Novel Protein Kinase C Delta Activators
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 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.
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.
- Oncology therapeutics
- 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