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.
Export Options
About this article
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 |
Call for Papers in Thematic Issues
Drug-Targeted Approach with Polymer Nanocomposites for Improved Therapeutics
Polymer nanocomposites have been recognized as an advanced and cutting-edge technique in drug targeting administration. These materials combine the unique features of nanoparticles with the adaptability of polymers to produce highly personalized drug administration devices. Integrating nanoparticles containing pharmaceuticals into a polymer matrix enables researchers to regulate the rates at ...read more
RNA Molecules in the Treatment of Human Diseases
Messenger and non-coding RNAs, including long and small transcripts, are mediators of gene expression. Gene expression at the RNA level shows significant aberrations in human diseases, including cancer, leukemia, lymphoma, cardiovascular diseases, and neurological disorders. Human transcripts serve either as biomarkers of diagnosis, prognosis, prediction of treatment response, and/or therapy ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Oxazolidinones as Chiral Auxiliaries in the Asymmetric 1,4-Conjugate Addition Reaction Applied to the Total Synthesis of Natural Products: A Supplemental Mini-Review
Current Organic Synthesis Polo-Like Kinase 1 Pharmacological Inhibition as Monotherapy or in Combination: Comparative Effects of Polo-Like Kinase 1 Inhibition in Medulloblastoma Cells
Anti-Cancer Agents in Medicinal Chemistry Targeting Ceramide Metabolism in Hepatocellular Carcinoma: New Points for Therapeutic Intervention
Current Medicinal Chemistry Recent Developments in the Understanding and Treatment of Neurodegenerative Disorders Involving Protein Conformational Misfolding and Amyloid Formation
Medicinal Chemistry Reviews - Online (Discontinued) Tumor-Derived Extracellular Fragments of Receptor Protein Tyrosine Phosphatases (RPTPs) as Cancer Molecular Diagnostic Tools
Anti-Cancer Agents in Medicinal Chemistry Biological Role of Formaldehyde, and Cycles Related to Methylation, Demethylation, and Formaldehyde Production
Mini-Reviews in Medicinal Chemistry Curcumin and its Derivatives: Their Application in Neuropharmacology and Neuroscience in the 21st Century
Current Neuropharmacology Understanding Epigenetic Alterations in Alzheimer's and Parkinson's Disease: Towards Targeted Biomarkers and Therapies
Current Pharmaceutical Design Betulin-Betulinic Acid Natural Product Based Analogs as Anti-Cancer Agents
Anti-Cancer Agents in Medicinal Chemistry Amyloid-Binding Compounds and their Anti-Prion Potency
Current Topics in Medicinal Chemistry Development of ATP13A2-deficient In vitro Model for PARK9 Parkinson’s Disease
Current Signal Transduction Therapy Current Understanding of HSP90 as a Novel Therapeutic Target: An Emerging Approach for the Treatment of Cancer
Current Pharmaceutical Design The Cholesterol Transport Inhibitor U18666a Regulates Amyloid Precursor Protein Metabolism and Trafficking in N2aAPP “Swedish” Cells
Current Alzheimer Research Effects of Proteoglycans on Oxidative/Nitrative Stress
Current Organic Chemistry NPFF2 Receptor is Involved in the Modulatory Effects of Neuropeptide FF for Macrophage Cell Line
Protein & Peptide Letters A Fluorescent Alkyllysophospholipid Analog Exhibits Selective Cytotoxicity Against the Hormone-Insensitive Prostate Cancer Cell Line PC3
Anti-Cancer Agents in Medicinal Chemistry Serotonin Receptors of Type 6 (5-HT6): What can we Expect from them?
Current Medicinal Chemistry Neuroprotective Effects of Ellagitannins: A Brief Review
Current Drug Targets Exploring Pharmacological Significance of Chalcone Scaffold: A Review
Current Medicinal Chemistry Biological Responses to Hydrogen Molecule and its Preventive Effects on Inflammatory Diseases
Current Pharmaceutical Design