The major drug discovery efforts in oncology have been concentrated on the development of
selective molecules that are supposed to act specifically on one anticancer mechanism by modulating a
single or several closely related drug targets. However, a bird's eye view on data from multiple available
bioassays implies that most approved anticancer agents do, in fact, target many more proteins with different
functions. Here we will review and systematize currently available information on the targets of
several anticancer drugs along with revision of their potential mechanisms of action. Polypharmacology
of the current antineoplastic agents suggests that drug clinical efficacy in oncology can be achieved only
via modulation of multiple cellular mechanisms.
Keywords: Polypharmacology, tyrosine kinase inhibitors, histone deacetylase inhibitors, DNA topoisomerase inhibitors, tamoxifen,
drug targets, rational design of multitarget drugs.
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