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What is a biological benefit of some HER2 kinase inhibitors outside of kinase activity inhibition, and...

What is a biological benefit of some HER2 kinase inhibitors outside of kinase activity inhibition, and how can this be exploited pharmaceutically? Please use detail. 16pts.

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Answer #1

The HER2 overexpression is seen almost 25-30% of the breast cancers. Targeted therapy using trastuzumab is used to treat these cancers though they have poor prognosis. HER2 tyrosine kinase inhibitors like lapatinib , canertinib are under trials.

The effects of these agents include ;

1. Antibody dependant cell mediated cytotoxicity

2. Downregulation of HER2 signaling

3. Inhibition of cell proliferation and survival signals

4. Interference with the DNA repair

Combination of trastuzumab with other cytotoxic agents are used to treat metastatic cancers

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