期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 162, 期 -, 页码 455-464出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2018.11.010
关键词
IDO1 inhibition; IDO2 inhibition; TDO inhibition; Diaryl oalkylhydroxylamines; Antitumor therapy; Pan inhibition; Dual inhibitor
资金
- NIH [R01 CA109542, R01 GM086482, GM087291]
- Lankenau Medical Center Foundation
- Main Line Health
- Bryn Mawr College
- National Science Foundation [CHE-0958996]
Tryptophan (Trp) catabolizing enzymes play an important and complex role in the development of cancer. Significant evidence implicates them in a range of inflammatory and immunosuppressive activities. Whereas inhibitors of indoleamine 2,3-dioxygenase-1 (IDO1) have been reported and analyzed in the clinic, fewer inhibitors have been described for tryptophan dioxygenase (TDO) and indoleamine 2,3-dioxygenase-2 (IDO2) which also have been implicated more recently in cancer, inflammation and immune control. Consequently the development of dual or pan inhibitors of these Trp catabolizing enzymes may represent a therapeutically important area of research. This is the first report to describe the development of dual and pan inhibitors of IDO1, TDO and IDO2. (C) 2018 Elsevier Masson SAS. All rights reserved.
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