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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 201

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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
Tuning Ligand Density To Optimize Pharmacokinetics of Targeted Nanoparticles for Dual Protection against Tumor-Induced Bone Destruction.
Vanderburgh J, Hill JL, Gupta MK, Kwakwa KA, Wang SK, Moyer K, Bedingfield SK, Merkel AR, d'Arcy R, Guelcher SA, Rhoades JA, Duvall CL
(2020) ACS Nano 14: 311-327
MeSH Terms: Animals, Antineoplastic Agents, Bone Neoplasms, Cell Line, Tumor, Cell Proliferation, Disease Models, Animal, Drug Screening Assays, Antitumor, Female, Humans, Ligands, Mice, Mice, Inbred C57BL, Mice, Knockout, Nanoparticles, Optical Imaging, Particle Size, Polymers, Pyridines, Surface Properties, Thiophenes, X-Ray Microtomography
Added March 19, 2020
0 Communities
3 Members
0 Resources
21 MeSH Terms
Discovery of a novel 3,4-dimethylcinnoline carboxamide M positive allosteric modulator (PAM) chemotype via scaffold hopping.
Temple KJ, Engers JL, Long MF, Gregro AR, Watson KJ, Chang S, Jenkins MT, Luscombe VB, Rodriguez AL, Niswender CM, Bridges TM, Conn PJ, Engers DW, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 126678
MeSH Terms: Allosteric Regulation, Amides, Azetidines, Benzene, Molecular Structure, Protein Binding, Pyrazines, Pyridines, Pyrimidines, Receptor, Muscarinic M4, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
11 MeSH Terms
Systemic delivery of a Gli inhibitor via polymeric nanocarriers inhibits tumor-induced bone disease.
Vanderburgh JP, Kwakwa KA, Werfel TA, Merkel AR, Gupta MK, Johnson RW, Guelcher SA, Duvall CL, Rhoades JA
(2019) J Control Release 311-312: 257-272
MeSH Terms: Animals, Antineoplastic Agents, Apoptosis, Bone Neoplasms, Cell Line, Tumor, Cell Proliferation, Cell Survival, Drug Carriers, Drug Liberation, Female, Gene Expression Regulation, Neoplastic, Humans, Mammary Neoplasms, Animal, Mesenchymal Stem Cells, Mice, Inbred C57BL, Mice, Knockout, Mice, Nude, Nanoparticles, Osteogenesis, Polymers, Pyridines, Thiophenes, Zinc Finger Protein Gli2
Added March 3, 2020
0 Communities
4 Members
0 Resources
23 MeSH Terms
Aberrant FGFR signaling mediates resistance to CDK4/6 inhibitors in ER+ breast cancer.
Formisano L, Lu Y, Servetto A, Hanker AB, Jansen VM, Bauer JA, Sudhan DR, Guerrero-Zotano AL, Croessmann S, Guo Y, Ericsson PG, Lee KM, Nixon MJ, Schwarz LJ, Sanders ME, Dugger TC, Cruz MR, Behdad A, Cristofanilli M, Bardia A, O'Shaughnessy J, Nagy RJ, Lanman RB, Solovieff N, He W, Miller M, Su F, Shyr Y, Mayer IA, Balko JM, Arteaga CL
(2019) Nat Commun 10: 1373
MeSH Terms: Aminopyridines, Animals, Antineoplastic Agents, Hormonal, Antineoplastic Combined Chemotherapy Protocols, Breast Neoplasms, Circulating Tumor DNA, Cyclin D1, Cyclin-Dependent Kinase 4, Cyclin-Dependent Kinase 6, Drug Resistance, Neoplasm, Female, Fulvestrant, High-Throughput Nucleotide Sequencing, Humans, MCF-7 Cells, Mice, Mutation, Naphthalenes, Piperazines, Progression-Free Survival, Proportional Hazards Models, Protein Kinase Inhibitors, Purines, Pyrazoles, Pyridines, Quinolines, Quinoxalines, Receptor, Fibroblast Growth Factor, Type 1, Receptor, Fibroblast Growth Factor, Type 2, Receptors, Estrogen, Signal Transduction, Xenograft Model Antitumor Assays
Added April 2, 2019
0 Communities
1 Members
0 Resources
32 MeSH Terms
Repurposing cabozantinib to GISTs: Overcoming multiple imatinib-resistant cKIT mutations including gatekeeper and activation loop mutants in GISTs preclinical models.
Lu T, Chen C, Wang A, Jiang Z, Qi Z, Hu Z, Hu C, Liu F, Wang W, Wu H, Wang B, Wang L, Qi S, Wu J, Wang W, Tang J, Yan H, Bai M, Liu Q, Liu J
(2019) Cancer Lett 447: 105-114
MeSH Terms: Anilides, Antineoplastic Agents, Cell Line, Tumor, Drug Repositioning, Drug Resistance, Neoplasm, Gastrointestinal Stromal Tumors, Humans, Imatinib Mesylate, Mutation, Proto-Oncogene Proteins c-kit, Pyridines
Added April 2, 2019
0 Communities
1 Members
0 Resources
11 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 of Tricyclic Triazolo- and Imidazopyridine Lactams as M Positive Allosteric Modulators.
Engers JL, Bender AM, Kalbfleisch JJ, Cho HP, Lingenfelter KS, Luscombe VB, Han C, Melancon BJ, Blobaum AL, Dickerson JW, Rook JM, Niswender CM, Emmitte KA, Conn PJ, Lindsley CW
(2019) ACS Chem Neurosci 10: 1035-1042
MeSH Terms: Allosteric Regulation, Animals, Drug Discovery, Humans, Imidazoles, Lactams, Mice, Muscarinic Agonists, Pyridines, Rats, Receptor, Muscarinic M1
Added March 3, 2020
0 Communities
2 Members
0 Resources
11 MeSH Terms
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu positive allosteric modulators that mitigate CYP1A2 induction liability.
Engers DW, Bollinger SR, Engers JL, Panarese JD, Breiner MM, Gregro A, Blobaum AL, Bronson JJ, Wu YJ, Macor JE, Rodriguez AL, Zamorano R, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
(2018) Bioorg Med Chem Lett 28: 2641-2646
MeSH Terms: Allosteric Regulation, Animals, Antiparkinson Agents, Cytochrome P-450 CYP1A2, Cytochrome P-450 CYP1A2 Inducers, Drug Discovery, Enzyme Induction, Humans, Pyrazoles, Pyridines, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Therapeutic endocannabinoid augmentation for mood and anxiety disorders: comparative profiling of FAAH, MAGL and dual inhibitors.
Bedse G, Bluett RJ, Patrick TA, Romness NK, Gaulden AD, Kingsley PJ, Plath N, Marnett LJ, Patel S
(2018) Transl Psychiatry 8: 92
MeSH Terms: Amidohydrolases, Animals, Anti-Anxiety Agents, Anxiety Disorders, Behavior, Animal, Benzodioxoles, Body Temperature, Brain, Carbamates, Endocannabinoids, Female, Locomotion, Male, Maze Learning, Mice, Inbred C57BL, Mice, Inbred ICR, Monoacylglycerol Lipases, Piperazines, Piperidines, Pyridines, Stress, Psychological
Added April 12, 2019
0 Communities
1 Members
0 Resources
MeSH Terms