Polypharmacology of Approved Anticancer Drugs

Author(s): Ivano Amelio, Andrey Lisitsa, Richard A. Knight, Gerry Melino, Alexey V. Antonov.

Journal Name: Current Drug Targets

Volume 18 , Issue 5 , 2017

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Graphical Abstract:


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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Article Details

Year: 2017
Page: [534 - 543]
Pages: 10
DOI: 10.2174/1389450117666160301095233
Price: $65

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PDF: 35
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