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Gregory Lesinski, PhD

Award Name CCTS Pilot 2009
Award Date 04/01/2009


Evaluation of Novel Jak2-STAT3 Inhibitors in Melanoma

Gregory Lesinski, PhD has been awarded a one year pilot grant from the Pilot and Collaborative Transitional and Clinical Science program. Providing researchers with the necessary funds needed to complete preliminary studies, this grant gives Lesinski the opportunity to study a “novel class of anti-cancer, small molecule inhibitors, that are actually derived from a natural product called curcumin.” These inhibitors would target the STAT3 pathway which is highly activated in numerous types of cancer cells, particularly Melanoma.

“Melanoma is the most deadly form of skin cancer and there are very few therapies effective for this type of cancer,” Lesinski said.

Melanoma is rising faster than any other type of cancer in the world, with a response rate of only 10-15% in the most effective therapies available. The goal of this project, which collaborates with the College of Pharmacy, is to discover a new class of compounds that could result in human clinical trials.

The College of Pharmacy designed the new drug, called FLLL-32 using computer modeling. Lesinski and his colleagues tested this compound to validate its ability to kill melanoma cells in cell cultures and animal models. They now have data which shows that this new compound kills melanoma cells in test tubes at relatively low doses. The next step was to look at the overall effects of its use and how specific it was to the anticipated target, without any unwanted side effects.

“In the early experiments it has shown to be very specific, in fact more specific than any other inhibitors that we have worked with in the past,” Lesinski said.

The research team injected the compound into mice and recorded the side effects to follow how long it stays in the system. Finally, the study will determine the efficacy of FLLL-32 to inhibit growth in vivo, by injecting it into mice with cancer.

Although the main purpose is to inhibit STAT3 in cancer cells, this compound could also alter the STAT3 protein in white blood cells, which is thought to be important in turning down the body’s immune response to cancer. Not only could it attack cancer cells, but also help remedy the ill affects cancer has on the host’s white blood cells.

Future research is necessary to refine the potency and structure of the inhibitors that are being tested. After completing larger studies and testing derivative compounds, Lesinski is hopeful this series of compounds might result in a suitable new drug for evaluation in future pre-clinical and possibly even human clinical studies. This could help with the problem of limited, effective therapy available for melanoma patients.

By Samantha Smith, October 05, 2009

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