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Molecules 2014, 19(9), 15196-15212; doi:10.3390/molecules190915196

Small Molecule Tyrosine Kinase Inhibitors of ErbB2/HER2/Neu in the Treatment of Aggressive Breast Cancer

1
Department of Chemistry, Xavier University of Louisiana, 1 Drexel Drive, New Orleans, LA 70125, USA
2
Ogden College of Science and Engineering, Western Kentucky University, 1906 College Heights Boulevard #11075, Bowling Green, KY 42101, USA
*
Author to whom correspondence should be addressed.
Received: 6 August 2014 / Revised: 8 September 2014 / Accepted: 10 September 2014 / Published: 23 September 2014
(This article belongs to the Special Issue Design and Study of Kinase Inhibitors)
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Abstract

The human epidermal growth factor receptor 2 (HER2) is a member of the erbB class of tyrosine kinase receptors. These proteins are normally expressed at the surface of healthy cells and play critical roles in the signal transduction cascade in a myriad of biochemical pathways responsible for cell growth and differentiation. However, it is widely known that amplification and subsequent overexpression of the HER2 encoding oncogene results in unregulated cell proliferation in an aggressive form of breast cancer known as HER2-positive breast cancer. Existing therapies such as trastuzumab (Herceptin®) and lapatinib (Tyverb/Tykerb®), a monoclonal antibody inhibitor and a dual EGFR/HER2 kinase inhibitor, respectively, are currently used in the treatment of HER2-positive cancers, although issues with high recurrence and acquired resistance still remain. Small molecule tyrosine kinase inhibitors provide attractive therapeutic targets, as they are able to block cell signaling associated with many of the proposed mechanisms for HER2 resistance. In this regard we aim to present a review on the available HER2 tyrosine kinase inhibitors, as well as those currently in development. The use of tyrosine kinase inhibitors as sequential or combinatorial therapeutic strategies with other HER family inhibitors is also discussed. View Full-Text
Keywords: human epidermal growth factor 2 (HER2); kinase domain; HER2 inhibition; monoclonal antibodies; small molecule inhibitors human epidermal growth factor 2 (HER2); kinase domain; HER2 inhibition; monoclonal antibodies; small molecule inhibitors
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MDPI and ACS Style

Schroeder, R.L.; Stevens, C.L.; Sridhar, J. Small Molecule Tyrosine Kinase Inhibitors of ErbB2/HER2/Neu in the Treatment of Aggressive Breast Cancer. Molecules 2014, 19, 15196-15212.

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