Ontology highlight
ABSTRACT:
SUBMITTER: Tan L
PROVIDER: S-EPMC5484535 | biostudies-literature | 2017 Feb
REPOSITORIES: biostudies-literature
Tan Li L Gurbani Deepak D Weisberg Ellen L EL Jones Douglas S DS Rao Suman S Singer William D WD Bernard Faviola M FM Mowafy Samar S Jenney Annie A Du Guangyan G Nonami Atsushi A Griffin James D JD Lauffenburger Douglas A DA Westover Kenneth D KD Sorger Peter K PK Gray Nathanael S NS
Bioorganic & medicinal chemistry 20161207 4
Targeted polypharmacology provides an efficient method of treating diseases such as cancer with complex, multigenic causes provided that compounds with advantageous activity profiles can be discovered. Novel covalent TAK1 inhibitors were validated in cellular contexts for their ability to inhibit the TAK1 kinase and for their polypharmacology. Several inhibitors phenocopied reported TAK1 inhibitor 5Z-7-oxozaenol with comparable efficacy and complementary kinase selectivity profiles. Compound 5 e ...[more]