메뉴 건너뛰기




Volumn 17, Issue 2, 2012, Pages 104-115

Design of an automated enhanced- throughput platform for functional characterization of positive allosteric modulator-induced leftward shifts in apparent agonist potency in vitro

Author keywords

Allosteric modulator; Automation; Functional assay; GPCR

Indexed keywords

AUTOMATION; PULSE AMPLITUDE MODULATION;

EID: 84863813096     PISSN: 22110682     EISSN: 22110690     Source Type: Journal    
DOI: 10.1177/2211068211435301     Document Type: Article
Times cited : (5)

References (27)
  • 1
    • 0033669603 scopus 로고    scopus 로고
    • Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation
    • Hall, D. A. Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation. Mol. Pharmacol. 2000, 58(6), 1412-1423.
    • (2000) Mol. Pharmacol. , vol.58 , Issue.6 , pp. 1412-1423
    • Hall, D.A.1
  • 2
    • 0036490942 scopus 로고    scopus 로고
    • Allosteric Binding Sites on Cell-Surface Receptors: Novel Targets for Drug Discovery
    • Christopoulos, A. Allosteric Binding Sites on Cell-Surface Receptors: Novel Targets for Drug Discovery. Nat. Rev. Drug Discov. 2002, 1, 198-210.
    • (2002) Nat. Rev. Drug Discov. , vol.1 , pp. 198-210
    • Christopoulos, A.1
  • 4
    • 53449093828 scopus 로고    scopus 로고
    • G-Protein-Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms
    • Bridges, T. M.; Lindsley, C. W. G-Protein-Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms. ACS Chem. Biol. 2008, 3(9), 530-541.
    • (2008) ACS Chem. Biol. , vol.3 , Issue.9 , pp. 530-541
    • Bridges, T.M.1    Lindsley, C.W.2
  • 5
    • 0036258990 scopus 로고    scopus 로고
    • G-Protein Coupled Receptor Allosterism and Complexing
    • Christopoulos, A.; Kenakin, T. G-Protein Coupled Receptor Allosterism and Complexing. Pharmacol. Rev. 2002, 54, 323-374.
    • (2002) Pharmacol. Rev. , vol.54 , pp. 323-374
    • Christopoulos, A.1    Kenakin, T.2
  • 7
    • 77957864491 scopus 로고    scopus 로고
    • The Role of GABA(A) Receptor Subtypes as Analgesic Targets
    • Mirza, N. R.; Munro, G. The Role of GABA(A) Receptor Subtypes as Analgesic Targets. Drug News Perspect. 2010, 23(6), 351-360.
    • (2010) Drug News Perspect. , vol.23 , Issue.6 , pp. 351-360
    • Mirza, N.R.1    Munro, G.2
  • 8
    • 0038798022 scopus 로고    scopus 로고
    • Direct and Indirect Modulation of the N-methyl D-aspartate Receptor
    • Marino, M. J.; Conn, P. J. Direct and Indirect Modulation of the N-methyl D-aspartate Receptor. Curr. Drug Targets CNS Neurol. Disord. 2003, 1(1), 1-16.
    • (2003) Curr. Drug Targets CNS Neurol. Disord. , vol.1 , Issue.1 , pp. 1-16
    • Marino, M.J.1    Conn, P.J.2
  • 10
    • 0038155299 scopus 로고    scopus 로고
    • Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine
    • Johnson, M. P.; Baez, M.; Jagdmann, G. E., Jr.; Britton, T. C.; Large, T. H.; Callagaro, D. O.; Tizzano, J. P.; Monn, J. A.; Schoepp, D. D. Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2-trifluoroethylsulfonyl)pyrid-3-ylmethylamine. J. Med. Chem. 2003, 46(15), 3189-3192.
    • (2003) J. Med. Chem. , vol.46 , Issue.15 , pp. 3189-3192
    • Johnson, M.P.1    Baez, M.2    Jagdmann Jr., G.E.3    Britton, T.C.4    Large, T.H.5    Callagaro, D.O.6    Tizzano, J.P.7    Monn, J.A.8    Schoepp, D.D.9
  • 11
    • 0347091891 scopus 로고    scopus 로고
    • Modulation of Excitatory Transmission onto Midbrain Dopaminergic Neurons of the Rat by Activation of Group III Metabotropic Glutamate Receptors
    • Valenti, O.; Marino, M. J.; Conn, P. J. Modulation of Excitatory Transmission onto Midbrain Dopaminergic Neurons of the Rat by Activation of Group III Metabotropic Glutamate Receptors. Ann. N. Y. Acad. Sci. 2003, 1003, 479-480.
    • (2003) Ann. N. Y. Acad. Sci. , vol.1003 , pp. 479-480
    • Valenti, O.1    Marino, M.J.2    Conn, P.J.3
  • 12
    • 33746265808 scopus 로고    scopus 로고
    • A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct from That of Negative Allosteric Modulators
    • Hemstapat, K.; de Paulis, T.; Chen, Y.; Brady, A. E.; Grover, V. K.; Alagille, D.; Tamagnan, G. D.; Conn, P. J. A Novel Class of Positive Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 1 Interact with a Site Distinct from That of Negative Allosteric Modulators. Mol. Pharmacol. 2006, 70(2), 616-626.
    • (2006) Mol. Pharmacol. , vol.70 , Issue.2 , pp. 616-626
    • Hemstapat, K.1    de Paulis, T.2    Chen, Y.3    Brady, A.E.4    Grover, V.K.5    Alagille, D.6    Tamagnan, G.D.7    Conn, P.J.8
  • 13
    • 49949084014 scopus 로고    scopus 로고
    • Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells
    • Sheffler, D. J.; Conn, P. J. Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells. Neuropharmacology 2008, 55(4), 419-427.
    • (2008) Neuropharmacology , vol.55 , Issue.4 , pp. 419-427
    • Sheffler, D.J.1    Conn, P.J.2
  • 17
    • 76749144987 scopus 로고    scopus 로고
    • Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties
    • Leach, K.; Loiacono, R. E.; Felder, C. C.; McKinzie, D. L.; Mogg, A.; Shaw, D. B.; Sexton, P. M.; Christopoulos, A. Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties. Neuropsychopharmacology 2010, 35(4), 855-869.
    • (2010) Neuropsychopharmacology , vol.35 , Issue.4 , pp. 855-869
    • Leach, K.1    Loiacono, R.E.2    Felder, C.C.3    McKinzie, D.L.4    Mogg, A.5    Shaw, D.B.6    Sexton, P.M.7    Christopoulos, A.8
  • 18
    • 33645108415 scopus 로고    scopus 로고
    • The Positive Allosteric Modulator GS39783 Enhances GABA(B) Receptor-Mediated Inhibition of Cyclic AMP Formation in Rat Striatum In Vivo
    • Gjoni, T.; Desreyaud, S.; Imobersteg, S.; Urwyler, S. The Positive Allosteric Modulator GS39783 Enhances GABA(B) Receptor-Mediated Inhibition of Cyclic AMP Formation in Rat Striatum In Vivo. J. Neurochem. 2006, 96(5), 1416-1422.
    • (2006) J. Neurochem. , vol.96 , Issue.5 , pp. 1416-1422
    • Gjoni, T.1    Desreyaud, S.2    Imobersteg, S.3    Urwyler, S.4
  • 19
    • 43249095827 scopus 로고    scopus 로고
    • Allosteric Modulators of GABA(B) Receptors: Mechanism of Action and Therapeutic Perspective
    • Pin, J. P.; Prézeau, L. Allosteric Modulators of GABA(B) Receptors: Mechanism of Action and Therapeutic Perspective. Curr. Neuropharmacol. 2007, 5(3), 195-201.
    • (2007) Curr. Neuropharmacol. , vol.5 , Issue.3 , pp. 195-201
    • Pin, J.P.1    Prézeau, L.2
  • 20
    • 27744560413 scopus 로고    scopus 로고
    • Calindol, a Positive Allosteric Modulator of the Human Ca(2+) Receptor, Activates an Extracellular Ligand-Binding Domain-Deleted Rhodopsin-Like Seven-Transmembrane Structure in the Absence of Ca(2+)
    • Ray, K.; Tisdale, J.; Dodd, R. H.; Dauban, P.; Ruat, M.; Northup, J. K. Calindol, a Positive Allosteric Modulator of the Human Ca(2+) Receptor, Activates an Extracellular Ligand-Binding Domain-Deleted Rhodopsin-Like Seven-Transmembrane Structure in the Absence of Ca(2+). J. Biol. Chem. 2005, 280(44), 37013-37020.
    • (2005) J. Biol. Chem. , vol.280 , Issue.44 , pp. 37013-37020
    • Ray, K.1    Tisdale, J.2    Dodd, R.H.3    Dauban, P.4    Ruat, M.5    Northup, J.K.6
  • 21
    • 36849028142 scopus 로고    scopus 로고
    • Calcium Sensing Receptor Activators: Calcimimetics
    • Harrington, P. E.; Fotsch, C. Calcium Sensing Receptor Activators: Calcimimetics. Curr. Med. Chem. 2007, 14(28), 3027-3034.
    • (2007) Curr. Med. Chem. , vol.14 , Issue.28 , pp. 3027-3034
    • Harrington, P.E.1    Fotsch, C.2
  • 22
    • 45749141326 scopus 로고    scopus 로고
    • Allosteric Modulation of the Calcium-Sensing Receptor
    • Jensen, A. A.; Bräuner-Osborne, H. Allosteric Modulation of the Calcium-Sensing Receptor. Curr. Neuropharmacol. 2007, 5(3), 180-186.
    • (2007) Curr. Neuropharmacol. , vol.5 , Issue.3 , pp. 180-186
    • Jensen, A.A.1    Bräuner-Osborne, H.2
  • 24
    • 34447638166 scopus 로고    scopus 로고
    • Allosteric Enhancers, Allosteric Agonists, and Ago-Allosteric Modulators: Where Do They Bind and How Do They Act?
    • Schwartz, Y. W.; Holst, B. Allosteric Enhancers, Allosteric Agonists, and Ago-Allosteric Modulators: Where Do They Bind and How Do They Act? Trends Pharmacol. Sci. 2007, 28, 366-373.
    • (2007) Trends Pharmacol. Sci. , vol.28 , pp. 366-373
    • Schwartz, Y.W.1    Holst, B.2
  • 26
    • 47149106805 scopus 로고    scopus 로고
    • Synthesis and SAR of a mGluR5 Allosteric Partial Antagonist Lead: Unexpected Modulation of Pharmacology with Slight Structural Modifications to a 5-(Phenylethynyl)pyrimidine Scaffold
    • Sharma, S.; Rodriguez, A. L.; Conn, P. J.; Lindsley, C. W. Synthesis and SAR of a mGluR5 Allosteric Partial Antagonist Lead: Unexpected Modulation of Pharmacology with Slight Structural Modifications to a 5-(Phenylethynyl)pyrimidine Scaffold. Bioorg. Med. Chem. Lett. 2008, 18(14), 4098-4101.
    • (2008) Bioorg. Med. Chem. Lett. , vol.18 , Issue.14 , pp. 4098-4101
    • Sharma, S.1    Rodriguez, A.L.2    Conn, P.J.3    Lindsley, C.W.4
  • 27
    • 8644252687 scopus 로고    scopus 로고
    • Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-diphenyl-1H-pyrazol-5yl)benzamides That Potentiate Receptor Function In Vivo
    • Lindsley, C. W.; Wisnoski, D. D.; Leister, W. H.; O'Brien, J. A.; Lemaire, W.; Williams, D. L., Jr.; Burno, M.; Sur, C.; Kinney, G. G.; Pettibone, D. J.; et al. Discovery of Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 5 from a Series of N-(1,3-diphenyl-1H-pyrazol-5yl)benzamides That Potentiate Receptor Function In Vivo. J. Med. Chem. 2004, 47, 5825-5828.
    • (2004) J. Med. Chem. , vol.47 , pp. 5825-5828
    • Lindsley, C.W.1    Wisnoski, D.D.2    Leister, W.H.3    O'Brien, J.A.4    Lemaire, W.5    Williams Jr., D.L.6    Burno, M.7    Sur, C.8    Kinney, G.G.9    Pettibone, D.J.10


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.