Indole scaffolds as a promising class of the aryl hydrocarbon receptor ligands

Synthesis and biological evaluation of FICZ analogues as agonists of aryl hydrocarbon receptor

(2020) Hao Wu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Modulation of lymphocyte-mediated tissue repair by rational design of heterocyclic aryl hydrocarbon receptor agonists

(2020) Jiaxuan Chen et al.   Science Advances

Targeting the pregnane X receptor using microbial metabolite mimicry

(2020) Zdeněk Dvořák et al.   EMBO Molecular Medicine

Antimigraine Drug Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor that Induces CYP1A1 in Hepatic and Intestinal Cells

(2020) Barbora Vyhlídalová et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Gut Microbial Catabolites of Tryptophan Are Ligands and Agonists of the Aryl Hydrocarbon Receptor: A Detailed Characterization

(2020) Barbora Vyhlídalová et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Acyl glucuronide reactivity in perspective

(2020) Peter R. Bradshaw et al.   DRUG DISCOVERY TODAY

How the AHR Became Important in Intestinal Homeostasis—A Diurnal FICZ/AHR/CYP1A1 Feedback Controls Both Immunity and Immunopathology

(2020) Agneta Rannug   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Drug Induced Liver Injury (DILI). Mechanisms and Medicinal Chemistry Avoidance/Mitigation Strategies

(2020) Bryan H. Norman   JOURNAL OF MEDICINAL CHEMISTRY

WEAK MICROBIAL METABOLITES: A TREASURE TROVE FOR USING BIOMIMICRY TO DISCOVER AND OPTIMIZE DRUGS

(2020) Zdenek Dvorak et al.   MOLECULAR PHARMACOLOGY

AHR is a Zika virus host factor and a candidate target for antiviral therapy

(2020) Federico Giovannoni et al.   NATURE NEUROSCIENCE

Intestinal microbiota-derived tryptophan metabolites are predictive of Ah receptor activity

(2020) Fangcong Dong et al.   Gut Microbes

Extended Multicomponent Reactions with Indole Aldehydes. Access to Unprecedented Polyheterocyclic Scaffolds, Ligands of the Aryl Hydrocarbon Receptor

(2020) Rodolfo Lavilla et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Drug Mimicry: Promiscuous Receptors PXR and AhR, and Microbial Metabolite Interactions in the Intestine

(2020) Zdeněk Dvořák et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Targeting the aryl hydrocarbon receptor with a novel set of triarylmethanes

(2020) Elizabeth Goya-Jorge et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Tryptophan Metabolism as a Pharmacological Target

(2020) Morgane Modoux et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Identification of an irreversible PPARγ antagonist with potent anticancer activity

(2020) Youyi Peng et al.   Pharmacology Research & Perspectives

Medicinal chemistry of indole derivatives: Current to future therapeutic prospectives

(2019) Archana Kumari et al.   BIOORGANIC CHEMISTRY

A Biomimetic, One-Step Transformation of Simple Indolic Compounds to Malassezia-Related Alkaloids with High AhR Potency and Efficacy

(2019) Nikitia Mexia et al.   CHEMICAL RESEARCH IN TOXICOLOGY

The aryl hydrocarbon receptor (AhR) as a breast cancer drug target

(2019) Jennifer R. Baker et al.   MEDICINAL RESEARCH REVIEWS

Regulation of the Immune Response by the Aryl Hydrocarbon Receptor

(2018) Cristina Gutiérrez-Vázquez et al.   IMMUNITY

A Phase 2, Randomized Dose-Finding Study of Tapinarof (GSK2894512 Cream) for the Treatment of Atopic Dermatitis

(2018) Johnny Peppers et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

Methylindoles and Methoxyindoles are Agonists and Antagonists of Human Aryl Hydrocarbon Receptor

(2018) Martina Stepankova et al.   MOLECULAR PHARMACOLOGY

The Environmental Sensor AHR Protects from Inflammatory Damage by Maintaining Intestinal Stem Cell Homeostasis and Barrier Integrity

(2018) Amina Metidji et al.   IMMUNITY

Microbial tryptophan catabolites in health and disease

(2018) Henrik M. Roager et al.   Nature Communications

A Phase 2, Randomized Dose-Finding Study of Tapinarof (GSK2894512 Cream) for the Treatment of Plaque Psoriasis

(2018) Kevin Robbins et al.   JOURNAL OF THE AMERICAN ACADEMY OF DERMATOLOGY

The Aryl Hydrocarbon Receptor Pathway Defines the Time Frame for Restorative Neurogenesis

(2018) Rossella Di Giaimo et al.   Cell Reports

Trace derivatives of kynurenine potently activate the aryl hydrocarbon receptor (AHR)

(2017) Seung-Hyeon Seok et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Short Chain Fatty Acids Enhance Aryl Hydrocarbon (Ah) Responsiveness in Mouse Colonocytes and Caco-2 Human Colon Cancer Cells

(2017) Un-Ho Jin et al.   Scientific Reports

Aryl hydrocarbon receptor activation and CYP1A induction by cooked food-derived carcinogenic heterocyclic amines in human HepG2 cell lines

(2016) Masashi Sekimoto et al.   FOOD AND CHEMICAL TOXICOLOGY

The aryl hydrocarbon receptor AhR links atopic dermatitis and air pollution via induction of the neurotrophic factor artemin

(2016) Takanori Hidaka et al.   NATURE IMMUNOLOGY

A novel AhR ligand, 2AI, protects the retina from environmental stress

(2016) Mark A. Gutierrez et al.   Scientific Reports

Skatole (3-Methylindole) Is a Partial Aryl Hydrocarbon Receptor Agonist and Induces CYP1A1/2 and CYP1B1 Expression in Primary Human Hepatocytes

(2016) Martin Krøyer Rasmussen et al.   PLoS One

Pityriazepin and other potent AhR ligands isolated from Malassezia furfur yeast

(2015) Nikitia Mexia et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS

Naturally Occurring Marine Brominated Indoles Are Aryl Hydrocarbon Receptor Ligands/Agonists

(2015) Danica E. DeGroot et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Evidence for New Light-Independent Pathways for Generation of the Endogenous Aryl Hydrocarbon Receptor Agonist FICZ

(2015) Anna Smirnova et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Characterization and Biological Potency of Mono- to Tetra-Halogenated Carbazoles

(2015) Nicole Riddell et al.   ENVIRONMENTAL SCIENCE & TECHNOLOGY

Studies on the Synthesis of Indothiazinone and Its Derivatives via Direct 3-Acylation of Indole

(2015) Sugyeong Kwon et al.   SYNTHETIC COMMUNICATIONS

Analysis of Glycogen Synthase Kinase Inhibitors That Regulate Cytochrome P450 Expression in Primary Human Hepatocytes by Activation of β-Catenin, Aryl Hydrocarbon Receptor and Pregnane X Receptor Signaling

(2015) Philippe Briolotti et al.   TOXICOLOGICAL SCIENCES

Adaptation of the human aryl hydrocarbon receptor to sense microbiota-derived indoles

(2015) Troy D. Hubbard et al.   Scientific Reports

Synthesis and biological evaluation of 2,3′-diindolylmethanes as agonists of aryl hydrocarbon receptor

(2014) Gabrielle N. Winston-McPherson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In vivoeffects of the pure aryl hydrocarbon receptor antagonist GNF-351 after oral administration are limited to the gastrointestinal tract

(2014) Zhong-Ze Fang et al.   BRITISH JOURNAL OF PHARMACOLOGY

Indothiazinone, an Indolyl Thiazolyl Ketone from a Novel Myxobacterium Belonging to the Sorangiineae

(2014) Rolf Jansen et al.   JOURNAL OF NATURAL PRODUCTS

Sunitinib, a tyrosine kinase inhibitor, induces cytochrome P450 1A1 gene in human breast cancer MCF7 cells through ligand-independent aryl hydrocarbon receptor activation

(2013) Zaid H. Maayah et al.   ARCHIVES OF TOXICOLOGY

Malassezia Yeasts Produce a Collection of Exceptionally Potent Activators of the Ah (Dioxin) Receptor Detected in Diseased Human Skin

(2013) Prokopios Magiatis et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

Endogenous and Exogenous Ligands of Aryl Hydrocarbon Receptor: Current State of Art

(2011) Lucie Stejskalova et al.   CURRENT DRUG METABOLISM

Aryl Hydrocarbon Receptor-Induced Signals Up-regulate IL-22 Production and Inhibit Inflammation in the Gastrointestinal Tract

(2011) Ivan Monteleone et al.   GASTROENTEROLOGY

Identification of a High-Affinity Ligand That Exhibits Complete Aryl Hydrocarbon Receptor Antagonism

(2011) K. J. Smith et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Regulation of dioxin receptor function by different beta-carboline alkaloids

(2010) Thomas Haarmann-Stemmann et al.   ARCHIVES OF TOXICOLOGY

TSU-16, (Z)-3-[(2,4-dimethylpyrrol-5-yl)methylidenyl]-2-indolinone, is a potent activator of aryl hydrocarbon receptor and increases CYP1A1 and CYP1A2 expression in human hepatocytes

(2010) Kazuaki Matsuoka-Kawano et al.   CHEMICO-BIOLOGICAL INTERACTIONS

A Novel Role for the Dioxin Receptor in Fatty Acid Metabolism and Hepatic Steatosis

(2010) Jung Hoon Lee et al.   GASTROENTEROLOGY

Aryl Hydrocarbon Receptor Antagonists Promote the Expansion of Human Hematopoietic Stem Cells

(2010) Anthony E. Boitano et al.   SCIENCE

Kynurenic Acid Is a Potent Endogenous Aryl Hydrocarbon Receptor Ligand that Synergistically Induces Interleukin-6 in the Presence of Inflammatory Signaling

(2010) Brett C. DiNatale et al.   TOXICOLOGICAL SCIENCES

The Uremic Toxin 3-Indoxyl Sulfate Is a Potent Endogenous Agonist for the Human Aryl Hydrocarbon Receptor

(2009) Jennifer C. Schroeder et al.   BIOCHEMISTRY

Synthesis and biological evaluation of fused thio- and selenopyrans as new indolocarbazole analogues with aryl hydrocarbon receptor affinity

(2009) Emma Wincent et al.   BIOORGANIC & MEDICINAL CHEMISTRY

d-Amino Acid Oxidase Generates Agonists of the Aryl Hydrocarbon Receptor fromd-Tryptophan

(2009) Linh P. Nguyen et al.   CHEMICAL RESEARCH IN TOXICOLOGY

Structural Identification of Diindole Agonists of the Aryl Hydrocarbon Receptor Derived from Degradation of Indole-3-pyruvic Acid

(2009) Goutam Chowdhury et al.   CHEMICAL RESEARCH IN TOXICOLOGY

The Glycogen Synthase Kinase Inhibitor 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763) Is a Partial Agonist of the Aryl Hydrocarbon Receptor

(2009) A. Braeuning et al.   DRUG METABOLISM AND DISPOSITION

From Nature to Drug Discovery: The Indole Scaffold as a ‘Privileged Structure’

(2009) Fernando de Sa Alves et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

The Suggested Physiologic Aryl Hydrocarbon Receptor Activator and Cytochrome P4501 Substrate 6-Formylindolo[3,2-b]carbazole Is Present in Humans

(2008) Emma Wincent et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Antagonistic and agonistic effects of indigoids on the transformation of an aryl hydrocarbon receptor

(2007) Shin Nishiumi et al.   ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS