Oncogenic Fusion Tyrosine Kinases as Molecular Targets for Anti-Cancer Therapy

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


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Oncogenic Fusion Tyrosine Kinases as Molecular Targets for Anti-Cancer Therapy



Anti-Cancer Agents in Medicinal Chemistry, 7(6): 594-611.

Author(s): Rosalind H. Gunby, Elisa Sala, Carmen J. Tartari, Miriam Puttini, Carlo Gambacorti-Passerini and Luca Mologni.

Affiliation: Department of Clinical Medicine,University of Milano-Bicocca, Via Cadore 48, Monza 20052, Italy.

Abstract

Deregulated activation of protein tyrosine kinases (PTKs) is a frequent event underlying malignant transformation in many types of cancer. The formation of oncogenic fusion tyrosine kinases (FTKs) resulting from genomic rearrangements, represents a common mechanism by which kinases escape the strict controls that normally regulate their expression and activation. FTKs are typically composed of an N-terminal dimerisation domain, provided by the fusion partner protein, fused to the kinase domain of receptor or nonreceptor tyrosine kinases (non-RTKs). Since FTKs do not contain extracellular domains, they share many characteristics with non-RTKs in terms of their properties and approaches for therapeutic targeting. FTKs are cytoplasmic or sometimes nuclear proteins, depending on the normal distribution of their fusion partner. FTKs no longer respond to ligand and are instead constitutively activated by dimerisation induced by the fusion partner. Unlike RTKs, FTKs cannot be targeted by therapeutic antibodies, instead they require agents that can cross the cell membrane as with non-RTKs. Here we review the PTKs known to be expressed as FTKs in cancer and the strategies for molecularly targeting these FTKs in anti-cancer therapy.

Keywords:

Oncogenic fusion proteins, anti-cancer therapy, tyrosine kinase, small molecule inhibitors.



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Article Details

Volume: 7
Issue Number: 6
First Page: 594
Last Page: 611
Page Count: 18
DOI: 10.2174/187152007784111340
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