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Results: 1 to 10 of 143

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Primary prevention of venous thromboembolism with apixaban for multiple myeloma patients receiving immunomodulatory agents.
Cornell RF, Goldhaber SZ, Engelhardt BG, Moslehi J, Jagasia M, Harrell S, Rubinstein SM, Hall R, Wyatt H, Piazza G
(2020) Br J Haematol 190: 555-561
MeSH Terms: Aged, Comorbidity, Consolidation Chemotherapy, Factor Xa Inhibitors, Female, Hemorrhage, Humans, Immunologic Factors, Lenalidomide, Maintenance Chemotherapy, Male, Middle Aged, Multiple Myeloma, Myocardial Infarction, Pilot Projects, Proof of Concept Study, Prospective Studies, Pulmonary Embolism, Pyrazoles, Pyridones, Stroke, Thalidomide, Thrombophilia, Venous Thromboembolism, Venous Thrombosis
Added May 29, 2020
0 Communities
1 Members
0 Resources
25 MeSH Terms
Cardiovascular Toxicities Associated With Ibrutinib.
Salem JE, Manouchehri A, Bretagne M, Lebrun-Vignes B, Groarke JD, Johnson DB, Yang T, Reddy NM, Funck-Brentano C, Brown JR, Roden DM, Moslehi JJ
(2019) J Am Coll Cardiol 74: 1667-1678
MeSH Terms: Adverse Drug Reaction Reporting Systems, Aged, Aged, 80 and over, Cardiovascular Diseases, Databases, Factual, Female, Humans, Male, Mortality, Pharmacovigilance, Pyrazoles, Pyrimidines, Retrospective Studies
Added November 12, 2019
0 Communities
2 Members
0 Resources
13 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
Surveying heterocycles as amide bioisosteres within a series of mGlu NAMs: Discovery of VU6019278.
Reed CW, Washecheck JP, Quitlag MC, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW
(2019) Bioorg Med Chem Lett 29: 1211-1214
MeSH Terms: Allosteric Regulation, Amides, Animals, Central Nervous System, Hepatocytes, Heterocyclic Compounds, Inhibitory Concentration 50, Pyrazoles, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Glucose-mediated inhibition of calcium-activated potassium channels limits α-cell calcium influx and glucagon secretion.
Dickerson MT, Dadi PK, Altman MK, Verlage KR, Thorson AS, Jordan KL, Vierra NC, Amarnath G, Jacobson DA
(2019) Am J Physiol Endocrinol Metab 316: E646-E659
MeSH Terms: Alkanes, Animals, Apamin, Calcium, Calcium Channels, Calcium Channels, L-Type, Calcium Channels, P-Type, Calcium Channels, Q-Type, Endoplasmic Reticulum, Glucagon, Glucagon-Secreting Cells, Glucose, Mice, Mice, Transgenic, Patch-Clamp Techniques, Peptides, Potassium Channel Blockers, Potassium Channels, Calcium-Activated, Pyrazoles, Quinolinium Compounds
Added February 13, 2019
0 Communities
1 Members
0 Resources
20 MeSH Terms
Incidence of and risk factors for major haemorrhage in patients treated with ibrutinib: An integrated analysis.
Brown JR, Moslehi J, Ewer MS, O'Brien SM, Ghia P, Cymbalista F, Shanafelt TD, Fraser G, Rule S, Coutre SE, Dilhuydy MS, Cramer P, Jaeger U, Dreyling M, Byrd JC, Treon S, Liu EY, Chang S, Bista A, Vempati R, Boornazian L, Valentino R, Reddy V, Mahler M, Yang H, Graef T, Burger JA
(2019) Br J Haematol 184: 558-569
MeSH Terms: Aged, Female, Hematologic Neoplasms, Hemorrhage, Humans, Incidence, Male, Middle Aged, Pyrazoles, Pyrimidines, Randomized Controlled Trials as Topic, Risk Factors, Time Factors
Added December 13, 2018
0 Communities
1 Members
0 Resources
13 MeSH Terms
Analgesic Effects of the GIRK Activator, VU0466551, Alone and in Combination with Morphine in Acute and Persistent Pain Models.
Abney KK, Bubser M, Du Y, Kozek KA, Bridges TM, Linsdley CW, Daniels JS, Morrison RD, Wickman K, Hopkins CR, Jones CK, Weaver CD
(2019) ACS Chem Neurosci 10: 1294-1299
MeSH Terms: Analgesics, Animals, Disease Models, Animal, Dose-Response Relationship, Drug, Drug Therapy, Combination, Formaldehyde, G Protein-Coupled Inwardly-Rectifying Potassium Channels, HEK293 Cells, Hot Temperature, Humans, Male, Mice, Inbred C57BL, Morphine, Pain, Phenylurea Compounds, Pyrazoles
Added April 10, 2019
0 Communities
2 Members
0 Resources
16 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 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
The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine core.
Bertron JL, Cho HP, Garcia-Barrantes PM, Panarese JD, Salovich JM, Nance KD, Engers DW, Rook JM, Blobaum AL, Niswender CM, Stauffer SR, Conn PJ, Lindsley CW
(2018) Bioorg Med Chem Lett 28: 2175-2179
MeSH Terms: Animals, CHO Cells, Cricetulus, Drug Discovery, Humans, Molecular Structure, Morpholines, Pyrazoles, Rats, Receptor, Muscarinic M1, Structure-Activity Relationship
Added March 3, 2020
0 Communities
2 Members
0 Resources
MeSH Terms