European Journal of Medicinal Chemistry p. 455 - 464 (2019)
Update date:2022-07-29
Topics:
Winters, Maria
DuHadaway, James B.
Pham, Khoa N.
Lewis-Ballester, Ariel
Badir, Shorouk
Wai, Jenny
Sheikh, Eesha
Yeh, Syun-Ru
Prendergast, George C.
Muller, Alexander J.
Malachowski, William P.
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.
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