Ontology highlight
ABSTRACT:
SUBMITTER: Pei Z
PROVIDER: S-EPMC5949840 | biostudies-literature | 2018 May
REPOSITORIES: biostudies-literature
Pei Zhonghua Z Mendonca Rohan R Gazzard Lewis L Pastor Richard R Goon Leanne L Gustafson Amy A VanderPorten Erica E Hatzivassiliou Georgia G Dement Kevin K Cass Robert R Yuen Po-Wai PW Zhang Yamin Y Wu Guosheng G Lin Xingyu X Liu Yichin Y Sellers Benjamin D BD
ACS medicinal chemistry letters 20180402 5
Tryptophan 2,3-dioxygenase 2 (TDO2) catalyzes the conversion of tryptophan to the immunosuppressive metabolite kynurenine. TDO2 overexpression has been observed in a number of cancers; therefore, TDO inhibition may be a useful therapeutic intervention for cancers. We identified an aminoisoxazole series as potent TDO2 inhibitors from a high-throughput screen (HTS). An extensive medicinal chemistry effort revealed that both the amino group and the isoxazole moiety are important for TDO2 inhibitory ...[more]