Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs)
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...
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doaj-b11444fadfaf47ecbdf80caf6a46a3012020-11-25T03:48:07ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672020-09-01216654665410.3390/ijms21186654Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs)Stephen Safe0Un-ho Jin1Hyejin Park2Robert S. Chapkin3Arul Jayaraman4Department of Veterinary Physiology and Pharmacology, Texas A&M University, College Station, TX 77843, USADepartment of Veterinary Physiology and Pharmacology, Texas A&M University, College Station, TX 77843, USADepartment of Veterinary Physiology and Pharmacology, Texas A&M University, College Station, TX 77843, USADepartments of Nutrition and Food Science and Biochemistry and Biophysics, Texas A&M University, College Station, TX 77843, USADepartment of Chemical Engineering, Texas A&M University, College Station, TX 77843, USAThe 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.https://www.mdpi.com/1422-0067/21/18/6654AhRligand selectivityagonistantagonist |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Stephen Safe Un-ho Jin Hyejin Park Robert S. Chapkin Arul Jayaraman |
spellingShingle |
Stephen Safe Un-ho Jin Hyejin Park Robert S. Chapkin Arul Jayaraman Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) International Journal of Molecular Sciences AhR ligand selectivity agonist antagonist |
author_facet |
Stephen Safe Un-ho Jin Hyejin Park Robert S. Chapkin Arul Jayaraman |
author_sort |
Stephen Safe |
title |
Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) |
title_short |
Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) |
title_full |
Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) |
title_fullStr |
Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) |
title_full_unstemmed |
Aryl Hydrocarbon Receptor (AHR) Ligands as Selective AHR Modulators (SAhRMs) |
title_sort |
aryl hydrocarbon receptor (ahr) ligands as selective ahr modulators (sahrms) |
publisher |
MDPI AG |
series |
International Journal of Molecular Sciences |
issn |
1661-6596 1422-0067 |
publishDate |
2020-09-01 |
description |
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. |
topic |
AhR ligand selectivity agonist antagonist |
url |
https://www.mdpi.com/1422-0067/21/18/6654 |
work_keys_str_mv |
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