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Polyphenols as Receptor Tyrosine Kinase Inhibitors and Anti-cancer Agents

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Abstract

Historically, there has been a great deal of interest in the use of natural products to promote human health. A large number of publications have demonstrated that phytochemicals, especially polyphenols, have biological activities that suggest they could positively impact a variety of health problems including cancer. The number of polyphenols is extremely large and we are just now learning the vast number of cellular molecular targets they affect to act as chemopreventive and anti-cancer agents. An important problem yet to be resolved is to identify those key molecular targets impacted by polyphenols that are most critical in cancer progression. Receptor tyrosine kinases (RTKs) are important proteins that couple extracellular signals with intracellular signaling pathways that can contribute to all stages of cancer development. This review will focus on the various ways in which a number of polyphenols can inhibit RTKs. We will discuss the possibility that the inhibition of a multitude of RTKs, often impacted by single polyphenols, can be explained by a few molecular mechanisms. We will discuss the current clinical trials that have been done using polyphenols and approaches that are being used to overcome the issue of bioavailability. Finally, we will also discuss the challenges and possible solutions to advancing polyphenols for actual clinical use as anti-cancer agents.

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Coleman, D.T., Cardelli, J.A. (2012). Polyphenols as Receptor Tyrosine Kinase Inhibitors and Anti-cancer Agents. In: Sarkar, F. (eds) Nutraceuticals and Cancer. Springer, Dordrecht. https://doi.org/10.1007/978-94-007-2630-7_3

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