Unknown

Dataset Information

0

Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase.


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.

SUBMITTER: Winters M 

PROVIDER: S-EPMC6318801 | biostudies-literature | 2019 Jan

REPOSITORIES: biostudies-literature

altmetric image

Publications

Diaryl hydroxylamines as pan or dual inhibitors of indoleamine 2,3-dioxygenase-1, indoleamine 2,3-dioxygenase-2 and tryptophan dioxygenase.

Winters Maria M   DuHadaway James B JB   Pham Khoa N KN   Lewis-Ballester Ariel A   Badir Shorouk S   Wai Jenny J   Sheikh Eesha E   Yeh Syun-Ru SR   Prendergast George C GC   Muller Alexander J AJ   Malachowski William P WP  

European journal of medicinal chemistry 20181114


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 c  ...[more]

Similar Datasets

| S-EPMC2939288 | biostudies-literature
| S-EPMC1221754 | biostudies-other
| S-EPMC7366343 | biostudies-literature
| S-EPMC5900342 | biostudies-literature
| S-EPMC4368142 | biostudies-literature
| S-EPMC5150662 | biostudies-literature