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Novel Protein Kinase C Delta Activators

Life Sciences
Therapeutics
Drugs / Pharmaceuticals
College
College of Pharmacy
Researchers
Chen, Ching-Shih
Byrd, John
Kulp, Samuel
Muthusamy, Natarajan
Wang, Dasheng
Licensing Manager
Davis, Stewart
6142927170
Davis.6014@osu.edu

T2011-054 A novel anti-cancer agent (OSU-2S) that is devoid of S1P1 receptor activity and is highly effective in suppressing hepatocellular carcinoma tumor growth in vivo.

The Need

The third leading cause of cancer death worldwide is hepatocellular carcinoma (HCC). Due to the rise in the incidence of hepatitis C virus infection, HCC is expected to increase in the United States. Many patients with HCC are not candidates for surgery because of the location or size of their tumor. Furthermore, current drugs, such as FTY720, have undesired side effects, including infections, cardiovascular complications, and brain inflammation. Alternative antitumor agents with less side effects are needed for better treatment of HCC.

    The Technology

    Researchers at The Ohio State University, led by Dr. Ching-Shih Chen, have developed a novel FTY720 analogue, OSU-2S. This new drug is an anti-cancer therapeutic agent that is non-immunosuppressive and inhibits cell growth by activating the PKCdelta signaling pathway. This anti-tumor agent developed induces 80% apoptosis in hepatocellular carcinoma cells and has a higher in vitro and in vivo potency than the parent compound. Furthermore, the drug is less cytotoxic, which makes it a good candidate for pairing with genotoxic agents as a therapeutic strategy.

    Commercial Applications

    • Oncology therapeutics

    Benefits/Advantages

    • Induces 80% apoptosis in hepatocellular carcinoma cells
    • Higher in vitro and in vivo potency than parent compound
    • Able to activate PKCdelta, making it a good candidate for pairing with genotoxic agents