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 (http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3821994/). 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 (cancer.gov). 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

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