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Updated: Jan 29, 2026

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Published on: March 20, 2020
Src kinase: a therapeutic opportunity in endocrine-responsive and resistant breast cancer
Stephen Hiscox1,2, Robert I Nicholson1
1a Breast Cancer (Molecular Pharmacology) Group, Welsh School of Pharmacy, Redwood Building, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3NB, UK.
Abstract:
The intracellular kinase, Src, interacts with a diverse array of signaling elements, including the estrogen receptor to regulate breast cancer progression. Recent evidence has also implicated Src in mediating the response of breast cancer to endocrine agents and in the acquisition of antihormone resistance, a significant limiting factor to the clinical effectiveness of systemic endocrine therapy. A number of pharmacological inhibitors of Src kinase have been developed that are effective at suppressing breast cancer growth and invasion in vitro and inhibiting disease spread in vivo. Significantly, there appears to be added benefit when these agents are given in combination with anti-estrogens in endocrine-sensitive and -resistant models. These new findings suggest that Src inhibitors might have therapeutic value in breast cancer patients to improve endocrine response and circumvent resistance.
Insights
Src kinase plays a key role in breast cancer progression and endocrine resistance. Inhibiting Src kinase may improve treatment response and overcome resistance to endocrine therapy in breast cancer patients.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The intracellular kinase, Src, interacts with signaling elements like the estrogen receptor, regulating breast cancer progression.
- Src is implicated in mediating breast cancer response to endocrine agents and the development of antihormone resistance, limiting endocrine therapy effectiveness.
Purpose of the Study:
- To investigate the role of Src kinase in breast cancer endocrine resistance.
- To evaluate the therapeutic potential of Src kinase inhibitors, alone and in combination with anti-estrogens, for breast cancer treatment.
Main Methods:
- Utilized in vitro and in vivo models of endocrine-sensitive and -resistant breast cancer.
- Assessed the efficacy of pharmacological Src kinase inhibitors in suppressing tumor growth, invasion, and disease spread.
- Examined the combined effects of Src inhibitors and anti-estrogens.
Main Results:
- Pharmacological Src kinase inhibitors demonstrated effectiveness in suppressing breast cancer growth and invasion in vitro.
- These inhibitors were also effective in inhibiting disease spread in vivo.
- Combination therapy with Src inhibitors and anti-estrogens showed added benefit in both endocrine-sensitive and -resistant breast cancer models.
Conclusions:
- Src kinase inhibitors show therapeutic promise for breast cancer.
- Combining Src inhibitors with anti-estrogens may improve endocrine response and circumvent resistance in breast cancer patients.
- Targeting Src kinase represents a potential strategy to enhance the clinical effectiveness of endocrine therapy.
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