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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 103

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Small Molecule Inhibitor Screen Reveals Calcium Channel Signaling as a Mechanistic Mediator of TcdB-Induced Necrosis.
Farrow MA, Chumber NM, Bloch SC, King M, Moton-Melancon K, Shupe J, Washington MK, Spiller BW, Lacy DB
(2020) ACS Chem Biol 15: 1212-1221
MeSH Terms: Actin Cytoskeleton, Animals, Anti-Infective Agents, Bacterial Toxins, Calcium Channel Blockers, Calcium Channels, Calcium Signaling, Clostridioides difficile, Cytokines, Dihydropyridines, Dose-Response Relationship, Drug, Drug Evaluation, Preclinical, Glucosyltransferases, Humans, Kinetics, Mice, NADPH Oxidases, Necrosis, Reactive Oxygen Species, Virulence Factors
Added March 24, 2020
0 Communities
2 Members
0 Resources
20 MeSH Terms
Discovery of a novel 2,3-dimethylimidazo[1,2-a]pyrazine-6-carboxamide M positive allosteric modulator (PAM) chemotype.
Temple KJ, Engers JL, Long MF, Watson KJ, Chang S, Luscombe VB, Jenkins MT, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2020) Bioorg Med Chem Lett 30: 126812
MeSH Terms: Allosteric Regulation, Drug Design, Drug Evaluation, Preclinical, Humans, Imidazoles, Kinetics, Protein Binding, Pyrazines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
10 MeSH Terms
Discovery of Potent Myeloid Cell Leukemia-1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer.
Lee T, Christov PP, Shaw S, Tarr JC, Zhao B, Veerasamy N, Jeon KO, Mills JJ, Bian Z, Sensintaffar JL, Arnold AL, Fogarty SA, Perry E, Ramsey HE, Cook RS, Hollingshead M, Davis Millin M, Lee KM, Koss B, Budhraja A, Opferman JT, Kim K, Arteaga CL, Moore WJ, Olejniczak ET, Savona MR, Fesik SW
(2019) J Med Chem 62: 3971-3988
MeSH Terms: Animals, Antineoplastic Agents, Azepines, Binding Sites, Cell Line, Tumor, Cell Survival, Crystallography, X-Ray, Drug Evaluation, Preclinical, Female, Humans, Mice, Mice, Inbred NOD, Mice, SCID, Molecular Dynamics Simulation, Myeloid Cell Leukemia Sequence 1 Protein, Neoplasms, Protein Structure, Tertiary, Small Molecule Libraries, Structure-Activity Relationship, Xenograft Model Antitumor Assays
Added April 15, 2019
0 Communities
1 Members
0 Resources
20 MeSH Terms
A Coordinated Attack: Rett Syndrome Therapeutic Development.
Gogliotti RG, Niswender CM
(2019) Trends Pharmacol Sci 40: 233-236
MeSH Terms: Animals, Drug Discovery, Drug Evaluation, Preclinical, Drug Repositioning, Female, Humans, Methyl-CpG-Binding Protein 2, Mutation, Research Design, Rett Syndrome
Added March 3, 2020
0 Communities
1 Members
0 Resources
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
Chemical Screening Using Cell-Free Egg Extract.
Broadus MR, Lee E
(2018) Cold Spring Harb Protoc 2018:
MeSH Terms: Animals, Cell-Free System, Drug Evaluation, Preclinical, Ovum, Xenopus laevis
Added April 8, 2018
0 Communities
1 Members
0 Resources
5 MeSH Terms
Cancer therapy-induced cardiomyopathy: can human induced pluripotent stem cell modelling help prevent it?
Stack JP, Moslehi J, Sayed N, Wu JC
(2019) Eur Heart J 40: 1764-1770
MeSH Terms: Animals, Antineoplastic Agents, Cardiomyopathies, Cardiotoxicity, Cardiotoxins, Drug Evaluation, Preclinical, Genomics, Humans, Induced Pluripotent Stem Cells, Mice, Models, Biological, Neoplasms, Precision Medicine
Added April 22, 2018
0 Communities
1 Members
0 Resources
13 MeSH Terms
GBT1118, a compound that increases the oxygen affinity of hemoglobin, improves survival in murine hypoxic acute lung injury.
Putz ND, Shaver CM, Dufu K, Li CM, Xu Q, Hutchaleelaha A, Lehrer-Graiwer J, Majka SM, Ware LB, Bastarache JA
(2018) J Appl Physiol (1985) 124: 899-905
MeSH Terms: Acute Lung Injury, Animals, Benzaldehydes, Disease Models, Animal, Drug Evaluation, Preclinical, Hypoxia, Lipopolysaccharides, Male, Mice, Inbred C57BL, Niacinamide
Added May 31, 2018
0 Communities
1 Members
0 Resources
10 MeSH Terms
When Enough Is Enough: Decision Criteria for Moving a Known Drug into Clinical Testing for a New Indication in the Absence of Preclinical Efficacy Data.
Pulley JM, Jerome RN, Zaleski NM, Shirey-Rice JK, Pruijssers AJ, Lavieri RR, Chettiar SN, Naylor HM, Aronoff DM, Edwards DA, Niswender CM, Dugan LL, Crofford LJ, Bernard GR, Holroyd KJ
(2017) Assay Drug Dev Technol 15: 354-361
MeSH Terms: Animals, Clinical Trials as Topic, Decision Making, Drug Evaluation, Preclinical, Drug Repositioning, Humans, Models, Animal
Added March 26, 2019
0 Communities
4 Members
0 Resources
MeSH Terms
Challenges in the development of an M PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.
Tarr JC, Wood MR, Noetzel MJ, Melancon BJ, Lamsal A, Luscombe VB, Rodriguez AL, Byers FW, Chang S, Cho HP, Engers DW, Jones CK, Niswender CM, Wood MW, Brandon NJ, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2017) Bioorg Med Chem Lett 27: 5179-5184
MeSH Terms: Allosteric Regulation, Amides, Azetidines, Drug Evaluation, Preclinical, Humans, Protein Binding, Pyridazines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms