ArticleMolecular pharmacology2018
Methylindoles and Methoxyindoles are Agonists and Antagonists of Human Aryl Hydrocarbon Receptor.
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Article in Molecular pharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17citing papers in PubMed
2.2field-weighted citation impact, top 15% of its field
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Who cites it
17 citing papers in PubMed, 39 citations in OpenAlex.
- Discrete interplay of gut microbiota L-tryptophan metabolites in host biology and disease.Molecular and cellular biochemistry · 2024Review
- TCDD and CH223191 Alter T Cell Balance but Fail to Induce Anti-Inflammatory Response in Adult Lupus Mice.ImmunoHorizons · 2024Article
- Jasmone Is a Ligand-Selective Allosteric Antagonist of Aryl Hydrocarbon Receptor (AhR).International journal of molecular sciences · 2023Article
- Microbiota-produced indole metabolites disrupt mitochondrial function and inhibit Cryptosporidium parvum growth.Cell reports · 2023Article
- Microbiota produced indole metabolites disrupt host cell mitochondrial energy production and inhibitbioRxiv : the preprint server for biology · 2023Article
- Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice.Nature communications · 2023Article
- Natural Product Skatole Ameliorates Lipotoxicity-Induced Multiple Hepatic Damage under Hyperlipidemic Conditions in Hepatocytes.Nutrients · 2023Article
- The Impact of Indoles Activating the Aryl Hydrocarbon Receptor on Androgen Receptor Activity in the 22Rv1 Prostate Cancer Cell Line.International journal of molecular sciences · 2022Article
- Mixture Effects of Tryptophan Intestinal Microbial Metabolites on Aryl Hydrocarbon Receptor Activity.International journal of molecular sciences · 2022Article
- High-fat diet and alcohol induced-mice could cause colonic injury through molecular mechanisms of endogenous toxins.Toxicology research · 2022Article
- Characterization of marine-derived halogenated indoles as ligands of the aryl hydrocarbon receptor.Toxicology reports · 2022Article
- Diverse roles of microbial indole compounds in eukaryotic systems.Biological reviews of the Cambridge Philosophical Society · 2021Review
- Impact of Bacterial Metabolites on Gut Barrier Function and Host Immunity: A Focus on Bacterial Metabolism and Its Relevance for Intestinal Inflammation.Frontiers in immunology · 2021Review
- Antimigraine Drug Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells.International journal of molecular sciences · 2020Article
- Gut Microbial Catabolites of Tryptophan Are Ligands and Agonists of the Aryl Hydrocarbon Receptor: A Detailed Characterization.International journal of molecular sciences · 2020Article
- Mono-methylindoles induce CYP1A genes and inhibit CYP1A1 enzyme activity in human hepatocytes and HepaRG cells.Toxicology letters · 2019Article
- Article
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 2 countries.
Martina StepankovaRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.).
Iveta BartonkovaRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.).
Eva JiskrovaRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.).
Radim VrzalRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.).
Sridhar ManiRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.) moulin@email.cz sridhar.mani@einstein.yu.edu.
Sandhya KortagereRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.).
Zdenek DvorakRegional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Olomouc, Czech Republic (M.S., I.B., E.J., R.V., Z.D.); Departments of Genetics and Medicine, Albert Einstein College of Medicine, Bronx, New York (S.M.); and Department of Microbiology and Immunology, Drexel University College of Medicine, Philadelphia, Pennsylvania (S.K.) moulin@email.cz sridhar.mani@einstein.yu.edu.
Albert Einstein College of Medicine · USDrexel University · USPalacký University Olomouc · CZRegional Centre of Advanced Technologies and Materials · CZ
Funding
WORD PROCESSORP30CA013330 · NCI · YESHIVA UNIVERSITY · PI THOMAS E ROHAN · 1985 to 2026
$111.2MTranslational Research CoreP30DK020541 · NIDDK · ALBERT EINSTEIN COLLEGE OF MEDICINE, INC · PI STREAMSON C CHUA · 2015 to 2026
$27.7MSpecial Animal CoreP30DK041296 · NIDDK · YESHIVA UNIVERSITY · PI WOLKOFF, ALLAN W · 1989 to 2018
$22.9MChemical Modulation of Orphan Nuclear Receptor FunctionR01CA127231 · NCI · ALBERT EINSTEIN COLLEGE OF MEDICINE · PI MANI, SRIDHAR · 2009 to 2014
$1.6MDevelopment of Novel Drugs to Alleviate CPT-11 ToxicityR01CA161879 · NCI · ALBERT EINSTEIN COLLEGE OF MEDICINE, INC · PI MANI, SRIDHAR, REDINBO, MATTHEW R · 2012 to 2016
$1.6MPregnane X Receptor (PXR) Antagonists for Non-Alcoholic Fatty Liver DiseaseR43DK105694 · NIDDK · FOX CHASE CHEMICAL DIVERSITY CENTER, INC · PI WROBEL, JAY EDWARD · 2015 to 2015
$300kNCI NIH HHS P30 CA013330NCI NIH HHS R01 CA127231NCI NIH HHS R01 CA161879NIDDK NIH HHS P30 DK020541NIDDK NIH HHS P30 DK041296NIDDK NIH HHS R43 DK105694
Abstract
Novel methylindoles were identified as endobiotic and xenobiotic ligands of the human aryl hydrocarbon receptor (AhR). We examined the effects of 22 methylated and methoxylated indoles on the transcriptional activity of AhRs. Employing reporter gene assays in AZ-AHR transgenic cells, we determined full agonist, partial agonist, or antagonist activities of tested compounds, having substantially variable EC
Indexed as
Basic Helix-Loop-Helix ProteinsCell Line, TumorCytochrome P-450 CYP1A1Genes, ReporterHep G2 CellsHumansIndolesLigandsPromoter Regions, GeneticReceptors, Aryl HydrocarbonRNA, MessengerAHR protein, humanBasic Helix-Loop-Helix ProteinsCytochrome P-450 CYP1A1indoleIndolesLigandsReceptors, Aryl HydrocarbonRNA, Messenger
Identifiers
What OpenQuestion holds
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Registered trials
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.