Ontology highlight
ABSTRACT:
SUBMITTER: Almqvist H
PROVIDER: S-EPMC4820820 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Almqvist Helena H Axelsson Hanna H Jafari Rozbeh R Dan Chen C Mateus André A Haraldsson Martin M Larsson Andreas A Martinez Molina Daniel D Artursson Per P Lundbäck Thomas T Nordlund Pär P
Nature communications 20160324
Target engagement is a critical factor for therapeutic efficacy. Assessment of compound binding to native target proteins in live cells is therefore highly desirable in all stages of drug discovery. We report here the first compound library screen based on biophysical measurements of intracellular target binding, exemplified by human thymidylate synthase (TS). The screen selected accurately for all the tested known drugs acting on TS. We also identified TS inhibitors with novel chemistry and mar ...[more]