Design of an Automated Enhanced-Throughput Platform for Functional Characterization of Positive Allosteric Modulator-Induced Leftward Shifts in Apparent Agonist Potency In Vitro

SLAS Technology - Tập 17 - Trang 104-115 - 2012
Adam Hendricson1, Michele Matchett1, Meredith Ferrante1, Chris Ferrante1, Ed Hunnicutt1, Ryan Westphal1, Walt Kostich1, Yanling Huang1, Nelly Masias1, Debra Hong1, Rob Bertekap2, Neil Burford1, John Watson1, Andrew Alt1, Jim Myslik1, Litao Zhang1, Ron Knox1
1Bristol-Myers Squibb, Wallingford, CT, USA
2Bristol Myers Squibb, Wallingford, CT, USA

Tài liệu tham khảo

Hall, 2000, Modeling the Functional Effects of Allosteric Modulators at Pharmacological Receptors: An Extension of the Two-State Model of Receptor Activation, Mol. Pharmacol, 58, 1412, 10.1124/mol.58.6.1412 Christopoulos, 2002, Allosteric Binding Sites on Cell-Surface Receptors: Novel Targets for Drug Discovery, Nat. Rev. Drug Discov, 1, 198, 10.1038/nrd746 May, 2007, Allosteric Modulation of G-Protein Coupled Receptors, Annu. Rev. Pharmacol. Toxicol, 47, 1, 10.1146/annurev.pharmtox.47.120505.105159 Bridges, 2008, G-Protein-Coupled Receptors: From Classical Modes of Modulation to Allosteric Mechanisms, ACS Chem. Biol, 3, 530, 10.1021/cb800116f Christopoulos, 2002, G-Protein Coupled Receptor Allosterism and Complexing, Pharmacol. Rev, 54, 323, 10.1124/pr.54.2.323 Möhler, 2002, A New Benzodiazepine Pharmacology, J. Pharmacol. Exp. Ther, 300, 2, 10.1124/jpet.300.1.2 Mirza, 2010, The Role of GABA(A) Receptor Subtypes as Analgesic Targets, Drug News Perspect, 23, 351, 10.1358/dnp.2010.23.6.1489909 Marino, 2003, Direct and Indirect Modulation of the N-methyl D-aspartate Receptor, Curr. Drug Targets CNS Neurol. Disord, 1, 1, 10.2174/1568007023339544 Capelli, 2010, Identification of Novel alpha7 nAChR Positive Allosteric Modulators with the use of Pharmacophore In Silico Screening Methods, Bioorg. Med. Chem. Lett, 20, 4561, 10.1016/j.bmcl.2010.06.014 Johnson, 2003, 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, 46, 3189, 10.1021/jm034015u Valenti, 2003, Modulation of Excitatory Transmission onto Midbrain Dopaminergic Neurons of the Rat by Activation of Group III Metabotropic Glutamate Receptors, Ann. N. Y. Acad. Sci, 1003, 479, 10.1196/annals.1300.058 Hemstapat, 2006, 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, 70, 616, 10.1124/mol.105.021857 Sheffler, 2008, Allosteric Potentiators of Metabotropic Glutamate Receptor Subtype 1a Differentially Modulate Independent Signaling Pathways in Baby Hamster Kidney Cells, Neuropharmacology, 55, 419, 10.1016/j.neuropharm.2008.06.047 Valant, 2010, Delineating the Mode of Action of Adenosine A1 Receptor Allosteric Modulators, Mol. Pharmacol, 78, 444, 10.1124/mol.110.064568 Thomas, 2008, G Protein Coupling and Signaling Pathway Activation by M1 Muscarinic Acetylcholine Receptor Orthosteric and Allosteric Agonists, J. Pharmacol. Exp. Ther, 327, 365, 10.1124/jpet.108.141788 Yang, 2010, Parallel Synthesis of N-biaryl Quinolone Carboxylic Acids as Selective M(1) Positive Allosteric Modulators, Bioorg. Med. Chem. Lett, 20, 531, 10.1016/j.bmcl.2009.11.100 Leach, 2010, Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties, Neuropsychopharmacology, 35, 855, 10.1038/npp.2009.194 Gjoni, 2006, The Positive Allosteric Modulator GS39783 Enhances GABA(B) Receptor-Mediated Inhibition of Cyclic AMP Formation in Rat Striatum In Vivo, J. Neurochem, 96, 1416, 10.1111/j.1471-4159.2006.03660.x Pin, 2007, Allosteric Modulators of GABA(B) Receptors: Mechanism of Action and Therapeutic Perspective, Curr. Neuropharmacol, 5, 195, 10.2174/157015907781695919 Ray, 2005, 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, 280, 37013, 10.1074/jbc.M506681200 Harrington, 2007, Calcium Sensing Receptor Activators: Calcimimetics, Curr. Med. Chem, 14, 3027, 10.2174/092986707782794096 Jensen, 2007, Allosteric Modulation of the Calcium-Sensing Receptor, Curr. Neuropharmacol, 5, 180, 10.2174/157015907781695982 Kennedy, 2008, Application of Combinatorial Science on Modern Drug Discovery, J. Comb. Chem, 10, 345, 10.1021/cc700187t Schwartz, 2007, Allosteric Enhancers, Allosteric Agonists, and Ago-Allosteric Modulators: Where Do They Bind and How Do They Act?, Trends Pharmacol. Sci, 28, 366, 10.1016/j.tips.2007.06.008 O’Brien, 2003, A Family of Highly Selective Allosteric Modulators of the Metabotropic Glutamate Receptor Subtype 5, Mol. Pharmacol, 64, 731, 10.1124/mol.64.3.731 Sharma, 2008, 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, 18, 4098, 10.1016/j.bmcl.2008.05.091 Lindsley, 2004, 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, 47, 5825, 10.1021/jm049400d