Jump to main content
Jump to site search

Issue 7, 2017
Previous Article Next Article

Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry

Author affiliations

Abstract

Indoleamine 2,3-dioxygenase 1 (IDO1) mediates multiple immunoregulatory processes including the induction of regulatory T cell differentiation and activation, suppression of T cell immune responses and inhibition of dendritic cell function, which impair immune recognition of cancer cells and promote tumor growth. On this basis, this enzyme is widely recognized as a valuable drug target for the development of immunotherapeutic small molecules in oncology. Although medicinal chemistry has made a substantial contribution to the discovery of numerous chemical classes of potent IDO1 inhibitors in the past 20 years, only very few compounds have progressed in clinical trials. In this review, we provide an overview of the current understanding of structure–function relationships of the enzyme, and discuss structure–activity relationships of selected classes of inhibitors that have shaped the hitherto few successes of IDO1 medicinal chemistry. An outlook opinion is also given on trends in the design of next generation inhibitors of the enzyme.

Graphical abstract: Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry

Back to tab navigation

Publication details

The article was received on 01 Mar 2017, accepted on 11 May 2017 and first published on 16 May 2017


Article type: Review Article
DOI: 10.1039/C7MD00109F
Citation: Med. Chem. Commun., 2017,8, 1378-1392
  • Open access: Creative Commons BY license
  •   Request permissions

    Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry

    A. Coletti, F. A. Greco, D. Dolciami, E. Camaioni, R. Sardella, M. T. Pallotta, C. Volpi, C. Orabona, U. Grohmann and A. Macchiarulo, Med. Chem. Commun., 2017, 8, 1378
    DOI: 10.1039/C7MD00109F

    This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements