메뉴 건너뛰기




Volumn 20, Issue , 2015, Pages 1-7

Structures of mGluRs shed light on the challenges of drug development of allosteric modulators

Author keywords

[No Author keywords available]

Indexed keywords

2 METHYL 6 (PHENYLETHYNYL)PYRIDINE; DIPRAGLURANT; FENOBAM; G PROTEIN COUPLED RECEPTOR; GSK 221087; MAVOGLURANT; METABOTROPIC RECEPTOR; METABOTROPIC RECEPTOR 1; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR ANTAGONIST; QUISQUALIC ACID; RASEGLURANT; UNCLASSIFIED DRUG; AMINO ACID RECEPTOR BLOCKING AGENT; AMINO ACID RECEPTOR STIMULATING AGENT;

EID: 84908159410     PISSN: 14714892     EISSN: 14714973     Source Type: Journal    
DOI: 10.1016/j.coph.2014.09.022     Document Type: Review
Times cited : (29)

References (46)
  • 2
    • 0030995878 scopus 로고    scopus 로고
    • Pharmacology and functions of metabotropic glutamate receptors
    • P.J. Conn, and J.P. Pin Pharmacology and functions of metabotropic glutamate receptors Annu Rev Pharmacol Toxicol 37 1997 205 237
    • (1997) Annu Rev Pharmacol Toxicol , vol.37 , pp. 205-237
    • Conn, P.J.1    Pin, J.P.2
  • 5
    • 24644471456 scopus 로고    scopus 로고
    • New therapeutic frontiers for metabotropic glutamate receptors
    • C. Niswender, C. Jones, and P. Conn New therapeutic frontiers for metabotropic glutamate receptors Curr Top Med Chem 5 2005 847 857
    • (2005) Curr Top Med Chem , vol.5 , pp. 847-857
    • Niswender, C.1    Jones, C.2    Conn, P.3
  • 7
    • 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
    • P. Malherbe, N. Kratochwil, M.T. Zenner, J. Piussi, C. Diener, C. Kratzeisen, C. Fischer, and R.H. Porter 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 2003 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
  • 8
    • 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
    • A. Pagano, D. Ruegg, S. Litschig, N. Stoehr, C. Stierlin, M. Heinrich, P. Floersheim, L. Prezèau, F. Carroll, and J.P. Pin 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 2000 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    Prezèau, L.8    Carroll, F.9    Pin, J.P.10
  • 9
    • 84864116271 scopus 로고    scopus 로고
    • Orthosteric versus allosteric GPCR activation: The great challenge of group-III mGluRs
    • P.J. Flor, and F.C. Acher Orthosteric versus allosteric GPCR activation: the great challenge of group-III mGluRs Biochem Pharmacol 84 2012 414 424
    • (2012) Biochem Pharmacol , vol.84 , pp. 414-424
    • Flor, P.J.1    Acher, F.C.2
  • 15
    • 77952473377 scopus 로고    scopus 로고
    • Glutamatergic fine tuning with ADX-10059: A novel therapeutic approach for migraine?
    • J.C. Marin, and P.J. Goadsby Glutamatergic fine tuning with ADX-10059: a novel therapeutic approach for migraine? Expert Opin Investig Drugs 19 2010 555 561
    • (2010) Expert Opin Investig Drugs , vol.19 , pp. 555-561
    • Marin, J.C.1    Goadsby, P.J.2
  • 16
    • 84875192840 scopus 로고    scopus 로고
    • MGlu5 negative allosteric modulators: A patent review (2010-2012)
    • K.A. Emmitte mGlu5 negative allosteric modulators: a patent review (2010-2012) Expert Opin Ther Patents 23 2013 393 408
    • (2013) Expert Opin Ther Patents , vol.23 , pp. 393-408
    • Emmitte, K.A.1
  • 19
    • 0018877483 scopus 로고
    • Phase II double-blind controlled study of a new anxiolytic, fenobam (McN-3377) vs placebo
    • C.T.H. Friedmann, L.J. Davis, P.E. Ciccone, and R.T. Rubin Phase II double-blind controlled study of a new anxiolytic, fenobam (McN-3377) vs placebo Curr Ther Res 27 1980 144 151
    • (1980) Curr Ther Res , vol.27 , pp. 144-151
    • Friedmann, C.T.H.1    Davis, L.J.2    Ciccone, P.E.3    Rubin, R.T.4
  • 30
    • 77957055780 scopus 로고
    • Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors
    • J.A. Ballesteros, and H. Weinstein Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors Methods Neurosci 25 1995 366 428
    • (1995) Methods Neurosci , vol.25 , pp. 366-428
    • Ballesteros, J.A.1    Weinstein, H.2
  • 31
    • 0038662595 scopus 로고    scopus 로고
    • Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors
    • J.P. Pin, T. Galvez, and L. Prézeau Evolution, structure, and activation mechanism of family 3/C G-protein-coupled receptors Pharmacol Ther 98 2003 325 354
    • (2003) Pharmacol Ther , vol.98 , pp. 325-354
    • Pin, J.P.1    Galvez, T.2    Prézeau, L.3
  • 37
    • 84860505658 scopus 로고    scopus 로고
    • New insights from structural biology into the druggability of G protein coupled receptors
    • J.S. Mason, A. Bortolato, M. Congreve, and F.H. Marshall New insights from structural biology into the druggability of G protein coupled receptors Trends Pharmacol Sci 33 2012 249 260
    • (2012) Trends Pharmacol Sci , vol.33 , pp. 249-260
    • Mason, J.S.1    Bortolato, A.2    Congreve, M.3    Marshall, F.H.4
  • 38
    • 84902164279 scopus 로고    scopus 로고
    • High end GPCR design: Crafted ligand design and druggability analysis using protein structure, lipophilic hotspots and explicit water networks
    • J.S. Mason, A. Bortolato, D.R. Weiss, F. Deflorian, B. Tehan, and F.H. Marshall High end GPCR design: crafted ligand design and druggability analysis using protein structure, lipophilic hotspots and explicit water networks In Silico Pharmacol 1 2013 1 12
    • (2013) Silico Pharmacol , vol.1 , pp. 1-12
    • Mason, J.S.1    Bortolato, A.2    Weiss, D.R.3    Deflorian, F.4    Tehan, B.5    Marshall, F.H.6
  • 43
    • 84897026211 scopus 로고    scopus 로고
    • Structure-based and fragment-based GPCR drug discovery
    • S.P. Andrews, G.A. Brown, and J.A. Christopher Structure-based and fragment-based GPCR drug discovery ChemMedChem 9 2014 256 275
    • (2014) ChemMedChem , vol.9 , pp. 256-275
    • Andrews, S.P.1    Brown, G.A.2    Christopher, J.A.3
  • 45
    • 79960176452 scopus 로고    scopus 로고
    • Progress in structure based drug design for G protein-coupled receptors
    • M. Congreve, C.J. Langmead, J.S. Mason, and F.H. Marshall Progress in structure based drug design for G protein-coupled receptors J Med Chem 54 2011 4283 4311
    • (2011) J Med Chem , vol.54 , pp. 4283-4311
    • Congreve, M.1    Langmead, C.J.2    Mason, J.S.3    Marshall, F.H.4


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.