Ontology highlight
ABSTRACT:
SUBMITTER: Steeneck C
PROVIDER: S-EPMC7025390 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20200127 2
Following the impressive success of checkpoint inhibitors in the treatment of cancer, combinations of IDO1 inhibitors with PD-1/PD-L1 antibodies are in clinical development aiming to increase response rates. Using the hydroxyamidine pharmacophore of the IDO1 inhibitor INCB14943 as a starting point for the design of new inhibitors, the potential shortcomings of extensive hydroxyamidine glucuronidation in humans was addressed. Compounds were optimized using a stability assay with recombinant UGT1A ...[more]