DEPTOR Inhibitors
- 技術優勢
- Increased personalization of treatment for multiple myelomaTreatments are currently similar for all patientsThe targeted subset of patients that overexpress DEPTOR is easily identifiable during routine pathology assessmentsDoes not affect normal lymphocytes or noncancerous blood cellsSelectively induces multiple myeloma cell apoptosis and cell cycle arrest
- 技術應用
- Targeted therapy for a subset of multiple myeloma patients that overexpress DEPTOR.Therapeutic for other cancers or diseases that have DEPTOR overexpression and increased mTOR activity.
- 詳細技術說明
- Researchers at UCLA have found a small molecule that prevents the binding of DEPTOR to mTOR. The inhibition of interaction between DEPTOR and mTOR has been shown to cause selective death of multiple myeloma cells both in vitro and in vivo. Importantly, this treatment does not affect noncancerous cells. Further, the researchers have synthesized derivatives of the small molecule DEPTOR inhibitor that have greater anti-myeloma activity than the parent molecule (10X decrease in IC50; 1µM to 0.1µM).
- *Abstract
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Researchers at UCLA have found a small molecule that prevents the binding of DEPTOR to mTOR. The inhibition of interaction between DEPTOR and mTOR results in selective death of multiple myeloma cells, and can therefore be used as a targeted therapy for the disease.
- *Principal Investigation
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Name: Joseph Gera
Department:
Name: Michael Jung
Department:
Name: Jihye Lee
Department:
Name: Alan Lichtenstein
Department:
Name: Yijiang Shi
Department:
Name: Joseph Gera
Department:
Name: Alan Lichtenstein
Department:
Name: Yijiang Shi
Department:
- 其他
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State Of Development
- Analogs have been synthesized with a 10-fold decrease in IC50 (1µM to 0.1µM) compared to parent molecule
- Validated with primary multiple myeloma cells in vitro, with a direct correlation between cytotoxicity and DEPTOR expression
- Validated in mouse model
Background
Multiple myeloma is the second most common hematological malignancy in the U.S., and constitutes 1% of all cancers. Despite the introduction of improved therapies in recent years, life expectancy after diagnosis is only 4 years. Therefore, treatments that improve patient prognosis are greatly needed.
A subset of multiple myeloma patients overexpress the protein DEPTOR. This protein can enhance cancer growth and proliferation by binding the protein mTOR. A drug that inhibits this interaction could stop the growth- and survival-promoting activity of DEPTOR in multiple myeloma cells, and be an effective treatment for the subset of patients overexpressing this protein.
Tech ID/UC Case
27474/2016-516-0
Related Cases
2016-516-0
- 國家/地區
- 美國
