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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
Induction of human cytochrome P450 3A enzymes in cultured placental cells by thalidomide and relevance to bioactivation and toxicity.
Murayama N, Kazuki Y, Satoh D, Arata K, Harada T, Shibata N, Guengerich FP, Yamazaki H
(2017) J Toxicol Sci 42: 343-348
MeSH Terms: Cells, Cultured, Cytochrome P-450 CYP3A, Enzyme Induction, Female, Humans, Liver, Oxidation-Reduction, Placenta, Pregnancy, Pregnane X Receptor, RNA, Messenger, Receptors, Steroid, Rifampin, Thalidomide
Added March 14, 2018
0 Communities
1 Members
0 Resources
14 MeSH Terms
Increased Helicobacter pylori-associated gastric cancer risk in the Andean region of Colombia is mediated by spermine oxidase.
Chaturvedi R, de Sablet T, Asim M, Piazuelo MB, Barry DP, Verriere TG, Sierra JC, Hardbower DM, Delgado AG, Schneider BG, Israel DA, Romero-Gallo J, Nagy TA, Morgan DR, Murray-Stewart T, Bravo LE, Peek RM, Fox JG, Woster PM, Casero RA, Correa P, Wilson KT
(2015) Oncogene 34: 3429-40
MeSH Terms: Adenocarcinoma, Adult, Animals, Cells, Cultured, Colombia, DNA Damage, Enzyme Induction, Gerbillinae, Helicobacter Infections, Helicobacter pylori, Humans, Hydrogen Peroxide, Male, Middle Aged, Oxidative Stress, Oxidoreductases Acting on CH-NH Group Donors, Risk Factors, Stomach Neoplasms
Added January 20, 2015
0 Communities
6 Members
0 Resources
18 MeSH Terms
Activation of MAPK and FoxO by manganese (Mn) in rat neonatal primary astrocyte cultures.
Exil V, Ping L, Yu Y, Chakraborty S, Caito SW, Wells KS, Karki P, Lee E, Aschner M
(2014) PLoS One 9: e94753
MeSH Terms: Active Transport, Cell Nucleus, Animals, Animals, Newborn, Astrocytes, Cell Nucleus, Cells, Cultured, Enzyme Activation, Enzyme Induction, Forkhead Box Protein O3, Forkhead Transcription Factors, Manganese, Mitogen-Activated Protein Kinases, Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha, Phosphorylation, Proto-Oncogene Proteins c-akt, Pyrrolidonecarboxylic Acid, Rats, Rats, Sprague-Dawley, Reactive Oxygen Species, Signal Transduction, Superoxide Dismutase, Thiazolidines, Time Factors, Transcription Factors
Added April 11, 2016
0 Communities
1 Members
0 Resources
24 MeSH Terms
Type 2 diabetes and congenital hyperinsulinism cause DNA double-strand breaks and p53 activity in β cells.
Tornovsky-Babeay S, Dadon D, Ziv O, Tzipilevich E, Kadosh T, Schyr-Ben Haroush R, Hija A, Stolovich-Rain M, Furth-Lavi J, Granot Z, Porat S, Philipson LH, Herold KC, Bhatti TR, Stanley C, Ashcroft FM, In't Veld P, Saada A, Magnuson MA, Glaser B, Dor Y
(2014) Cell Metab 19: 109-21
MeSH Terms: Animals, Biomarkers, Calcineurin, Cell Death, Cell Proliferation, Congenital Hyperinsulinism, DNA Breaks, Double-Stranded, Diabetes Mellitus, Type 2, Disease Models, Animal, Enzyme Activation, Enzyme Induction, Fasting, Glucagon-Like Peptide 1, Glucokinase, Glucose, Humans, Insulin-Secreting Cells, Membrane Potentials, Mice, Transgenes, Tumor Suppressor Protein p53
Added February 11, 2014
2 Communities
1 Members
1 Resources
21 MeSH Terms
Alkaline phosphatases contribute to uterine receptivity, implantation, decidualization, and defense against bacterial endotoxin in hamsters.
Lei W, Nguyen H, Brown N, Ni H, Kiffer-Moreira T, Reese J, Millán JL, Paria BC
(2013) Reproduction 146: 419-32
MeSH Terms: Alkaline Phosphatase, Animals, Cricetinae, Decidua, Embryo Implantation, Endometrium, Enzyme Induction, Escherichia coli Infections, Estrous Cycle, Female, Immunity, Innate, Isoenzymes, Lipopolysaccharides, Mesocricetus, Ovariectomy, Phosphorylation, Placentation, Pregnancy, RNA, Messenger, Uterus
Added April 9, 2015
0 Communities
1 Members
0 Resources
20 MeSH Terms
Increased dietary sodium induces COX2 expression by activating NFκB in renal medullary interstitial cells.
He W, Zhang M, Zhao M, Davis LS, Blackwell TS, Yull F, Breyer MD, Hao CM
(2014) Pflugers Arch 466: 357-367
MeSH Terms: Animals, Benzamides, Cyclooxygenase 2, Enzyme Induction, Kidney Medulla, Male, Mice, Mice, Inbred C57BL, NF-kappa B, Sodium, Sodium Chloride, Dietary
Added March 7, 2014
1 Communities
2 Members
0 Resources
11 MeSH Terms
β-Cell-specific protein kinase A activation enhances the efficiency of glucose control by increasing acute-phase insulin secretion.
Kaihara KA, Dickson LM, Jacobson DA, Tamarina N, Roe MW, Philipson LH, Wicksteed B
(2013) Diabetes 62: 1527-36
MeSH Terms: Animals, Crosses, Genetic, Cyclic AMP, Cyclic AMP-Dependent Protein Kinases, Enzyme Induction, Exenatide, Glucose Clamp Technique, Hyperglycemia, Hypoglycemic Agents, Insulin, Insulin Secretion, Insulin-Secreting Cells, Kinetics, Mice, Mutant Proteins, Patch-Clamp Techniques, Peptides, Phosphorylation, Protein Processing, Post-Translational, Protein Subunits, Second Messenger Systems, Up-Regulation, Venoms
Added February 12, 2015
0 Communities
1 Members
0 Resources
23 MeSH Terms
Brain-selective overexpression of angiotensin-converting enzyme 2 attenuates sympathetic nerve activity and enhances baroreflex function in chronic heart failure.
Xiao L, Gao L, Lazartigues E, Zucker IH
(2011) Hypertension 58: 1057-65
MeSH Terms: Angiotensin I, Angiotensin II, Angiotensin-Converting Enzyme 2, Animals, Baroreflex, Enzyme Induction, Heart Failure, Humans, Male, Medulla Oblongata, Mice, Mice, Knockout, Myocardial Ischemia, Nerve Tissue Proteins, Nitric Oxide, Norepinephrine, Organ Specificity, Peptide Fragments, Peptidyl-Dipeptidase A, Proto-Oncogene Mas, Proto-Oncogene Proteins, Receptors, Angiotensin, Receptors, G-Protein-Coupled, Recombinant Fusion Proteins, Reflex, Abnormal, Sympathetic Nervous System
Added August 5, 2014
0 Communities
1 Members
0 Resources
26 MeSH Terms
Immune evasion by Helicobacter pylori is mediated by induction of macrophage arginase II.
Lewis ND, Asim M, Barry DP, de Sablet T, Singh K, Piazuelo MB, Gobert AP, Chaturvedi R, Wilson KT
(2011) J Immunol 186: 3632-41
MeSH Terms: Animals, Arginase, Disease Models, Animal, Enzyme Induction, Helicobacter Infections, Helicobacter pylori, Immune Evasion, Intestinal Mucosa, Macrophages, Male, Mice, Mice, Inbred C57BL, Mice, Knockout, Nitric Oxide Synthase Type II
Added March 5, 2014
0 Communities
3 Members
0 Resources
14 MeSH Terms