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Challenges in the Discovery of Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitors.

Abstract：

:Since the discovery of indoleamine 2,3-dioxygenase 1 (IDO1) as an attractive target for anticancer therapy in 2003, the search for inhibitors has been intensely pursued both in academia and in pharmaceutical companies. Many novel IDO1 inhibitor scaffolds have been described, and a few potent compounds have entered clinical trials. However, a significant number of the reported compounds contain problematic functional groups, suggesting that enzyme inhibition could be the result of undesirable side reactions instead of selective binding to IDO1. Here, we describe issues in the employed experimental protocols, review and classify reported IDO1 inhibitors, and suggest different approaches for confirming viable inhibitor scaffolds.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Röhrig UF,Majjigapu SR,Vogel P,Zoete V,Michielin O

doi

10.1021/acs.jmedchem.5b00326

subject

Has Abstract

pub_date

2015-12-24 00:00:00

pages

9421-37

issue

24

eissn

0022-2623

issn

1520-4804

journal_volume

58

pub_type

杂志文章,评审

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