Endogenous kynurenines as targets for drug discovery and development

Nat Rev Drug Discov. 2002 Aug;1(8):609-20. doi: 10.1038/nrd870.


The kynurenine pathway is the main pathway for tryptophan metabolism. It generates compounds that can modulate activity at glutamate receptors and possibly nicotinic receptors, in addition to some as-yet-unidentified sites. The pathway is in a unique position to regulate other aspects of the metabolism of tryptophan to neuroactive compounds, and also seems to be a key factor in the communication between the nervous and immune systems. It also has potentially important roles in the regulation of cell proliferation and tissue function in the periphery. As a result, the pathway presents a multitude of potential sites for drug discovery in neuroscience, oncology and visceral pathology.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Drug Delivery Systems / methods*
  • Drug Design*
  • Humans
  • Kynurenic Acid / chemistry
  • Kynurenic Acid / metabolism
  • Kynurenine / analogs & derivatives
  • Kynurenine / chemistry
  • Kynurenine / metabolism*
  • Signal Transduction / physiology
  • Technology, Pharmaceutical / methods*
  • Tryptophan / metabolism


  • Kynurenine
  • Tryptophan
  • Kynurenic Acid