Targeting the Aryl Hydrocarbon Receptor with Microbial Metabolite Mimics Alleviates Experimental Colitis in Mice

Journal of Medicinal Chemistry
2022.0

Abstract

Targeting the aryl hydrocarbon receptor (AhR) is an emerging therapeutic strategy for multiple diseases (e.g., inflammatory bowel disease). <i>Thermosporothrix hazakensis</i> microbial metabolite 2-(1'<i>H</i>-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) is a putative AhR endogenous ligand. To improve the chemical stability, we synthesized a series of ITE chemical mimics. Using a series of in vitro assays, we identified 2-(1<i>H</i>-indole-3-carbonyl)-<i>N</i>-methyl thiazole-4-carboxamide (ITE-CONHCH<sub>3</sub>) as a highly potent (EC<sub>50</sub> = 1.6 nM) AhR agonist with high affinity (<i>K</i><sub>i</sub> = 88 nM). ITE-CONHCH<sub>3</sub> triggered AhR nuclear translocation and dimerization of AhR-ARNT, enhanced AhR binding in the CYP1A1 promoter, and induced AhR-regulated genes in an AhR-dependent manner. The metabolic stability of ITE-CONHCH<sub>3</sub> in a cell culture was 10 times higher than that of ITE. Finally, we observed protective effects of ITE-CONHCH<sub>3</sub> in mice with DSS-induced colitis. Overall, we demonstrate and validate a concept of microbial metabolite mimicry in the therapeutic targeting of AhR.

Knowledge Graph

Similar Paper

Targeting the Aryl Hydrocarbon Receptor with Microbial Metabolite Mimics Alleviates Experimental Colitis in Mice
Journal of Medicinal Chemistry 2022.0
Discovery of Norisoboldine Analogue III<sub>11</sub> as a Novel and Potent Aryl Hydrocarbon Receptor Agonist for the Treatment of Ulcerative Colitis
Journal of Medicinal Chemistry 2023.0
Pityriazepin and other potent AhR ligands isolated from Malassezia furfur yeast
Archives of Biochemistry and Biophysics 2015.0
Targeting Aryl hydrocarbon receptor for next-generation immunotherapies: Selective modulators (SAhRMs) versus rapidly metabolized ligands (RMAhRLs)
European Journal of Medicinal Chemistry 2020.0
An overview of aryl hydrocarbon receptor ligands in the Last two decades (2002–2022): A medicinal chemistry perspective
European Journal of Medicinal Chemistry 2022.0
The Highly Potent AhR Agonist Picoberin Modulates Hh-Dependent Osteoblast Differentiation
Journal of Medicinal Chemistry 2022.0
Synthesis and evaluation of 6-heteroarylamino-2,4,5-trimethylpyridin-3-ols as inhibitors of TNF-α-induced cell adhesion and inflammatory bowel disease
MedChemComm 2018.0
New FAAH inhibitors based on 3-carboxamido-5-aryl-isoxazole scaffold that protect against experimental colitis
Bioorganic &amp; Medicinal Chemistry 2011.0
3-Aroylmethylene-2,3,6,7-tetrahydro-1H-pyrazino[2,1-a]isoquinolin-4(11bH)-ones as Potent Nrf2/ARE Inducers in Human Cancer Cells and AOM-DSS Treated Mice
Journal of Medicinal Chemistry 2013.0
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists
Journal of Medicinal Chemistry 2016.0