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.
Current Drug Targets
Title:Polypharmacology of Approved Anticancer Drugs
Volume: 18 Issue: 5
Author(s): Ivano Amelio, Andrey Lisitsa, Richard A. Knight, Gerry Melino and Alexey V. Antonov
Affiliation:
Keywords: Polypharmacology, tyrosine kinase inhibitors, histone deacetylase inhibitors, DNA topoisomerase inhibitors, tamoxifen, drug targets, rational design of multitarget drugs.
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.
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Cite this article as:
Amelio Ivano, Lisitsa Andrey, Knight A. Richard, Melino Gerry and Antonov V. Alexey, Polypharmacology of Approved Anticancer Drugs, Current Drug Targets 2017; 18 (5) . https://dx.doi.org/10.2174/1389450117666160301095233
DOI https://dx.doi.org/10.2174/1389450117666160301095233 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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