Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810.

ABSTRACT: Novel drugs are designed against specific molecular targets, but almost unavoidably they bind non-targets, which can cause additional biological effects that may result in increased activity or, more frequently, undesired toxicity. Chemical proteomics is an ideal approach for the systematic identification of drug targets and off-targets, allowing unbiased screening of candidate interactors in their natural context (tissue or cell extracts). E-3810 is a novel multi-kinase inhibitor currently in clinical trials for its anti-angiogenic and anti-tumor activity. In biochemical assays, E-3810 targets primarily vascular endothelial growth factor and fibroblast growth factor receptors. Interestingly, E-3810 appears to inhibit the growth of tumor cells with low to undetectable levels of these prote

SUBMITTER: Colzani M 

PROVIDER: S-EPMC4047469 | biostudies-literature | 2014 Jun

REPOSITORIES: biostudies-literature