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The publication data currently available has been vetted by Vanderbilt faculty, staff, administrators and trainees. The data itself is retrieved directly from NCBI's PubMed and is automatically updated on a weekly basis to ensure accuracy and completeness.

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Results: 1 to 10 of 67

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Discovery of structurally distinct tricyclic M positive allosteric modulator (PAM) chemotypes.
Temple KJ, Long MF, Engers JL, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2020) Bioorg Med Chem Lett 30: 126811
MeSH Terms: Allosteric Regulation, Animals, Drug Design, Half-Life, Humans, Inhibitory Concentration 50, Pyridazines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
1 Members
0 Resources
12 MeSH Terms
Discovery of Novel Central Nervous System Penetrant Metabotropic Glutamate Receptor Subtype 2 (mGlu) Negative Allosteric Modulators (NAMs) Based on Functionalized Pyrazolo[1,5- a]pyrimidine-5-carboxamide and Thieno[3,2- b]pyridine-5-carboxamide Cores.
Childress ES, Wieting JM, Felts AS, Breiner MM, Long MF, Luscombe VB, Rodriguez AL, Cho HP, Blobaum AL, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW
(2019) J Med Chem 62: 378-384
MeSH Terms: Allosteric Regulation, Amides, Animals, Central Nervous System, Drug Evaluation, Preclinical, Half-Life, Humans, Inhibitory Concentration 50, Protein Isoforms, Pyrazoles, Pyridines, Pyrimidines, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu).
Bollinger SR, Engers DW, Panarese JD, West M, Engers JL, Loch MT, Rodriguez AL, Blobaum AL, Jones CK, Thompson Gray A, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
(2019) J Med Chem 62: 342-358
MeSH Terms: Allosteric Regulation, Amides, Animals, Brain, Catalepsy, Cytochrome P-450 CYP1A2, Half-Life, Haloperidol, Humans, Isoxazoles, Male, Rats, Rats, Sprague-Dawley, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms
Surface-Matrix Screening Identifies Semi-specific Interactions that Improve Potency of a Near Pan-reactive HIV-1-Neutralizing Antibody.
Kwon YD, Chuang GY, Zhang B, Bailer RT, Doria-Rose NA, Gindin TS, Lin B, Louder MK, McKee K, O'Dell S, Pegu A, Schmidt SD, Asokan M, Chen X, Choe M, Georgiev IS, Jin V, Pancera M, Rawi R, Wang K, Chaudhuri R, Kueltzo LA, Manceva SD, Todd JP, Scorpio DG, Kim M, Reinherz EL, Wagh K, Korber BM, Connors M, Shapiro L, Mascola JR, Kwong PD
(2018) Cell Rep 22: 1798-1809
MeSH Terms: Antibodies, Neutralizing, Cell Membrane, HIV Antibodies, HIV Envelope Protein gp41, HIV-1, Half-Life, Humans, Neutralization Tests, Polysaccharides, Protein Binding
Added March 14, 2018
0 Communities
1 Members
0 Resources
10 MeSH Terms
Discovery of a novel 2,4-dimethylquinoline-6-carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping.
Long MF, Engers JL, Chang S, Zhan X, Weiner RL, Luscombe VB, Rodriguez AL, Cho HP, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2017) Bioorg Med Chem Lett 27: 4999-5001
MeSH Terms: Allosteric Regulation, Amides, Animals, Brain, Drug Evaluation, Preclinical, Half-Life, Protein Binding, Pyridines, Rats, Rats, Sprague-Dawley, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Discovery of imidazo[1,2-a]-, [1,2,4]triazolo[4,3-a]-, and [1,2,4]triazolo[1,5-a]pyridine-8-carboxamide negative allosteric modulators of metabotropic glutamate receptor subtype 5.
Felts AS, Rodriguez AL, Morrison RD, Bollinger KA, Venable DF, Blobaum AL, Byers FW, Thompson Gray A, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Emmitte KA
(2017) Bioorg Med Chem Lett 27: 4858-4866
MeSH Terms: Allosteric Regulation, Amides, Animals, Cell Membrane Permeability, Dogs, Dopamine Plasma Membrane Transport Proteins, Drug Evaluation, Preclinical, Half-Life, Humans, Inhibitory Concentration 50, Madin Darby Canine Kidney Cells, Mice, Microsomes, Liver, Pyridines, Rats, Receptor, Metabotropic Glutamate 5, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms
Optimization of the choline transporter (CHT) inhibitor ML352: Development of VU6001221, an improved in vivo tool compound.
Bertron JL, Ennis EA, Tarr CJ, Wright J, Dickerson JW, Locuson CW, Blobaum AL, Rook JM, Blakely RD, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 4637-4640
MeSH Terms: Animals, Benzamides, Dose-Response Relationship, Drug, Half-Life, Inhibitory Concentration 50, Isoxazoles, Membrane Transport Proteins, Oxazoles, Piperidines, Rats, Structure-Activity Relationship
Added March 21, 2018
0 Communities
1 Members
0 Resources
11 MeSH Terms
Optimization of the Solubility of HIV-1-Neutralizing Antibody 10E8 through Somatic Variation and Structure-Based Design.
Kwon YD, Georgiev IS, Ofek G, Zhang B, Asokan M, Bailer RT, Bao A, Caruso W, Chen X, Choe M, Druz A, Ko SY, Louder MK, McKee K, O'Dell S, Pegu A, Rudicell RS, Shi W, Wang K, Yang Y, Alger M, Bender MF, Carlton K, Cooper JW, Blinn J, Eudailey J, Lloyd K, Parks R, Alam SM, Haynes BF, Padte NN, Yu J, Ho DD, Huang J, Connors M, Schwartz RM, Mascola JR, Kwong PD
(2016) J Virol 90: 5899-5914
MeSH Terms: Animals, Antibodies, Neutralizing, Chemistry Techniques, Analytical, Crystallography, X-Ray, Disulfides, HIV Antibodies, HIV-1, Half-Life, High-Throughput Nucleotide Sequencing, Humans, Hydrophobic and Hydrophilic Interactions, Macaca mulatta, Models, Molecular, Solubility
Added May 3, 2017
0 Communities
1 Members
0 Resources
14 MeSH Terms
Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.
Garcia-Barrantes PM, Cho HP, Metts AM, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 751-756
MeSH Terms: Allosteric Regulation, Animals, Antipsychotic Agents, Coumarins, Furans, Half-Life, Heterocyclic Compounds, Humans, Protein Binding, Rats, Receptors, Metabotropic Glutamate, Schizophrenia, Structure-Activity Relationship
Added February 18, 2016
0 Communities
2 Members
0 Resources
13 MeSH Terms
Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.
Garcia-Barrantes PM, Cho HP, Niswender CM, Byers FW, Locuson CW, Blobaum AL, Xiang Z, Rook JM, Conn PJ, Lindsley CW
(2015) J Med Chem 58: 7959-71
MeSH Terms: Animals, Central Nervous System, Epilepsy, GABA Agonists, GABA Modulators, Half-Life, Humans, Molecular Conformation, Rats, Receptor, Metabotropic Glutamate 5, Receptors, Metabotropic Glutamate, Schizophrenia, Structure-Activity Relationship
Added February 18, 2016
0 Communities
3 Members
0 Resources
13 MeSH Terms