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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 20

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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
ML327 induces apoptosis and sensitizes Ewing sarcoma cells to TNF-related apoptosis-inducing ligand.
Rellinger EJ, Padmanabhan C, Qiao J, Appert A, Waterson AG, Lindsley CW, Beauchamp RD, Chung DH
(2017) Biochem Biophys Res Commun 491: 463-468
MeSH Terms: Antigens, CD, Antineoplastic Agents, Apoptosis, Cadherins, Caspase 3, Cell Cycle, Cell Line, Tumor, Drug Synergism, Epithelial-Mesenchymal Transition, Gene Expression Regulation, Humans, Isoxazoles, Mesenchymal Stem Cells, Niacinamide, Poly(ADP-ribose) Polymerases, Sarcoma, Ewing, Signal Transduction, Small Molecule Libraries, TNF-Related Apoptosis-Inducing Ligand, Vimentin
Added March 14, 2018
0 Communities
1 Members
0 Resources
20 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 a small molecule probe that restores e-cadherin expression.
Brogan JT, Stoops SL, Brady S, An H, Weaver C, Daniels JS, Beauchamp RD, Lindsley CW, Waterson AG
(2015) Bioorg Med Chem Lett 25: 4260-4
MeSH Terms: Animals, Cadherins, Cell Line, Tumor, Dose-Response Relationship, Drug, Humans, Isoxazoles, Mice, Molecular Structure, Rats, Structure-Activity Relationship
Added October 15, 2015
0 Communities
1 Members
0 Resources
10 MeSH Terms
Small molecule/ML327 mediated transcriptional de-repression of E-cadherin and inhibition of epithelial-to-mesenchymal transition.
An H, Stoops SL, Deane NG, Zhu J, Zi J, Weaver C, Waterson AG, Zijlstra A, Lindsley CW, Beauchamp RD
(2015) Oncotarget 6: 22934-48
MeSH Terms: Animals, Cadherins, Cell Line, Tumor, Chick Embryo, Colorectal Neoplasms, Epithelial-Mesenchymal Transition, Female, Humans, Isoxazoles, Lung Neoplasms, Mammary Neoplasms, Experimental, Mice, Neoplasm Invasiveness, Neoplasms, Niacinamide, Small Molecule Libraries, Transcription, Genetic
Added July 16, 2015
1 Communities
3 Members
0 Resources
17 MeSH Terms
Identification and characterization of ML352: a novel, noncompetitive inhibitor of the presynaptic choline transporter.
Ennis EA, Wright J, Retzlaff CL, McManus OB, Lin Z, Huang X, Wu M, Li M, Daniels JS, Lindsley CW, Hopkins CR, Blakely RD
(2015) ACS Chem Neurosci 6: 417-27
MeSH Terms: Animals, Benzamides, Choline, Dose-Response Relationship, Drug, Enzyme Inhibitors, Gene Expression Regulation, HEK293 Cells, Hemicholinium 3, Humans, Isoxazoles, Male, Membrane Potentials, Membrane Transport Proteins, Mice, Mice, Inbred C57BL, Models, Biological, Mutation, Neural Inhibition, Prosencephalon, Protein Binding, Rats, Rats, Sprague-Dawley, Synaptosomes
Added February 12, 2015
0 Communities
1 Members
0 Resources
23 MeSH Terms
PET radiotracer [¹⁸F]-P6 selectively targeting COX-1 as a novel biomarker in ovarian cancer: preliminary investigation.
Perrone MG, Malerba P, Uddin J, Vitale P, Panella A, Crews BC, Daniel CK, Ghebreselasie K, Nickels M, Tantawy MN, Manning HC, Marnett LJ, Scilimati A
(2014) Eur J Med Chem 80: 562-568
MeSH Terms: Animals, Biomarkers, Tumor, Cell Line, Tumor, Cell Transformation, Neoplastic, Cyclooxygenase 1, Cyclooxygenase Inhibitors, Female, Fluorine Radioisotopes, Furans, Humans, Isoxazoles, Mice, Ovarian Neoplasms, Positron-Emission Tomography, Radioactive Tracers, Radiochemistry, Tomography, X-Ray Computed
Added May 20, 2014
0 Communities
3 Members
0 Resources
17 MeSH Terms
Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.
Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW
(2014) ChemMedChem 9: 1677-82
MeSH Terms: Acetophenones, Animals, Drug Evaluation, Preclinical, Half-Life, Humans, Isoxazoles, Molecular Probes, Muscarinic Antagonists, Protein Binding, Rats, Receptor, Muscarinic M5
Added February 19, 2015
0 Communities
2 Members
0 Resources
11 MeSH Terms
Hsp90 inhibitors promote p53-dependent apoptosis through PUMA and Bax.
He K, Zheng X, Zhang L, Yu J
(2013) Mol Cancer Ther 12: 2559-68
MeSH Terms: Animals, Apoptosis, Apoptosis Regulatory Proteins, Benzoquinones, Cell Line, Tumor, Colorectal Neoplasms, DNA Damage, HCT116 Cells, HSP90 Heat-Shock Proteins, Humans, Isoxazoles, Lactams, Macrocyclic, Mice, Mice, Nude, Mitochondria, Proto-Oncogene Proteins, Resorcinols, Tumor Suppressor Protein p53, Xenograft Model Antitumor Assays, bcl-2-Associated X Protein
Added July 28, 2015
0 Communities
1 Members
0 Resources
20 MeSH Terms
Changes in cotherapies after initiation of disease-modifying antirheumatic drug therapy in patients with rheumatoid arthritis.
Kawai VK, Grijalva CG, Arbogast PG, Curtis JR, Solomon DH, Delzell E, Chen L, Ouellet-Hellstrom R, Herrinton L, Liu L, Mitchel EF, Stein CM, Griffin MR
(2011) Arthritis Care Res (Hoboken) 63: 1415-24
MeSH Terms: Adrenal Cortex Hormones, Adult, Aged, Anti-Inflammatory Agents, Non-Steroidal, Antirheumatic Agents, Arthritis, Rheumatoid, Cohort Studies, Drug Administration Schedule, Drug Therapy, Combination, Female, Humans, Hydroxychloroquine, Isoxazoles, Leflunomide, Male, Methotrexate, Middle Aged, Narcotics, Retrospective Studies, Sulfasalazine, Time Factors, Treatment Outcome, Tumor Necrosis Factor-alpha
Added December 10, 2013
0 Communities
3 Members
0 Resources
23 MeSH Terms