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Basal Glucose Transport Inhibitors as Anti-Cancer Therapeutics

技术优势

Benefits of Technology New compound and new target in the treatment of cancer. Broad application as a therapeutic across multiple cancer types. Targeted small molecule therapeutic that does not affect normal cells. Inhibits glucose transport, the first rate-limiting step of glucosemetabolism ΓÇô the primary energy source for cancer cell growth,angiogenesis, and metastasis ΓÇô for earlier therapeutic affects in thecancer cell cycle.

技术应用

Novel oral cancer therapeutic targeted against multiple cancer types.

详细技术说明

Researchers at Ohio University have created a new class of therapeutic compounds targeting basalglucose transport with implications for broad efficacy across multiple cancer types. This group ofcompounds focuses on the inhibition of basal glucose transport as astrategy for cancer treatment.Cancer cells are known to have up-regulated basal glucose transportand are “addicted” to glucose as their energy source. Inhibition ofbasal glucose transport cuts off this energy supply to starve andultimately kill the cancer cells. Normal cells are less sensitive toglucose deprivation as a result of their ability to use alternative energysources, e.g., amino acids and lipids. Clinical trials have been basedon the concept of glucose deprivation through metabolic targeting(inhibition) of glycolysis. However, glucose deprivation throughinhibition of glucose transport, the first rate-limiting step of glucosemetabolism, has never been attempted due to the lack of specificglucose transporter inhibitors. The current invention provides a novel,proprietary group of potent small molecules that effectively andselectively target basal glucose transport.A second generation compound, known as DRB-18, was tested foranti-cancer activity in the NCI-60 cancer cells panel in a single-dosetest. DRB-18 showed strong inhibition in all cell lines of six cancer types—leukemia, CNS cancer,melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. Of note, a metastatic triplenegativeand Krasonc breast cancer cell line was significantly decreased by DRB-18. Triple-negative breastcancer cells, which lack estrogen receptor (ER), progesterone receptor (PR) and Her2/neu receptor, areknown to be more aggressive and resistant to chemotherapies targeting the three receptors. Therefore,DRB-18 has the potential to be a valuable new weapon against triple-negative breast cancer.

*Abstract

Benefits 

· New class of cancer therapeutic compounds 

· Effective across multiple cancer types 

· Specific targeting of cancer cells that minimizes damage to healthy cells 

· Starves cancer cells of their primary energy source for growth, angiogenesis, and metastasis 

Commercial Application 

· Oral cancer therapy targeted against multiple cancer types

*Principal Investigation

Name: Stephen C. Bergmeier, PhD and Xiaozhuo Chen, PhD

Department:

国家/地区

美国