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Cancer Treatment Decreases Side Effects of Treatment

Technology #z07120

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HA 14-1 is a qualified antagonist against Bcl-2 proteins.Bcl-2 Proteins prevent apoptosis in cancer cells, allowing them to survive cancer treatments.  sHA 14-1 increases apoptosis.sHA 14-1 lowers cancer treatment side effects by increasing the cancer cell?s sensitivity to cancer drugs and allowing lower dosages to be effective.Bcl-2 proteins inhibit apoptosis and have been linked to resistance of chemotherapy, radiotherapy, and hormone treatments.
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Researchers
Chengguo (Chris) Xing, Ph.D
Associate Professor, Medicinal Chemistry, College of Pharmacy
Managed By
Raj Udupa
Technology Licensing Officer 612-624-3966
Patent Protection
US Patent 8,394,794

Cancer Treatment with sHA 14-1 Reduces Side Effects by Increasing Programmed Cell Death

Bcl-2 Proteins Inhibit Apoptosis and Increase Drug Resistance to Cancer Treatment

An antagonist that targets anti-apoptotic Bcl-2 proteins has been developed for potential treatment of cancer. The Bcl-2 protein inhibits programmed cell death, or apoptosis, in cancer cells. In tumor cells, over expression of Bcl-2 has been correlated with the development of resistance to chemotherapy, radiotherapy, and hormone treatments. Because of drug resistance due to Bcl-2 proteins, cancer treatment dosages are increased to be more effective, but this leads to greater side effects.

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Bcl-2 Protein Antagonists Improve the Effectiveness of Cancer Treatment

HA 14-1 is a qualified antagonist against the anti-apoptotic Bcl-2 protein. The HA 14-1 molecule is an inhibitor that can sensitize cancer cells to cancer treatments, thereby lowering the effective dosage of anticancer agent and lowering the side effects. New analogs of HA 14-1 have demonstrated improved binding interaction with anti-apoptotic Bcl-2 proteins. One of these analogs, sHA 14-1, has greater stability compared to HA 14-1 but displays similar effectiveness on cancer cells. sHA 14-1 is insensitive to the drug resistance induced by anti-apoptotic Bcl-2 proteins in cancer cells. sHA 14-1 also synergizes the anti-cancer activities of both intrinsic and extrinsic apoptotic stimuli, increasing the potential of sHA 14-1 in cancer therapy.

BENEFITS OF Bcl-2 PROTEIN ANTAGONIST sHA 14-1 IN CANCER TREATMENT:

  • Candidate for the treatment of drug-resistant cancers either as a monotherapy or in combination with current cancer treatments
  • sHA 14-1 analog can sensitize cancers to cancer treatment as an antagonist to Bcl-2
  • Reduces side effects by lowering the effective dosage of anticancer agent

Phase of Development HA14-1 analogues have been synthesized and tested for stability. In vitro binding assays have identified optimum structures and in vivo studies have been completed.