Ontology highlight
ABSTRACT:
SUBMITTER: Lewis-Ballester A
PROVIDER: S-EPMC5700043 | biostudies-literature | 2017 Nov
REPOSITORIES: biostudies-literature
Lewis-Ballester Ariel A Pham Khoa N KN Batabyal Dipanwita D Karkashon Shay S Bonanno Jeffrey B JB Poulos Thomas L TL Yeh Syun-Ru SR
Nature communications 20171122 1
Human indoleamine 2,3-dioxygenase 1 (hIDO1) is an attractive cancer immunotherapeutic target owing to its role in promoting tumoral immune escape. However, drug development has been hindered by limited structural information. Here, we report the crystal structures of hIDO1 in complex with its substrate, Trp, an inhibitor, epacadostat, and/or an effector, indole ethanol (IDE). The data reveal structural features of the active site (Sa) critical for substrate activation; in addition, they disclose ...[more]