Research ArticleArticle
Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships
Karen J. Gregory, Meredith J. Noetzel, Jerri M. Rook, Paige N. Vinson, Shaun R. Stauffer, Alice L. Rodriguez, Kyle A. Emmitte, Ya Zhou, Aspen C. Chun, Andrew S. Felts, Brian A. Chauder, Craig W. Lindsley, Colleen M. Niswender and P. Jeffrey Conn
Molecular Pharmacology November 2012, 82 (5) 860-875; DOI: https://doi.org/10.1124/mol.112.080531
Karen J. Gregory
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Meredith J. Noetzel
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Jerri M. Rook
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Paige N. Vinson
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Shaun R. Stauffer
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Alice L. Rodriguez
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Kyle A. Emmitte
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Ya Zhou
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Aspen C. Chun
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Andrew S. Felts
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Brian A. Chauder
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Craig W. Lindsley
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
Colleen M. Niswender
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
P. Jeffrey Conn
Vanderbilt Center for Neuroscience Drug Discovery (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Departments of Pharmacology (K.J.G., M.J.N., J.M.R., P.N.V., S.R.S., A.L.R., K.A.E., Y.Z., A.C.C., A.S.F., B.A.C., C.W.L., C.M.N., P.J.C.) and Chemistry (K.A.E., C.W.L.), Vanderbilt University Medical Center, Nashville, Tennessee; and Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Australia (K.J.G.)
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Research ArticleArticle
Delineating mGlu5 Modulator Affinity and Cooperativity
Karen J. Gregory, Meredith J. Noetzel, Jerri M. Rook, Paige N. Vinson, Shaun R. Stauffer, Alice L. Rodriguez, Kyle A. Emmitte, Ya Zhou, Aspen C. Chun, Andrew S. Felts, Brian A. Chauder, Craig W. Lindsley, Colleen M. Niswender and P. Jeffrey Conn
Molecular Pharmacology November 1, 2012, 82 (5) 860-875; DOI: https://doi.org/10.1124/mol.112.080531
Research ArticleArticle
Delineating mGlu5 Modulator Affinity and Cooperativity
Karen J. Gregory, Meredith J. Noetzel, Jerri M. Rook, Paige N. Vinson, Shaun R. Stauffer, Alice L. Rodriguez, Kyle A. Emmitte, Ya Zhou, Aspen C. Chun, Andrew S. Felts, Brian A. Chauder, Craig W. Lindsley, Colleen M. Niswender and P. Jeffrey Conn
Molecular Pharmacology November 1, 2012, 82 (5) 860-875; DOI: https://doi.org/10.1124/mol.112.080531
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