The FAK inhibitor BI 853520 exerts anti-tumor effects in breast cancer
Open accessAbstract
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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IN10018 is a highly selective clinical-stage FAK inhibitor.
“it is a highly selective clinical‐stage FAK inhibitor.[ 23, 24 ]”
From Focal Adhesion Kinase (FAK) Inhibition Synergizes with KRAS G12C Inhibitors in Treating Cancer through the Regulation of the FAK–YAP Signaling (2021) · cites this paper as [23]
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References 68 · Cited by 66
Research works printed but not linked: 1
- [33]Shapiro IM Merlin deficiency predicts FAK inhibitor sensitivity: a synthetic lethal relationship Sci. Transl. Med. 2014 6 237ra68 PMC4165339 24848258
- Authors
- Tiede, S., Meyer-Schaller, N., Kalathur, R. K. R., Ivanek, R., Fagiani, E., Schmassmann, P., Stillhard, P., Häfliger, S., Kraut, N., Schweifer, N., Waizenegger, I. C., Bill, R., & Christofori, G.
- Affiliations
- University of Basel (CH)
- SIB Swiss Institute of Bioinformatics (CH)
- Boehringer Ingelheim (Austria) (AT)
- Corresponding author
- Bill, Ruben
- Christofori, Gerhard
- ORCID
- Venue
- Oncogenesis
- Published
- 2018-09-20
- Volume
- 7
- Issue
- 9
- Pages
- 73-73
- ISSN
- 2157-9024 (ISSN-L)
- PMC
- PMC6148276
- OpenAlex
- W2891572542
- Cited by
- 66
- References
- 68
- Citations by year
- 2026: 2 · 2025: 5 · 2024: 10 · 2023: 10 · 2022: 6 · 2021: 11 · 2020: 13 · 2019: 9
- FWCI
- 7.32
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Locations
- Oncogenesis (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- BORIS (University Library Bern) (submittedVersion, cc-by)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion)
- Open Access CRIS of the University of Bern
- Funders
- National Science Foundation
- Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung
- Swiss Cancer Research Foundation
- Topics
- Health Sciences › Medicine › Immunology and Allergy › Cell Adhesion Molecules Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › Cellular Mechanics and Interactions
- Health Sciences › Medicine › Oncology › Cancer Cells and Metastasis
- Keywords
- focal adhesion kinase, breast cancer, FAK inhibitors, antiproliferative activity, tumor growth inhibition, metastasis, tyrosine kinase inhibitors, cancer therapy
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