Ontology highlight
ABSTRACT:
SUBMITTER: Tojo S
PROVIDER: S-EPMC4190630 | biostudies-literature | 2014 Oct
REPOSITORIES: biostudies-literature
Tojo Shingo S Kohno Tetsuya T Tanaka Tomoyuki T Kamioka Seiji S Ota Yosuke Y Ishii Takayuki T Kamimoto Keiko K Asano Shigehiro S Isobe Yoshiaki Y
ACS medicinal chemistry letters 20140821 10
Indoleamine 2,3-dioxygenase 1 (IDO1) is considered as a promising target for the treatment of several diseases, including neurological disorders and cancer. We report here the crystal structures of two IDO1/IDO1 inhibitor complexes, one of which shows that Amg-1 is directly bound to the heme iron of IDO1 with a clear induced fit. We also describe the identification and preliminary optimization of imidazothiazole derivatives as novel IDO1 inhibitors. Using our crystal structure information and st ...[more]