AI Article Synopsis
- Research on indoleamine 2,3-dioxygenase 1 (IDO1) as a cancer therapy target began in 2003, leading to intense development of inhibitor compounds in both academic and pharmaceutical settings.
- While several promising IDO1 inhibitors have been identified and moved into clinical trials, many contain functional groups that may cause unwanted side reactions instead of specifically targeting IDO1.
- The paper reviews existing IDO1 inhibitors, identifies problems in experimental methods used to evaluate them, and proposes new strategies for validating effective inhibitor designs.
Article 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.
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| http://dx.doi.org/10.1021/acs.jmedchem.5b00326 | DOI Listing |
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