Next Article in Journal
Dual Effects of Non-Coding RNAs (ncRNAs) in Cancer Stem Cell Biology
Next Article in Special Issue
From Suppressor T Cells to Regulatory T Cells: How the Journey that Began with the Discovery of the Toxic Effects of TCDD Led to Better Understanding of the Role of AhR in Immunoregulation
Previous Article in Journal
Editorial: Special Issue on “Therapeutic Approaches for Cystic Fibrosis”
Previous Article in Special Issue
How the AHR Became Important in Intestinal Homeostasis—A Diurnal FICZ/AHR/CYP1A1 Feedback Controls Both Immunity and Immunopathology
 
 
Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
Journals
IJMS
Volume 21
Issue 18
10.3390/ijms21186654
ijms-logo
Submit to this Journal Review for this Journal Propose a Special Issue
► Article Menu

Article Menu

share Share announcement Help format_quote Cite question_answer Discuss in SciProfiles
first_page
settings
Order Article Reprints
Font Type:
Arial Georgia Verdana
Font Size:
Aa Aa Aa
Line Spacing:
Column Width:
Background:
Review

Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs)

by
Stephen Safe
1,*,
Un-ho Jin
1,
Hyejin Park
1,
Robert S. Chapkin
2 and
Arul Jayaraman
3
1
Department of Veterinary Physiology and Pharmacology, Texas A&M University, College Station, TX 77843, USA
2
Departments of Nutrition and Food Science and Biochemistry and Biophysics, Texas A&M University, College Station, TX 77843, USA
3
Department of Chemical Engineering, Texas A&M University, College Station, TX 77843, USA
*
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2020, 21(18), 6654; https://doi.org/10.3390/ijms21186654
Submission received: 11 August 2020 / Revised: 1 September 2020 / Accepted: 9 September 2020 / Published: 11 September 2020
(This article belongs to the Special Issue How the AHR Became Important-A Lesson in How Basic Science Leads to Actionable Translational Medicine)
Browse Figures
Review Reports Versions Notes

Abstract

The aryl hydrocarbon receptor (AhR) was first identified as the intracellular protein that bound and mediated the toxic effects of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD, dioxin) and dioxin-like compounds (DLCs). Subsequent studies show that the AhR plays an important role in maintaining cellular homeostasis and in pathophysiology, and there is increasing evidence that the AhR is an important drug target. The AhR binds structurally diverse compounds, including pharmaceuticals, phytochemicals and endogenous biochemicals, some of which may serve as endogenous ligands. Classification of DLCs and non-DLCs based on their persistence (metabolism), toxicities, binding to wild-type/mutant AhR and structural similarities have been reported. This review provides data suggesting that ligands for the AhR are selective AhR modulators (SAhRMs) that exhibit tissue/cell-specific AhR agonist and antagonist activities, and that their functional diversity is similar to selective receptor modulators that target steroid hormone and other nuclear receptors.
Keywords: AhR; ligand selectivity; agonist; antagonist AhR; ligand selectivity; agonist; antagonist

Share and Cite

MDPI and ACS Style

Safe, S.; Jin, U.-h.; Park, H.; Chapkin, R.S.; Jayaraman, A. Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs). Int. J. Mol. Sci. 2020, 21, 6654. https://doi.org/10.3390/ijms21186654

AMA Style

Safe S, Jin U-h, Park H, Chapkin RS, Jayaraman A. Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs). International Journal of Molecular Sciences. 2020; 21(18):6654. https://doi.org/10.3390/ijms21186654

Chicago/Turabian Style

Safe, Stephen, Un-ho Jin, Hyejin Park, Robert S. Chapkin, and Arul Jayaraman. 2020. "Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs)" International Journal of Molecular Sciences 21, no. 18: 6654. https://doi.org/10.3390/ijms21186654

APA Style

Safe, S., Jin, U.-h., Park, H., Chapkin, R. S., & Jayaraman, A. (2020). Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs). International Journal of Molecular Sciences, 21(18), 6654. https://doi.org/10.3390/ijms21186654

Note that from the first issue of 2016, this journal uses article numbers instead of page numbers. See further details here.

Article Metrics

Back to TopTop