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Apoptosis Inducing Cancer Therapeutic Agents

Life Sciences
College of Pharmacy
Chen, Ching-Shih
Shaw, Yeng-Jeng
Licensing Manager
Paschall, Christopher

T2004-100 R1-adrenoreceptor antagonists that promote apoptosis in cancer cells.

The Need

The Akt pathway is one of the most commonly hyper-activated pathways in human cancers ( Once activated, the Akt protein works to maintain and regulate the survival and proliferation of the cell. Current treatment of cancer is a combination of chemotherapy, radiation, and biological therapy which are lacking in efficacy and can result in many harmful side effects for the patient ( To improve the effectiveness of cancer therapy, a novel drug that could act on the Akt pathway and promote apoptosis of cancerous cells needs to be developed.

    The Technology

    The Ohio State University researchers, led by Dr. Ching-Shih Chen, developed a new class of therapeutic agents that have been structurally modified from the R1-adrenoreceptor antagonist, doxazosin, to improve the outcomes of cancer treatment. These therapeutic agents function by inhibiting the activation of the intracellular protein, Akt. This protein plays a vital role in cell survival and proliferation, thus its inhibition results in cell death. Dr. Chen’s agents are being developed into a new line of cancer therapeutic drugs that induce apoptosis with improved efficiency in mutated cancer cells.

    Commercial Applications

    • Cancer therapeutics


    • Improved efficacy in blocking intracellular Akt activation and inducing apoptosis than parent compound, doxazosin
    • Active in suppressing the growth of 60 cancer cell lines
    • Lead compounds 33 and 44 have IC50 values of 2.2 and 1.5µM, respectively
    • Lead compound 33 exhibits an order of magnitude higher potency than parent compound in triggering apoptotic death in PC-3 cells