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Thursday, 04/23/2015 4:07:19 PM

Thursday, April 23, 2015 4:07:19 PM

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http://www.pharmacychoice.com/news/article.cfm?Article_ID=1360614

4/22/15 - Regen BioPharma Inc. Announces Small Molecule Drug Discovery Milestones at the American Association for Cancer Research's 2015 Annual Meeting
By a News Reporter-Staff News Editor at Biotech Week Regen BioPharma Inc. (OTCBB: RGBP) (OTC PINK: RGBP) announced the acceptance of its abstract "Discovery of retinoic acids as low affinity inhibitors of the leukemia stem cell target NR2F6" at the American Association for Cancer Research Annual Meeting taking place April 18-22, 2015 in Philadelphia, Pennsylvania.

Christine Ichim, PhD, first author of the abstract and Director of Molecular Therapeutics for Regen BioPharma Inc., will be presenting major milestones in the drug discovery process for small molecule inhibitors of the cancer stem cell gene NR2F6. Cancer stem cells are a novel and coveted therapeutic target in cancer research because they represent the cancer cells that are immortal.

Most cancer cells do not divide or can only divide a limited number of times. On the other hand, cancer stem cells can divide an unlimited number of times making them immortal. While conventional chemotherapy kills the most populous cancer cells, cancer stem cells are often resistant to cancer therapy. The resistance of cancer stem cells to conventional cancer therapy is believed to be the main reason for disease relapse and drug resistance.

Regen BioPharma has recently acquired intellectual property to the cancer stem cell gene NR2F6 and began developing drugs against this therapeutic target from researchers at the University of Toronto.

Regen BioPharma will be announcing at the American Association for Cancer Research Annual Meeting attainment of significant milestones in the drug discovery process, specifically assay development and hit identification. Discussed in the presentation will be the proprietary experimental system that was used to identify small molecules that bind to the active site of the NR2F6 gene product. NR2F6 encodes a nuclear receptor. It is known that this family of drug targets contain an active site called the ligand binding domain. This portion of the protein is the "on-off" switch of its activity. Regen BioPharma has devised a method of zeroing in on this part of the protein, which allows for screening of drugs that selectively that bind to, and turn off the switch. Using this method, existing compounds have been tested for binding as a method of validating the system before novel compounds can be tested for efficacy.

Using this technique, researches showed that retinoic acid was able to activate the assay at supra-physiological concentrations, acting as a "hit". "The role of retinoids as agents of differentiation in embryology, stem cell biology and the maturation of blood cells has been well established. That retinoic acid can bind to our gene, albeit at super-physiological concentrations, is exciting because it validates our initial observation that our target gene functions to inhibit differentiation and to maintain cancer cells in a stem cell state. It validates the hypothesis that by turning off our gene using a small molecule like retinoic acid, we can target specifically the cancer stem cells to mature," said Dr. Christine Ichim.

"The in vitro validation of the critical role of NR2F6 in cancer stem cell maintenance using shRNA, combined with the in vivo validation that NR2F6 transfection causes cancer, strongly convinces us of the therapeutic relevance of our target. The results which will be disclosed at the AACR meeting are the first step in development of small molecule drugs addressing the problem of cancer stem cells," said Thomas Ichim, PhD, Chief Scientific Officer of Regen BioPharma (see also Stem Cells).

Keywords for this news article include: Cancer, Therapy, Oncology, Stem Cell Research.

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