Authors: Lamoral-Theys, D.; Pottier, L.; Dufrasne, F.; Neve, J.; Dubois, J.; Kornienko, A.; Kiss, R.; Ingrassia, L.

Source: Current Medicinal Chemistry, Volume 17, Number 9, March 2010 , pp. 812-825(14)

Publisher: Bentham Science Publishers

Abstract:

Over eleven hundred publications reporting anticancer activities of polyphenols have appeared in the peerreviewed literature. In addition, a search of the PubMed database using “polyphenols ” cancer “ review” as keywords produced over 320 hits for review articles (July 2009). Polyphenol anticancer activities include, among others, anti-oxidative, pro-apoptotic, DNA damaging, anti-angiogenic, and immunostimulatory effects. Targeting specific protein kinases to combat cancer represents a major focus of oncology research within the so-called targeted therapy approach. An exhaustive search of the PubMed database (July 2009) using “polyphenols - cancer - kinases” as keywords resulted in more than 130 hits, half of them having been published within the past five years. Furthermore, the PubMed database contains 25 reviews on the subject of anti-kinase activity of some specific polyphenols, including mainly curcumin and the green tea polyphenol (-)-epigallocatechin 3-gallate (EGCG). However, no attempt has been made yet to review this area of research in a comprehensive, general manner. The current review therefore aims to highlight those anticancer polyphenols that target specific kinases in various types of cancer. The present review also provides an in-depth analysis of polyphenol structure- activity relationships in relation to their anticancer activities and specific kinase targeting. Lastly, a number of polyphenols are identified as potential antitumor agents that could be used to combat biologically aggressive cancers, including metastasizing cancers, through the targeting of specific kinases.

Document Type: Research article

DOI: http://dx.doi.org/10.2174/092986710790712183

Affiliations: 1: Laboratoire de Toxicologie - Institut de Pharmacie, Universite Libre de Bruxelles (ULB), Campus de la Plaine - CP205/1 - Boulevard du Triomphe, 1050 Brussels, Belgium.

Publication date: 2010-03-01

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• Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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