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Updated: Jun 10, 2026

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Advances in targeting SRC in the treatment of breast cancer and other solid malignancies
1Dana-Farber Cancer Institute, Boston, Massachusetts 02115, USA. emayer@partners.org
Abstract:
Src, a membrane-associated nonreceptor tyrosine kinase, plays a crucial role in the coordination and facilitation of cell-signaling pathways controlling a wide range of cellular functions, including growth, survival, invasion, adhesion, and migration. Deregulation and increased activity of Src has been observed in multiple human malignancies, prompting the development of specific inhibitors of Src. In preclinical studies, Src inhibitors show antitumor effects in multiple solid tumor types. Recently completed early-phase trials using the inhibitors dasatinib and bosutinib have suggested modest activity as monotherapy in breast and prostate cancer, with potentially greater activity in combination regimens. Given the interaction between Src and the estrogen receptor, ongoing trials are exploring combinations with endocrine therapy. The relationship between Src and the vascular endothelial growth factor receptor also justifies investigation of combinations with angiogenesis inhibitors. Future trials will continue to explore the contribution of Src inhibition with both chemotherapy and targeted agents.
Insights
Src tyrosine kinase is implicated in cancer growth and migration. Inhibitors show promise in early trials, especially when combined with other cancer therapies like endocrine or angiogenesis treatments.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Src is a nonreceptor tyrosine kinase crucial for cell signaling pathways.
- Increased Src activity is linked to various human cancers, including breast and prostate cancer.
- Src regulates critical cellular functions such as growth, survival, invasion, adhesion, and migration.
Purpose of the Study:
- To review the role of Src in malignancies.
- To discuss the therapeutic potential of Src inhibitors in cancer treatment.
- To explore ongoing and future clinical trials investigating Src inhibitor combinations.
Main Methods:
- Preclinical studies evaluating Src inhibitors.
- Analysis of early-phase clinical trials (e.g., dasatinib, bosutinib).
- Review of interactions between Src and other signaling pathways (estrogen receptor, VEGFR).
Main Results:
- Src inhibitors demonstrate antitumor effects in preclinical models.
- Early trials suggest modest efficacy of Src inhibitors as monotherapy in breast and prostate cancer.
- Potential for enhanced activity when Src inhibitors are used in combination regimens.
Conclusions:
- Src inhibitors represent a promising therapeutic strategy for various solid tumors.
- Combination therapies involving Src inhibitors with endocrine agents, angiogenesis inhibitors, chemotherapy, and targeted agents warrant further investigation.
- Targeting Src signaling offers a viable approach to combatting human malignancies.
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