Ligands and agonists of the aryl hydrocarbon receptor AhR: Facts and myths

Abstract

The aryl hydrocarbon receptor (AhR) belongs to the essential helix-loop-helix transcription factors family. This receptor has a central role in determining host physiology and a variety of pathophysiologies ranging from inflammation and metabolism to cancer. AhR is a ligand-driven receptor with intricate pharmacology of activation depending on the type and quantity of ligand present. Therefore, a better understanding of AhR ligands per se is critical to move the field forward. In this minireview, we clarify some facts and myths about AhR ligands and how further studies could shed light on the true nature of AhR activation by these ligands. The review covers select chemical classes and explores parameters that qualify them as true receptor ligands.

Keywords: Agonists; Aryl hydrocarbon receptor; Ligands; Receptor theory.