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Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
[Farnesyl transferase inhibitors--a novel agent for breast cancer]
1Department of Medical Oncology, The Fourth Affiliated Hospital, Hebei Medical University, Shijiazhuang, Hebei 050011, P. R. China.
Abstract:
The ras family of proto-oncogenes are upstream mediators of several essential cellular signal transduction pathways involved in cell proliferation and survival. Point mutations of ras oncogenes result in constitutive activation of oncogenic Ras. The key step in post-translational processing of Ras protein is farnesylation by farnesyl transferase. Inhibitors of this enzyme were developed initially as a therapeutic strategy for Ras-mutated tumors. Moreover, it is now clear that farnesyl transferase inhibitors (FTIs) have activity independent of Ras, and show some effects on tumors without oncogenic ras mutations. Preclinical data show that FTIs can inhibit proliferation of breast cancer cells in vitro and in vivo, and phase II studies of FTI-R115777 in advanced breast cancer show encouraging results. Therefore, FTIs, used alone or with other agents, may be a novel therapeutic approach for breast cancer.
Insights
Farnesyl transferase inhibitors (FTIs) show promise in treating breast cancer by inhibiting cell proliferation. These inhibitors may offer a novel therapeutic strategy for breast cancer, even in tumors without ras mutations.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Ras proto-oncogenes regulate cell proliferation and survival pathways.
- Constitutive activation of oncogenic Ras occurs due to point mutations.
- Ras protein post-translational processing involves farnesylation by farnesyl transferase.
Purpose of the Study:
- To investigate the therapeutic potential of farnesyl transferase inhibitors (FTIs) in breast cancer.
- To evaluate FTI activity independent of Ras mutations.
- To explore FTIs as a novel treatment strategy for breast cancer.
Main Methods:
- Preclinical studies assessing FTI effects on breast cancer cell proliferation in vitro and in vivo.
- Phase II clinical trials evaluating FTI-R115777 in advanced breast cancer patients.
Main Results:
- FTIs demonstrated inhibition of breast cancer cell proliferation.
- Phase II studies of FTI-R115777 yielded encouraging results in advanced breast cancer.
- FTIs exhibit activity in tumors irrespective of oncogenic ras mutations.
Conclusions:
- FTIs represent a potential novel therapeutic approach for breast cancer.
- FTIs can be used alone or in combination with other agents.
- The therapeutic potential of FTIs extends to breast cancers with and without ras mutations.
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