:CAS:528:DyaK2sXisl2ktr0%3D
    • Conn PJ, Pin JP (1997) Pharmacology and functions of metabotropic glutamate receptors. Annu Rev Pharmacol Toxicol 37:205–237
    • (1997) Annu Rev Pharmacol Toxicol , vol.37 , pp. 205-237
    • Conn, P.J.1    Pin, J.P.2
  • 9
    • 78149495647 scopus 로고    scopus 로고
    • Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential
    • PID: 20637216, COI: 1:CAS:528:DC%2BC3cXhsVaitLzE
    • Gregory KJ, Dong EN, Meiler J, Conn PJ (2011) Allosteric modulation of metabotropic glutamate receptors: structural insights and therapeutic potential. Neuropharmacology 60:66–81
    • (2011) Neuropharmacology , vol.60 , pp. 66-81
    • Gregory, K.J.1    Dong, E.N.2    Meiler, J.3    Conn, P.J.4
  • 10
    • 0026437728 scopus 로고
    • Molecular diversity of glutamate receptors and implications for brain function
    • PID: 1329206, COI: 1:CAS:528:DyaK38Xmt1Knsbw%3D
    • Nakanishi S (1992) Molecular diversity of glutamate receptors and implications for brain function. Science 258:597–603
    • (1992) Science , vol.258 , pp. 597-603
    • Nakanishi, S.1
  • 11
    • 77949516412 scopus 로고    scopus 로고
    • Metabotropic glutamate receptors: physiology, pharmacology, and disease
    • PID: 20055706, COI: 1:CAS:528:DC%2BC3cXisVelurg%3D
    • Niswender CM, Conn PJ (2010) Metabotropic glutamate receptors: physiology, pharmacology, and disease. Annu Rev Pharmacol Toxicol 50:295–322
    • (2010) Annu Rev Pharmacol Toxicol , vol.50 , pp. 295-322
    • Niswender, C.M.1    Conn, P.J.2
  • 12
    • 0038662595 scopus 로고    scopus 로고
    • Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors
    • PID: 12782243, COI: 1:CAS:528:DC%2BD3sXktVOqsb8%3D
    • Pin JP, Galvez T, Prezeau L (2003) Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors. Pharmacol Ther 98:325–354
    • (2003) Pharmacol Ther , vol.98 , pp. 325-354
    • Pin, J.P.1    Galvez, T.2    Prezeau, L.3
  • 13
    • 66249144426 scopus 로고    scopus 로고
    • The structure and function of G-protein-coupled receptors
    • PID: 19458711, COI: 1:CAS:528:DC%2BD1MXmtFKmsLg%3D
    • Rosenbaum DM, Rasmussen SG, Kobilka BK (2009) The structure and function of G-protein-coupled receptors. Nature 459:356–363
    • (2009) Nature , vol.459 , pp. 356-363
    • Rosenbaum, D.M.1    Rasmussen, S.G.2    Kobilka, B.K.3
  • 14
    • 0038024615 scopus 로고    scopus 로고
    • The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints
    • PID: 12761335, COI: 1:CAS:528:DC%2BD3sXkt1Shu7k%3D
    • Fredriksson R, Lagerstrom MC, Lundin LG, Schioth HB (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 63:1256–1272
    • (2003) Mol Pharmacol , vol.63 , pp. 1256-1272
    • Fredriksson, R.1    Lagerstrom, M.C.2    Lundin, L.G.3    Schioth, H.B.4
  • 15
    • 0028338534 scopus 로고
    • GCRDb: a G-protein-coupled receptor database
    • PID: 8081729, COI: 1:CAS:528:DyaK2cXlslyktLw%3D
    • Kolakowski LF Jr (1994) GCRDb: a G-protein-coupled receptor database. Recept Channels 2:1–7
    • (1994) Recept Channels , vol.2 , pp. 1-7
    • Kolakowski, L.F.1
  • 16
    • 84875192840 scopus 로고    scopus 로고
    • mGlu5 negative allosteric modulators: a patent review (2010-2012)
    • PID: 23339457, COI: 1:CAS:528:DC%2BC3sXjvFWmtb4%3D
    • Emmitte KA (2013) mGlu5 negative allosteric modulators: a patent review (2010-2012). Expert Opin Ther Pat 23:393–408
    • (2013) Expert Opin Ther Pat , vol.23 , pp. 393-408
    • Emmitte, K.A.1
  • 17
    • 67650628028 scopus 로고    scopus 로고
    • Molecular basis for amino acid sensing by family C G-protein-coupled receptors
    • PID: 19298394, COI: 1:CAS:528:DC%2BD1MXlt1Oqsrs%3D
    • Wellendorph P, Bräuner-Osborne H (2009) Molecular basis for amino acid sensing by family C G-protein-coupled receptors. Br J Pharmacol 156:869–884
    • (2009) Br J Pharmacol , vol.156 , pp. 869-884
    • Wellendorph, P.1    Bräuner-Osborne, H.2
  • 19
    • 79251591614 scopus 로고    scopus 로고
    • A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors
    • PID: 20826542, COI: 1:CAS:528:DC%2BC3MXls1Gntg%3D%3D
    • Doumazane E, Scholler P, Zwier JM, Trinquet E, Rondard P, Pin JP (2011) A new approach to analyze cell surface protein complexes reveals specific heterodimeric metabotropic glutamate receptors. FASEB J 25:66–77
    • (2011) FASEB J , vol.25 , pp. 66-77
    • Doumazane, E.1    Scholler, P.2    Zwier, J.M.3    Trinquet, E.4    Rondard, P.5    Pin, J.P.6
  • 23
    • 0037022586 scopus 로고    scopus 로고
    • Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd3+
    • PID: 11867751, COI: 1:CAS:528:DC%2BD38Xit1Crsbo%3D
    • Tsuchiya D, Kunishima N, Kamiya N, Jingami H, Morikawa K (2002) Structural views of the ligand-binding cores of a metabotropic glutamate receptor complexed with an antagonist and both glutamate and Gd3+. Proc Natl Acad Sci U S A 99:2660–2665
    • (2002) Proc Natl Acad Sci U S A , vol.99 , pp. 2660-2665
    • Tsuchiya, D.1    Kunishima, N.2    Kamiya, N.3    Jingami, H.4    Morikawa, K.5
  • 25
    • 34247210665 scopus 로고    scopus 로고
    • Structures of the extracellular regions of the group II/III metabotropic glutamate receptors
    • PID: 17360426, COI: 1:CAS:528:DC%2BD2sXjt1ymsrs%3D
    • Muto T, Tsuchiya D, Morikawa K, Jingami H (2007) Structures of the extracellular regions of the group II/III metabotropic glutamate receptors. Proc Natl Acad Sci U S A 104:3759–3764
    • (2007) Proc Natl Acad Sci U S A , vol.104 , pp. 3759-3764
    • Muto, T.1    Tsuchiya, D.2    Morikawa, K.3    Jingami, H.4
  • 30
    • 84876065856 scopus 로고    scopus 로고
    • Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors
    • PID: 23487753, COI: 1:CAS:528:DC%2BC3sXnsFCmsL8%3D
    • Doumazane E, Scholler P, Fabre L, Zwier JM, Trinquet E, Pin JP, Rondard P (2013) Illuminating the activation mechanisms and allosteric properties of metabotropic glutamate receptors. Proc Natl Acad Sci U S A 110:E1416–E1425
    • (2013) Proc Natl Acad Sci U S A , vol.110 , pp. E1416-E1425
    • Doumazane, E.1    Scholler, P.2    Fabre, L.3    Zwier, J.M.4    Trinquet, E.5    Pin, J.P.6    Rondard, P.7
  • 32
    • 36448988595 scopus 로고    scopus 로고
    • Activation of a dimeric metabotropic glutamate receptor by intersubunit rearrangement
    • PID: 17855348, COI: 1:CAS:528:DC%2BD2sXht1Clur7L
    • Brock C, Oueslati N, Soler S, Boudier L, Rondard P, Pin JP (2007) Activation of a dimeric metabotropic glutamate receptor by intersubunit rearrangement. J Biol Chem 282:33000–33008
    • (2007) J Biol Chem , vol.282 , pp. 33000-33008
    • Brock, C.1    Oueslati, N.2    Soler, S.3    Boudier, L.4    Rondard, P.5    Pin, J.P.6
  • 34
    • 84875972037 scopus 로고    scopus 로고
    • Glutamate acts as a partial inverse agonist to metabotropic glutamate receptor with a single amino acid mutation in the transmembrane domain
    • PID: 23420844, COI: 1:CAS:528:DC%2BC3sXlsVGjtr8%3D
    • Yanagawa M, Yamashita T, Shichida Y (2013) Glutamate acts as a partial inverse agonist to metabotropic glutamate receptor with a single amino acid mutation in the transmembrane domain. J Biol Chem 288:9593–9601
    • (2013) J Biol Chem , vol.288 , pp. 9593-9601
    • Yanagawa, M.1    Yamashita, T.2    Shichida, Y.3
  • 35
    • 79951854466 scopus 로고    scopus 로고
    • Dimers and beyond: the functional puzzles of class C GPCRs
    • PID: 21256155, COI: 1:CAS:528:DC%2BC3MXit1Gmt74%3D
    • Kniazeff J, Prezeau L, Rondard P, Pin JP, Goudet C (2011) Dimers and beyond: the functional puzzles of class C GPCRs. Pharmacol Ther 130:9–25
    • (2011) Pharmacol Ther , vol.130 , pp. 9-25
    • Kniazeff, J.1    Prezeau, L.2    Rondard, P.3    Pin, J.P.4    Goudet, C.5
  • 36
    • 20444362759 scopus 로고    scopus 로고
    • Towards a view of functioning dimeric metabotropic receptors
    • PID: 15922585, COI: 1:CAS:528:DC%2BD2MXlt1Srsrw%3D
    • Kubo Y, Tateyama M (2005) Towards a view of functioning dimeric metabotropic receptors. Curr Opin Neurobiol 15:289–295
    • (2005) Curr Opin Neurobiol , vol.15 , pp. 289-295
    • Kubo, Y.1    Tateyama, M.2
  • 37
    • 78149497839 scopus 로고    scopus 로고
    • The complexity of their activation mechanism opens new possibilities for the modulation of mGlu and GABAB class C G protein-coupled receptors
    • PID: 20713070, COI: 1:CAS:528:DC%2BC3cXhsVaitL3M
    • Rondard P, Goudet C, Kniazeff J, Pin JP, Prezeau L (2011) The complexity of their activation mechanism opens new possibilities for the modulation of mGlu and GABAB class C G protein-coupled receptors. Neuropharmacology 60:82–92
    • (2011) Neuropharmacology , vol.60 , pp. 82-92
    • Rondard, P.1    Goudet, C.2    Kniazeff, J.3    Pin, J.P.4    Prezeau, L.5
  • 39
    • 78149499680 scopus 로고    scopus 로고
    • Exploration of structure-based drug design opportunities for mGluRs
    • PID: 20705075, COI: 1:CAS:528:DC%2BC3cXhsVaitL3N
    • Topiol S, Sabio M, Uberti M (2011) Exploration of structure-based drug design opportunities for mGluRs. Neuropharmacology 60:93–101
    • (2011) Neuropharmacology , vol.60 , pp. 93-101
    • Topiol, S.1    Sabio, M.2    Uberti, M.3
  • 47
    • 65749103258 scopus 로고    scopus 로고
    • Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator
    • PID: 19443216, COI: 1:CAS:528:DC%2BD1MXms1eksbs%3D
    • Ritzen A, Sindet R, Hentzer M, Svendsen N, Brodbeck RM, Bundgaard C (2009) Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator. Bioorg Med Chem Lett 19:3275–3278
    • (2009) Bioorg Med Chem Lett , vol.19 , pp. 3275-3278
    • Ritzen, A.1    Sindet, R.2    Hentzer, M.3    Svendsen, N.4    Brodbeck, R.M.5    Bundgaard, C.6
  • 48
    • 27844482134 scopus 로고    scopus 로고
    • A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators
    • PID: 16155210, COI: 1:CAS:528:DC%2BD2MXht1yktr7M
    • Rodriguez AL, Nong Y, Sekaran NK, Alagille D, Tamagnan GD, Conn PJ (2005) A close structural analog of 2-methyl-6-(phenylethynyl)-pyridine acts as a neutral allosteric site ligand on metabotropic glutamate receptor subtype 5 and blocks the effects of multiple allosteric modulators. Mol Pharmacol 68:1793–1802
    • (2005) Mol Pharmacol , vol.68 , pp. 1793-1802
    • Rodriguez, A.L.1    Nong, Y.2    Sekaran, N.K.3    Alagille, D.4    Tamagnan, G.D.5    Conn, P.J.6
  • 50
    • 40849124248 scopus 로고    scopus 로고
    • N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hy droxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors
    • PID: 18056795, COI: 1:CAS:528:DC%2BD1cXjt1egsLk%3D
    • Chen Y, Goudet C, Pin JP, Conn PJ (2008) N-{4-Chloro-2-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]phenyl}-2-hy droxybenzamide (CPPHA) acts through a novel site as a positive allosteric modulator of group 1 metabotropic glutamate receptors. Mol Pharmacol 73:909–918
    • (2008) Mol Pharmacol , vol.73 , pp. 909-918
    • Chen, Y.1    Goudet, C.2    Pin, J.P.3    Conn, P.J.4
  • 51
    • 34247477329 scopus 로고    scopus 로고
    • Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses
    • PID: 17303702, COI: 1:CAS:528:DC%2BD2sXlslSis7o%3D
    • Chen Y, Nong Y, Goudet C, Hemstapat K, de Paulis T, Pin JP, Conn PJ (2007) Interaction of novel positive allosteric modulators of metabotropic glutamate receptor 5 with the negative allosteric antagonist site is required for potentiation of receptor responses. Mol Pharmacol 71:1389–1398
    • (2007) Mol Pharmacol , vol.71 , pp. 1389-1398
    • Chen, Y.1    Nong, Y.2    Goudet, C.3    Hemstapat, K.4    de Paulis, T.5    Pin, J.P.6    Conn, P.J.7
  • 52
    • 33746484507 scopus 로고    scopus 로고
    • Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP
    • PID: 16805850, COI: 1:CAS:528:DC%2BD28Xot1Omsbw%3D
    • Malherbe P, Kratochwil N, Muhlemann A, Zenner MT, Fischer C, Stahl M, Gerber PR, Jaeschke G, Porter RH (2006) Comparison of the binding pockets of two chemically unrelated allosteric antagonists of the mGlu5 receptor and identification of crucial residues involved in the inverse agonism of MPEP. J Neurochem 98:601–615
    • (2006) J Neurochem , vol.98 , pp. 601-615
    • Malherbe, P.1    Kratochwil, N.2    Muhlemann, A.3    Zenner, M.T.4    Fischer, C.5    Stahl, M.6    Gerber, P.R.7    Jaeschke, G.8    Porter, R.H.9
  • 53
    • 0141569326 scopus 로고    scopus 로고
    • Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine
    • PID: 14500738, COI: 1:CAS:528:DC%2BD3sXnslGrur8%3D
    • Malherbe P, Kratochwil N, Zenner MT, Piussi J, Diener C, Kratzeisen C, Fischer C, Porter RH (2003) Mutational analysis and molecular modeling of the binding pocket of the metabotropic glutamate 5 receptor negative modulator 2-methyl-6-(phenylethynyl)-pyridine. Mol Pharmacol 64:823–832
    • (2003) Mol Pharmacol , vol.64 , pp. 823-832
    • Malherbe, P.1    Kratochwil, N.2    Zenner, M.T.3    Piussi, J.4    Diener, C.5    Kratzeisen, C.6    Fischer, C.7    Porter, R.H.8
  • 54
    • 29344436808 scopus 로고    scopus 로고
    • Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors
    • PID: 16352303
    • Mühlemann A, Ward NA, Kratochwil N, Diener C, Fischer C, Stucki A, Jaeschke G, Malherbe P, Porter RH (2006) Determination of key amino acids implicated in the actions of allosteric modulation by 3,3′-difluorobenzaldazine on rat mGlu5 receptors. Eur J Pharmacol 529:95–104
    • (2006) Eur J Pharmacol , vol.529 , pp. 95-104
    • Mühlemann, A.1    Ward, N.A.2    Kratochwil, N.3    Diener, C.4    Fischer, C.5    Stucki, A.6    Jaeschke, G.7    Malherbe, P.8    Porter, R.H.9
  • 55
    • 84867805089 scopus 로고    scopus 로고
    • Pharmacological characterization and modeling of the binding sites of novel 1,3-Bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators
    • PID: 22899869
    • Mølck C, Harpsøe K, Gloriam DE, Clausen RP, Madsen U, Pedersen LØ, Jimenez HN, Nielsen SM, Mathiesen JM, Bräuner-Osborne H (2012) Pharmacological characterization and modeling of the binding sites of novel 1,3-Bis(pyridinylethynyl)benzenes as metabotropic glutamate receptor 5-selective negative allosteric modulators. Mol Pharmacol 82:929–937
    • (2012) Mol Pharmacol , vol.82 , pp. 929-937
    • Mølck, C.1    Harpsøe, K.2    Gloriam, D.E.3    Clausen, R.P.4    Madsen, U.5    Pedersen, L.Ø.6    Jimenez, H.N.7    Nielsen, S.M.8    Mathiesen, J.M.9    Bräuner-Osborne, H.10
  • 56
    • 0034721795 scopus 로고    scopus 로고
    • The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors
    • PID: 10934211, COI: 1:CAS:528:DC%2BD3cXnvVyjtr4%3D
    • Pagano A, Ruegg D, Litschig S, Stoehr N, Stierlin C, Heinrich M, Floersheim P, Prezeau L, Carroll F, Pin JP, Cambria A, Vranesic I, Flor PJ, Gasparini F, Kuhn R (2000) The non-competitive antagonists 2-methyl-6-(phenylethynyl)pyridine and 7-hydroxyiminocyclopropan[b]chromen-1a-carboxylic acid ethyl ester interact with overlapping binding pockets in the transmembrane region of group I metabotropic glutamate receptors. J Biol Chem 275:33750–33758
    • (2000) J Biol Chem , vol.275 , pp. 33750-33758
    • Pagano, A.1    Ruegg, D.2    Litschig, S.3    Stoehr, N.4    Stierlin, C.5    Heinrich, M.6    Floersheim, P.7    Prezeau, L.8    Carroll, F.9    Pin, J.P.10    Cambria, A.11    Vranesic, I.12    Flor, P.J.13    Gasparini, F.14    Kuhn, R.15
  • 57
    • 68749094966 scopus 로고    scopus 로고
    • Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one
    • PID: 19559036, COI: 1:CAS:528:DC%2BD1MXhtVeis7jN
    • Fukuda J, Suzuki G, Kimura T, Nagatomi Y, Ito S, Kawamoto H, Ozaki S, Ohta H (2009) Identification of a novel transmembrane domain involved in the negative modulation of mGluR1 using a newly discovered allosteric mGluR1 antagonist, 3-cyclohexyl-5-fluoro-6-methyl-7-(2-morpholin-4-ylethoxy)-4H-chromen-4-one. Neuropharmacology 57:438–445
    • (2009) Neuropharmacology , vol.57 , pp. 438-445
    • Fukuda, J.1    Suzuki, G.2    Kimura, T.3    Nagatomi, Y.4    Ito, S.5    Kawamoto, H.6    Ozaki, S.7    Ohta, H.8
  • 58
    • 0035818605 scopus 로고    scopus 로고
    • Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site
    • PID: 11606768, COI: 1:CAS:528:DC%2BD3MXosFygtbc%3D
    • Knoflach F, Mutel V, Jolidon S, Kew JN, Malherbe P, Vieira E, Wichmann J, Kemp JA (2001) Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A 98:13402–13407
    • (2001) Proc Natl Acad Sci U S A , vol.98 , pp. 13402-13407
    • Knoflach, F.1    Mutel, V.2    Jolidon, S.3    Kew, J.N.4    Malherbe, P.5    Vieira, E.6    Wichmann, J.7    Kemp, J.A.8
  • 59
    • 0033028258 scopus 로고    scopus 로고
    • CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding
    • PID: 10051528, COI: 1:CAS:528:DyaK1MXhslWjtbY%3D
    • Litschig S, Gasparini F, Rueegg D, Stoehr N, Flor PJ, Vranesic I, Prezeau L, Pin JP, Thomsen C, Kuhn R (1999) CPCCOEt, a noncompetitive metabotropic glutamate receptor 1 antagonist, inhibits receptor signaling without affecting glutamate binding. Mol Pharmacol 55:453–461
    • (1999) Mol Pharmacol , vol.55 , pp. 453-461
    • Litschig, S.1    Gasparini, F.2    Rueegg, D.3    Stoehr, N.4    Flor, P.J.5    Vranesic, I.6    Prezeau, L.7    Pin, J.P.8    Thomsen, C.9    Kuhn, R.10
  • 60
    • 0037424518 scopus 로고    scopus 로고
    • Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor
    • PID: 12509432, COI: 1:CAS:528:DC%2BD3sXhsF2hsLo%3D
    • Malherbe P, Kratochwil N, Knoflach F, Zenner MT, Kew JN, Kratzeisen C, Maerki HP, Adam G, Mutel V (2003) Mutational analysis and molecular modeling of the allosteric binding site of a novel, selective, noncompetitive antagonist of the metabotropic glutamate 1 receptor. J Biol Chem 278:8340–8347
    • (2003) J Biol Chem , vol.278 , pp. 8340-8347
    • Malherbe, P.1    Kratochwil, N.2    Knoflach, F.3    Zenner, M.T.4    Kew, J.N.5    Kratzeisen, C.6    Maerki, H.P.7    Adam, G.8    Mutel, V.9
  • 61
    • 34248667888 scopus 로고    scopus 로고
    • Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl- 3,6-dihydropyridine-1(2H)-carboxamide (FTIDC)
    • PID: 17360958, COI: 1:CAS:528:DC%2BD2sXmsFeqsL0%3D
    • Suzuki G, Kimura T, Satow A, Kaneko N, Fukuda J, Hikichi H, Sakai N, Maehara S, Kawagoe-Takaki H, Hata M, Azuma T, Ito S, Kawamoto H, Ohta H (2007) Pharmacological characterization of a new, orally active and potent allosteric metabotropic glutamate receptor 1 antagonist, 4-[1-(2-fluoropyridin-3-yl)-5-methyl-1H-1,2,3-triazol-4-yl]-N-isopropyl-N-methyl- 3,6-dihydropyridine-1(2H)-carboxamide (FTIDC). J Pharmacol Exp Ther 321:1144–1153
    • (2007) J Pharmacol Exp Ther , vol.321 , pp. 1144-1153
    • Suzuki, G.1    Kimura, T.2    Satow, A.3    Kaneko, N.4    Fukuda, J.5    Hikichi, H.6    Sakai, N.7    Maehara, S.8    Kawagoe-Takaki, H.9    Hata, M.10    Azuma, T.11    Ito, S.12    Kawamoto, H.13    Ohta, H.14
  • 62
    • 84876593223 scopus 로고    scopus 로고
    • Probing the metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a “molecular switch” in PAM pharmacology
    • PID: 23444015, COI: 1:CAS:528:DC%2BC3sXmtFarsLc%3D
    • Gregory KJ, Nguyen ED, Reiff SD, Squire EF, Stauffer SR, Lindsley CW, Meiler J, Conn PJ (2013) Probing the metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulator (PAM) binding pocket: discovery of point mutations that engender a “molecular switch” in PAM pharmacology. Mol Pharmacol 83:991–1006
    • (2013) Mol Pharmacol , vol.83 , pp. 991-1006
    • Gregory, K.J.1    Nguyen, E.D.2    Reiff, S.D.3    Squire, E.F.4    Stauffer, S.R.5    Lindsley, C.W.6    Meiler, J.7    Conn, P.J.8
  • 72
    • 58149193205 scopus 로고    scopus 로고
    • Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders
    • PID: 19116626, COI: 1:CAS:528:DC%2BD1cXhsFCkurfF
    • Conn PJ, Christopoulos A, Lindsley CW (2009) Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 8:41–54
    • (2009) Nat Rev Drug Discov , vol.8 , pp. 41-54
    • Conn, P.J.1    Christopoulos, A.2    Lindsley, C.W.3
  • 74
    • 0037363728 scopus 로고    scopus 로고
    • Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP
    • PID: 12684257, COI: 1:CAS:528:DC%2BD3sXjtVahsLc%3D
    • Mathiesen JM, Svendsen N, Brauner-Osborne H, Thomsen C, Ramirez MT (2003) Positive allosteric modulation of the human metabotropic glutamate receptor 4 (hmGluR4) by SIB-1893 and MPEP. Br J Pharmacol 138:1026–1030
    • (2003) Br J Pharmacol , vol.138 , pp. 1026-1030
    • Mathiesen, J.M.1    Svendsen, N.2    Brauner-Osborne, H.3    Thomsen, C.4    Ramirez, M.T.5
  • 75
    • 79953213637 scopus 로고    scopus 로고
    • Molecular switches” on mGluR allosteric ligands that modulate modes of pharmacology
    • PID: 21341760, COI: 1:CAS:528:DC%2BC3MXislGntbg%3D
    • Wood MR, Hopkins CR, Brogan JT, Conn PJ, Lindsley CW (2011) “Molecular switches” on mGluR allosteric ligands that modulate modes of pharmacology. Biochemistry 50:2403–2410
    • (2011) Biochemistry , vol.50 , pp. 2403-2410
    • Wood, M.R.1    Hopkins, C.R.2    Brogan, J.T.3    Conn, P.J.4    Lindsley, C.W.5
  • 76
    • 84875416160 scopus 로고    scopus 로고
    • A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling
    • PID: 23348500, COI: 1:CAS:528:DC%2BC3sXlsVyrt7s%3D
    • Noetzel MJ, Gregory KJ, Vinson PN, Manka JT, Stauffer SR, Lindsley CW, Niswender CM, Xiang Z, Conn PJ (2013) A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling. Mol Pharmacol 83:835–847
    • (2013) Mol Pharmacol , vol.83 , pp. 835-847
    • Noetzel, M.J.1    Gregory, K.J.2    Vinson, P.N.3    Manka, J.T.4    Stauffer, S.R.5    Lindsley, C.W.6    Niswender, C.M.7    Xiang, Z.8    Conn, P.J.9
  • 81
    • 84888040704 scopus 로고    scopus 로고
    • Development of allosteric modulators of GPCRs for treatment of CNS disorders
    • PID: 24076101
    • Nickols HH, Conn PJ (2013) Development of allosteric modulators of GPCRs for treatment of CNS disorders. Neurobiol Dis 61:55–71
    • (2013) Neurobiol Dis , vol.61 , pp. 55-71
    • Nickols, H.H.1    Conn, P.J.2
  • 82
    • 75849152052 scopus 로고    scopus 로고
    • Glutamate receptors as therapeutic targets for Parkinson’s disease
    • COI: 1:CAS:528:DC%2BD1MXhsFGqt7fM
    • Johnson KA, Conn PJ, Niswender CM (2009) Glutamate receptors as therapeutic targets for Parkinson’s disease. CNS Neurol Disord: Drug Targets 8:475–491
    • (2009) CNS Neurol Disord: Drug Targets , vol.8 , pp. 475-491
    • Johnson, K.A.1    Conn, P.J.2    Niswender, C.M.3
  • 83
    • 34347241277 scopus 로고    scopus 로고
    • Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs
    • PID: 17582504, COI: 1:CAS:528:DC%2BD2sXntFyitbs%3D
    • Palucha A, Pilc A (2007) Metabotropic glutamate receptor ligands as possible anxiolytic and antidepressant drugs. Pharmacol Ther 115:116–147
    • (2007) Pharmacol Ther , vol.115 , pp. 116-147
    • Palucha, A.1    Pilc, A.2
  • 84
    • 0019957859 scopus 로고
    • Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study
    • PID: 7042771, COI: 1:STN:280:DyaL387ptVCqtA%3D%3D
    • Pecknold JC, McClure DJ, Appeltauer L, Wrzesinski L, Allan T (1982) Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study. J Clin Psychopharmacol 2:129–133
    • (1982) J Clin Psychopharmacol , vol.2 , pp. 129-133
    • Pecknold, J.C.1    McClure, D.J.2    Appeltauer, L.3    Wrzesinski, L.4    Allan, T.5
  • 86
    • 77953615107 scopus 로고    scopus 로고
    • Group 5 metabotropic glutamate receptors: role in modulating cortical activity and relevance to cognition
    • PID: 20371231, COI: 1:CAS:528:DC%2BC3cXntVShu7s%3D
    • Homayoun H, Moghaddam B (2010) Group 5 metabotropic glutamate receptors: role in modulating cortical activity and relevance to cognition. Eur J Pharmacol 639:33–39
    • (2010) Eur J Pharmacol , vol.639 , pp. 33-39
    • Homayoun, H.1    Moghaddam, B.2
  • 87
    • 84918785467 scopus 로고    scopus 로고
    • Accessed 28 Oct 2013
    • Novartis Clinical pipeline. http://www.novartis.com/innovation/research-development/clinical-pipeline/index.shtml. Accessed 28 Oct 2013
    • Novartis Clinical pipeline
  • 88
    • 58149119377 scopus 로고    scopus 로고
    • Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia
    • PID: 19058862, COI: 1:CAS:528:DC%2BD1MXktlygsg%3D%3D
    • Conn PJ, Lindsley CW, Jones CK (2009) Activation of metabotropic glutamate receptors as a novel approach for the treatment of schizophrenia. Trends Pharmacol Sci 30:25–31
    • (2009) Trends Pharmacol Sci , vol.30 , pp. 25-31
    • Conn, P.J.1    Lindsley, C.W.2    Jones, C.K.3
  • 90
    • 84876720539 scopus 로고    scopus 로고
    • Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks
    • PID: 23409764, COI: 1:CAS:528:DC%2BC3sXmtleqtbg%3D
    • Menniti FS, Lindsley CW, Conn PJ, Pandit J, Zagouras P, Volkmann RA (2013) Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks. Curr Top Med Chem 13:26–54
    • (2013) Curr Top Med Chem , vol.13 , pp. 26-54
    • Menniti, F.S.1    Lindsley, C.W.2    Conn, P.J.3    Pandit, J.4    Zagouras, P.5    Volkmann, R.A.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.