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

Tiede, Stefanie; Meyer-Schaller, Nathalie; Kalathur, Ravi Kiran Reddy; Ivanek, Robert; Fagiani, Ernesta; Schmassmann, Philip; Stillhard, Patrick; Häfliger, Simon; Kraut, Norbert; Schweifer, Norbert; Waizenegger, Irene C; Bill, Ruben; Christofori, Gerhard (2018). The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer. Oncogenesis, 7(9), p. 73. Springer Nature 10.1038/s41389-018-0083-1

Preview

Text 41389_2018_Article_83.pdf - Published Version Available under License Creative Commons: Attribution (CC-BY). Download (4MB) | Preview

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.

Interest & Impact

Downloads

197 since deposited on 08 Mar 2019
16 in the past 12 months

Citations

5 Citations in Web of Science ®
6 Citations in Scopus

Search

in Google Scholar™

Services

Actions (login required)

Edit item

Actions (login required)

Edit item