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Advances in Indolemine 2,3-Dioxygenase 1 Medicinal Chemistry: Structure-Function and Structure-Activity Relationships of the Enzyme and its Inhibitors.

Abstract

Indolemine 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, the 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.

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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, Accepted Manuscript
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    Advances in Indolemine 2,3-Dioxygenase 1 Medicinal Chemistry: Structure-Function and Structure-Activity Relationships of the Enzyme and its Inhibitors.

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

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