The search for endogenous activators of the aryl hydrocarbon receptor

Chem Res Toxicol. 2008 Jan;21(1):102-16. doi: 10.1021/tx7001965. Epub 2007 Dec 13.


The primary design of this perspective is to describe the major ligand classes of the aryl hydrocarbon receptor (AHR). A grander objective is to provide models that may help define the physiological activator or "endogenous ligand" of the AHR. We present evidence supporting a developmental role for the AHR and propose mechanisms by which an endogenous ligand and consequent AHR activation might be important during normal physiology and development. From this vista, we survey the known xenobiotic, endogenous, dietary, and "unconventional" activators of the AHR, including, when possible, information about their induction potency, receptor binding affinity, and potential for exposure. In light of the essential function of the AHR in embryonic development, we discuss the candidacy of each of these compounds as physiologically important activators.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Animals
  • Diet
  • Humans
  • Ligands
  • Receptors, Aryl Hydrocarbon / agonists*
  • Receptors, Aryl Hydrocarbon / physiology
  • Receptors, Cell Surface / physiology
  • Signal Transduction / drug effects
  • Signal Transduction / physiology
  • Xenobiotics / pharmacology


  • Ligands
  • Receptors, Aryl Hydrocarbon
  • Receptors, Cell Surface
  • Xenobiotics