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
 
 
Review

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

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
Received: 11 August 2020 / Revised: 1 September 2020 / Accepted: 9 September 2020 / Published: 11 September 2020
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. View Full-Text
Keywords: AhR; ligand selectivity; agonist; antagonist AhR; ligand selectivity; agonist; antagonist
Show Figures

Figure 1

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

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop