The AhR twist: ligand-dependent AhR signaling and pharmaco-toxicological implications
Erwan Guyot1, Aline Chevallier, Robert Barouki
1INSERM UMR-S 747, Toxicologie Pharmacologie et Signalisation Cellulaire, 45 rue des Saints Pères, 75006 Paris, France.
Abstract:
The aryl hydrocarbon receptor (AhR) is a transcription factor which is activated by diverse compounds and regulates the expression of xenobiotic metabolism genes. Recent studies have unraveled unsuspected physiological roles and novel alternative ligand-specific pathways for this receptor. In this review, we discuss these novel aspects and focus on the different responses elicited by the diverse endogenous and/or exogenous AhR ligands. In addition to challenging the relevance of the 'agonist/antagonist' classification of ligands, we introduce the concept of AhR plasticity as a primordial factor in the generation of these pathways. Finally, we suggest several promising perspectives for the pharmacological modulation of these responses.
Related Concept Videos
Drug-Receptor Interactions
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.
Drug Toxicity: Overview
Drug Toxicity: Risk factors
Signal Transduction: Overview
Typically, signal transduction involves three...
Principles of Drug Action
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
The Two-State Receptor Model
The binding affinity of a drug determines its interaction with one...

