title: Polypharmacology of Approved Anticancer 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.
authors.affiliation: Medical Research Council Toxicology Unit, Leicester LE1 9HN, United Kingdom.
authors.forename: Ivano
authors.initials: I
authors.lastname: Amelio
authors.affiliation: Institute of Biomedical Chemistry of the Russian Academy of Medical Sciences, Pogodinskaya Street, Moscow, Russian Federation.
authors.forename: Andrey
authors.initials: A
authors.lastname: Lisitsa
authors.affiliation: Medical Research Council Toxicology Unit, Leicester LE1 9HN, United Kingdom.
authors.forename: Richard A
authors.initials: RA
authors.lastname: Knight
authors.affiliation: Institute of Cytology, Saint-Petersburg 194064, Russian Federation.
authors.forename: Gerry
authors.initials: G
authors.lastname: Melino
authors.affiliation: Medical Research Council Toxicology Unit, Leicester LE1 9HN, United Kingdom.
authors.forename: Alexey V
authors.initials: AV
authors.lastname: Antonov
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D017277:Drug Approval; D004359:Drug Therapy, Combination; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*; D064798:Polypharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents
keywords: DNA topoisomerase inhibitors; Polypharmacology; drug targets; histone deacetylase inhibitors; rational design of multitarget drugs.; tamoxifen; tyrosine kinase inhibitors