Cancer Treatment Through hTERT InhibitionTechnology #ua16-091
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- Laurence Hurley Professor, Pharmacology & Toxicology
- Vijay Gokhale Senior Research Scientist, BIO5
- HyunJin Kang Postdoctoral Research Associate I, Pharmacology & Toxicology
- Kui Wu Postdoctoral Research Associate I, Pharmacology & Toxicology
- Managed By
- Rakhi Gibbons Asst. Director, Life Sciences (520) 626-6695
Title: Cancer Treatment Through hTERT Inhibition
Invention: The invention is a small molecule that reduces human telomerase reverse transcriptase (hTERT), which is highly activated in cancer cells.
Background: In 2010, approximately 73,599 U.S. patients were diagnosed with melanoma with 8,700 of those incidences resulting in death. A hallmark of cancer, and melanoma specifically, overexpression of hTERT results in cell immortalization. These types tumors have transcription-activating mutations in the hTERT promoter region because of a pair of G-quadruplexes. The small molecule binds selectively to the G-quadruplex in the hTERT promoter mutant, reducing transcription activity. This technology has the potential to fill an unmet need in a market where only two effective drugs, with a host of side effects, are available for treating melanoma.
- An anticancer drug for a variety of cancers with an overexpression of hTERT, especially melanoma and glioma
- Direct inhibition of the hTERT promoter produces apoptosis within 2-5 days versus targeting the telomeric structure
- The small molecule has greater cellular selectivity over BRACO-19, a similar agent in mechanism of action
- Poised to fill the market demand for improved survival rate and reduced drug toxicity