Sphingolipid Drugs Triggering Nutrient Transporter Down-Regulation
- 技术应用
- These compounds may be developed for cancer therapies employing a novel mechanism of starving malignant cells. Specifically, these compounds could be useful for the treatment of certain blood-borne cancers and leukemias.
- 详细技术说明
- UCI researchers have designed and synthesized novel compounds that do not necessarily involve Fingolimod's S1P receptor-related, dose limiting toxicities. Specifically, the UCI researchers have designed a family of Azacyclic constrained analogs that overcome the dose-limiting toxicities of Fingolimod and down-regulate cellular nutrient transport. Studies in a mouse model suggest that these compounds do not exhibit undesirable cardio-vascular effects or sequester lymphocytes like Fingolimod.
- *Abstract
-
The immunosuppressant prodrug Fingolimod is approved for the treatment multiple sclerosis (MS). Fingolimod appears to be well tolerated at the dose necessary to treat MS, and it had been suggested that the compound may be useful for the treatment of certain types of cancer. But, recently, there have been studies that indicate bradycardia in patients at the elevated doses. Since high doses may be required for an anti-cancer treatment, use of Fingolimod as a cancer therapeutic may be significantly limited.
Mechanistically, Fingolimod is an immunosuppressant prodrug that functions by antagonizing S1P receptors. In its active, phosphorylated state, Fingolimod binds four of the five S1P receptors. It is further believed that binding of Fingolimod to S1P1 causes receptor activation and subsequent down regulation, causing circulating lymphocytes to migrate to secondary lymphoid tissues.
- *IP Issue Date
- Jun 9, 2016
- *Principal Investigation
-
Name: Aimee Edinger
Department:
Name: Stephen Hanessian
Department:
- 申请号码
- 2016015973
- 其他
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Tech ID/UC Case
23535/2013-802-0
Related Cases
2013-802-0, 2016-031-0
- 国家/地区
- 美国
