The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer

Oncogenesis
Stefanie TiedeGerhard Christofori

Abstract

Focal adhesion kinase (FAK) is a cytoplasmic tyrosine kinase that regulates a plethora of downstream signaling pathways essential for cell migration, proliferation and death, processes that are exploited by cancer cells during malignant progression. These well-established tumorigenic activities, together with its high expression and activity in different cancer types, highlight FAK as an attractive target for cancer therapy. We have assessed and characterized the therapeutic potential and the biological effects of BI 853520, a novel small chemical inhibitor of FAK, in several preclinical mouse models of breast cancer. Treatment with BI 853520 elicits a significant reduction in primary tumor growth caused by an anti-proliferative activity by BI 853520. In contrast, BI 853520 exerts effects with varying degrees of robustness on the different stages of the metastatic cascade. Together, the data demonstrate that the repression of FAK activity by the specific FAK inhibitor BI 853520 offers a promising anti-proliferative approach for cancer therapy.

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Citations

Mar 18, 2020·Expert Opinion on Investigational Drugs·Atish MohantyErminia Massarelli
Jun 13, 2019·Journal of Experimental & Clinical Cancer Research : CR·Jin ZhouLiling Tang
Mar 14, 2020·Pancreas·Francesco Di Maggio, Karim Hussien El-Shakankery
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Feb 11, 2021·Cancers·Damiano Cosimo RigiraccioloRosamaria Lappano
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Jul 10, 2020·Pathobiology : Journal of Immunopathology, Molecular and Cellular Biology·Yousif A KaririEmad A Rakha

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Datasets Mentioned

BETA
GSE116117

Methods Mentioned

BETA
transgenic
flow cytometry
surgical resection
Protein Assay
Protein
electrophoresis

Software Mentioned

ZEN 2 Zeiss Microscopy
R
ZEN
GO
edgeR
KEGG
db
GOstats
ImageJ
QuasR package

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