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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 254

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Sterol 14α-Demethylase Structure-Based Optimization of Drug Candidates for Human Infections with the Protozoan Trypanosomatidae.
Friggeri L, Hargrove TY, Rachakonda G, Blobaum AL, Fisher P, de Oliveira GM, da Silva CF, Soeiro MNC, Nes WD, Lindsley CW, Villalta F, Guengerich FP, Lepesheva GI
(2018) J Med Chem 61: 10910-10921
MeSH Terms: 14-alpha Demethylase Inhibitors, Antiprotozoal Agents, Chagas Disease, Drug Design, Drug Stability, Humans, Microsomes, Models, Molecular, Protein Conformation, Sterol 14-Demethylase, Trypanosoma cruzi
Added July 2, 2021
0 Communities
1 Members
0 Resources
MeSH Terms
Discovery and Optimization of Potent and CNS Penetrant M-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.
Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW
(2018) ACS Chem Neurosci 9: 1572-1581
MeSH Terms: Allosteric Regulation, Amides, Animals, Brain, Cholinergic Agents, Drug Discovery, Humans, Male, Microsomes, Liver, Molecular Structure, Piperidines, Rats, Sprague-Dawley, Receptors, Muscarinic, Structure-Activity Relationship
Added March 3, 2020
0 Communities
1 Members
0 Resources
MeSH Terms
Sulfenylation of Human Liver and Kidney Microsomal Cytochromes P450 and Other Drug-Metabolizing Enzymes as a Response to Redox Alteration.
Albertolle ME, Phan TTN, Pozzi A, Guengerich FP
(2018) Mol Cell Proteomics 17: 889-900
MeSH Terms: Animals, Biocatalysis, Cysteine, Cytochrome P-450 Enzyme System, Humans, Hydrogen Peroxide, Kidney, Mice, Transgenic, Microsomes, Liver, Oxidation-Reduction, Pharmaceutical Preparations, Recombinant Proteins, Staining and Labeling, Sulfenic Acids, Sulfhydryl Compounds
Added March 14, 2018
1 Communities
1 Members
0 Resources
15 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
Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators.
Wieting JM, Vadukoot AK, Sharma S, Abney KK, Bridges TM, Daniels JS, Morrison RD, Wickman K, Weaver CD, Hopkins CR
(2017) ACS Chem Neurosci 8: 1873-1879
MeSH Terms: Acetamides, Animals, Brain, G Protein-Coupled Inwardly-Rectifying Potassium Channels, HEK293 Cells, Humans, Liver, Membrane Transport Modulators, Mice, Microsomes, Liver, Molecular Structure, Pyrazoles, Structure-Activity Relationship
Added April 3, 2018
0 Communities
1 Members
0 Resources
13 MeSH Terms
Metabolic profiles of pomalidomide in human plasma simulated with pharmacokinetic data in control and humanized-liver mice.
Shimizu M, Suemizu H, Mitsui M, Shibata N, Guengerich FP, Yamazaki H
(2017) Xenobiotica 47: 844-848
MeSH Terms: Angiogenesis Inhibitors, Animals, Cytochrome P-450 Enzyme System, Glucuronides, Hepatocytes, Humans, Liver, Metabolome, Mice, Microsomes, Liver, Thalidomide
Added March 14, 2018
0 Communities
1 Members
0 Resources
11 MeSH Terms
Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).
Gogliotti RD, Blobaum AL, Morrison RM, Daniels JS, Salovich JM, Cheung YY, Rodriguez AL, Loch MT, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR
(2016) Bioorg Med Chem Lett 26: 2984-2987
MeSH Terms: Allosteric Regulation, Animals, Microsomes, Liver, Picolinic Acids, Pyrroles, Rats, Receptors, Metabotropic Glutamate, Structure-Activity Relationship, Sulfonamides, Triazoles
Added April 6, 2017
0 Communities
2 Members
0 Resources
10 MeSH Terms
Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core.
Wood MR, Noetzel MJ, Engers JL, Bollinger KA, Melancon BJ, Tarr JC, Han C, West M, Gregro AR, Lamsal A, Chang S, Ajmera S, Smith E, Chase P, Hodder PS, Bubser M, Jones CK, Hopkins CR, Emmitte KA, Niswender CM, Wood MW, Duggan ME, Conn PJ, Bridges TM, Lindsley CW
(2016) Bioorg Med Chem Lett 26: 3029-3033
MeSH Terms: Allosteric Regulation, Animals, Brain, Humans, Microsomes, Liver, Piperidines, Pyrimidines, Quinazolines, Rats, Receptor, Muscarinic M4, Structure-Activity Relationship, Thiophenes
Added April 6, 2017
0 Communities
3 Members
0 Resources
12 MeSH Terms
Increased lethality and defective pulmonary clearance of Streptococcus pneumoniae in microsomal prostaglandin E synthase-1-knockout mice.
Dolan JM, Weinberg JB, O'Brien E, Abashian A, Procario MC, Aronoff DM, Crofford LJ, Peters-Golden M, Ward L, Mancuso P
(2016) Am J Physiol Lung Cell Mol Physiol 310: L1111-20
MeSH Terms: Animals, Cyclooxygenase 1, Cytokines, Dinoprostone, Female, Immunity, Innate, Lung, Macrophages, Alveolar, Membrane Proteins, Mice, Inbred C57BL, Mice, Knockout, Microsomes, Nitric Oxide, Pneumonia, Pneumococcal, Streptococcus pneumoniae
Added June 2, 2017
0 Communities
2 Members
0 Resources
15 MeSH Terms
Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.
Garcia-Barrantes PM, Cho HP, Blobaum AL, Niswender CM, Conn PJ, Lindsley CW
(2015) Bioorg Med Chem Lett 25: 5107-10
MeSH Terms: Allosteric Regulation, Animals, Brain, Coumarins, Furans, Humans, Microsomes, Liver, Phthalimides, Rats, Receptors, Metabotropic Glutamate, Stereoisomerism, Structure-Activity Relationship
Added February 18, 2016
0 Communities
2 Members
0 Resources
12 MeSH Terms