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Results: 1 to 10 of 54

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The antifungal drug isavuconazole inhibits the replication of human cytomegalovirus (HCMV) and acts synergistically with anti-HCMV drugs.
Mercorelli B, Celegato M, Luganini A, Gribaudo G, Lepesheva GI, Loregian A
(2021) Antiviral Res 189: 105062
MeSH Terms: Antifungal Agents, Antiviral Agents, Cell Line, Cytomegalovirus, Cytomegalovirus Infections, Drug Repositioning, Drug Resistance, Viral, Drug Synergism, Drug Therapy, Combination, Humans, Nitriles, Pyridines, Sterol 14-Demethylase, Triazoles, Virus Replication
Added July 2, 2021
0 Communities
1 Members
0 Resources
15 MeSH Terms
The Clinically Approved Antifungal Drug Posaconazole Inhibits Human Cytomegalovirus Replication.
Mercorelli B, Luganini A, Celegato M, Palù G, Gribaudo G, Lepesheva GI, Loregian A
(2020) Antimicrob Agents Chemother 64:
MeSH Terms: Antifungal Agents, Antiviral Agents, Cytomegalovirus, Cytomegalovirus Infections, Ganciclovir, Humans, Pharmaceutical Preparations, Triazoles, Virus Replication
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
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 an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1 H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962).
Reed CW, Yohn SE, Washecheck JP, Roenfanz HF, Quitalig MC, Luscombe VB, Jenkins MT, Rodriguez AL, Engers DW, Blobaum AL, Conn PJ, Niswender CM, Lindsley CW
(2019) J Med Chem 62: 1690-1695
MeSH Terms: Allosteric Regulation, Animals, Anti-Anxiety Agents, Benzamides, Brain, Drug Discovery, Male, Mice, Inbred C57BL, Molecular Structure, Rats, Sprague-Dawley, Receptors, Metabotropic Glutamate, Structure-Activity Relationship, Triazoles
Added March 3, 2020
0 Communities
1 Members
0 Resources
13 MeSH Terms
AXL Mediates Esophageal Adenocarcinoma Cell Invasion through Regulation of Extracellular Acidification and Lysosome Trafficking.
Maacha S, Hong J, von Lersner A, Zijlstra A, Belkhiri A
(2018) Neoplasia 20: 1008-1022
MeSH Terms: Adenocarcinoma, Animals, Benzocycloheptenes, Biological Transport, Cathepsin B, Cell Line, Tumor, Chick Embryo, Chorioallantoic Membrane, Epithelial-Mesenchymal Transition, Esophageal Neoplasms, Gene Expression Regulation, Neoplastic, Humans, Hydrogen-Ion Concentration, Lactates, Lysosomes, Monocarboxylic Acid Transporters, Proto-Oncogene Proteins, Receptor Protein-Tyrosine Kinases, Symporters, Triazoles
Added April 10, 2019
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
Oestrogen inhibition reverses pulmonary arterial hypertension and associated metabolic defects.
Chen X, Austin ED, Talati M, Fessel JP, Farber-Eger EH, Brittain EL, Hemnes AR, Loyd JE, West J
(2017) Eur Respir J 50:
MeSH Terms: Anastrozole, Animals, Bone Morphogenetic Protein Receptors, Type II, Disease Models, Animal, Echocardiography, Estradiol, Estrogen Antagonists, Female, Fulvestrant, Hemodynamics, Humans, Hypertension, Pulmonary, Insulin Resistance, Lung, Mice, Mice, Knockout, Mutation, Nitriles, Signal Transduction, Tamoxifen, Triazoles
Added March 14, 2018
0 Communities
3 Members
0 Resources
21 MeSH Terms
Unexpected Efficacy of a Novel Sodium Channel Modulator in Dravet Syndrome.
Anderson LL, Hawkins NA, Thompson CH, Kearney JA, George AL
(2017) Sci Rep 7: 1682
MeSH Terms: Action Potentials, Animals, Epilepsies, Myoclonic, Ion Channel Gating, Mice, Inbred C57BL, Mice, Knockout, NAV1.1 Voltage-Gated Sodium Channel, NAV1.6 Voltage-Gated Sodium Channel, Neurons, Pyramidal Cells, Pyridines, Seizures, Survival Analysis, Triazoles
Added October 2, 2018
1 Communities
0 Members
0 Resources
14 MeSH Terms
Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity.
Hargrove TY, Garvey EP, Hoekstra WJ, Yates CM, Wawrzak Z, Rachakonda G, Villalta F, Lepesheva GI
(2017) Antimicrob Agents Chemother 61:
MeSH Terms: Antifungal Agents, Aspergillus fumigatus, Candida albicans, Drugs, Investigational, Fluconazole, Ketoconazole, Microbial Sensitivity Tests, Pyridines, Sterol 14-Demethylase, Tetrazoles, Triazoles, Voriconazole
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
High-Resolution Mapping of RNA Polymerases Identifies Mechanisms of Sensitivity and Resistance to BET Inhibitors in t(8;21) AML.
Zhao Y, Liu Q, Acharya P, Stengel KR, Sheng Q, Zhou X, Kwak H, Fischer MA, Bradner JE, Strickland SA, Mohan SR, Savona MR, Venters BJ, Zhou MM, Lis JT, Hiebert SW
(2016) Cell Rep 16: 2003-16
MeSH Terms: Antineoplastic Agents, Azepines, Cell Line, Tumor, Chromosomes, Human, Pair 21, Chromosomes, Human, Pair 8, Clustered Regularly Interspaced Short Palindromic Repeats, DNA-Directed RNA Polymerases, Drug Resistance, Neoplasm, Enhancer Elements, Genetic, Gene Expression Regulation, Leukemic, High-Throughput Nucleotide Sequencing, Humans, Leukemia, Myeloid, Acute, MicroRNAs, Multigene Family, Myeloid Cell Leukemia Sequence 1 Protein, Promoter Regions, Genetic, Protein Isoforms, Proteins, Proto-Oncogene Proteins c-kit, Transcription, Genetic, Translocation, Genetic, Triazoles
Added April 6, 2017
0 Communities
1 Members
0 Resources
23 MeSH Terms