Abstract
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.
Original language | English (US) |
---|---|
Pages (from-to) | 455-464 |
Number of pages | 10 |
Journal | European Journal of Medicinal Chemistry |
Volume | 162 |
DOIs | |
State | Published - Jan 15 2019 |
Keywords
- Antitumor therapy
- Diaryl oalkylhydroxylamines
- Dual inhibitor
- IDO1 inhibition
- IDO2 inhibition
- Pan inhibition
- TDO inhibition
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
- Organic Chemistry