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Blockade of the AHR restricts a Treg-macrophage suppressive axis induced by L-Kynurenine

Nat Commun. 2020 Aug 11;11(1):4011. doi: 10.1038/s41467-020-17750-z.

Abstract

Tryptophan catabolism by the enzymes indoleamine 2,3-dioxygenase 1 and tryptophan 2,3-dioxygenase 2 (IDO/TDO) promotes immunosuppression across different cancer types. The tryptophan metabolite L-Kynurenine (Kyn) interacts with the ligand-activated transcription factor aryl hydrocarbon receptor (AHR) to drive the generation of Tregs and tolerogenic myeloid cells and PD-1 up-regulation in CD8+ T cells. Here, we show that the AHR pathway is selectively active in IDO/TDO-overexpressing tumors and is associated with resistance to immune checkpoint inhibitors. We demonstrate that IDO-Kyn-AHR-mediated immunosuppression depends on an interplay between Tregs and tumor-associated macrophages, which can be reversed by AHR inhibition. Selective AHR blockade delays progression in IDO/TDO-overexpressing tumors, and its efficacy is improved in combination with PD-1 blockade. Our findings suggest that blocking the AHR pathway in IDO/TDO expressing tumors would overcome the limitation of single IDO or TDO targeting agents and constitutes a personalized approach to immunotherapy, particularly in combination with immune checkpoint inhibitors.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Resistance, Neoplasm
  • Humans
  • Immune Tolerance
  • Immunotherapy
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / genetics
  • Indoleamine-Pyrrole 2,3,-Dioxygenase / metabolism
  • Kynurenine / immunology*
  • Macrophages / immunology*
  • Mice
  • Neoplasms / immunology
  • Neoplasms / therapy
  • Programmed Cell Death 1 Receptor / antagonists & inhibitors
  • Programmed Cell Death 1 Receptor / immunology
  • Receptors, Aryl Hydrocarbon / antagonists & inhibitors*
  • Receptors, Aryl Hydrocarbon / genetics
  • Receptors, Aryl Hydrocarbon / metabolism
  • Signal Transduction
  • T-Lymphocytes, Regulatory / immunology*
  • Tryptophan Oxygenase / genetics
  • Tryptophan Oxygenase / metabolism
  • Tumor Cells, Cultured
  • Tumor Microenvironment

Substances

  • Indoleamine-Pyrrole 2,3,-Dioxygenase
  • PDCD1 protein, human
  • Programmed Cell Death 1 Receptor
  • Receptors, Aryl Hydrocarbon
  • Kynurenine
  • Tryptophan Oxygenase