Regen BioPharma Sees Additional Positive Results for Modulating NR2F6 Checkpoint

Regen BioPharma states that progress continues to be achieved by Regen in developing small molecule drugs that activate and inhibit NR2F6. The company reports that ChemDiv, Regen's medicinal chemistry partner, has currently identified three series of compounds which activate NR2F6. These compounds are further being refined to increase levels of modulation in the checkpoint. Regen is working towards small molecule therapies that can treat cancer as well as autoimmune disorders such as arthritis and lupus. These compounds have been identified from Regen's patented screening methodology and unique chemical libraries. ChemDiv is a fully integrated Target-to-Clinic Contract Research Organization headquartered in San Diego, CA.

Tests on each of these three structures and their analogues have resulted in one particular series becoming the favored activator. Over 250 analogues of this favored structure have been tested and there is a clear relationship between their structure and ability to activate NR2F6.

The NR2F6 nuclear receptor has been identified as a potentially extremely important immune cell inhibitor and cancer stem cell differentiator. Molecules which function as immune cell inhibitors are called 'immune checkpoints' and basically act as an 'on or off switch' to an immune response. Cancer cells sometimes find ways to use these checkpoints to avoid being attacked by the immune system therefore therapies that target these checkpoints demonstrate tremendous potential as cancer treatments.

The NR2F6 program at Regen aims to identify antagonists of NR2F6 in an effort to unleash the cancer-killing potential of a patient's own immune system as well as identifying agonists which should suppress the immune system in diseases where the immune system is over-activated, such as autoimmunity.

"It is exciting to see a structure-function relationship emerging with one class of our activator compounds," Harry Lander, Ph.D., MBA, President and Chief Scientific Officer of Regen said. "It clearly binds to the ligand binding domain of NR2F6 and it is encouraging to see that it does not display any toxicity at high concentrations in cellular systems. Of course it remains early in the process, but we seem to be hitting all the key points as the drug optimization process progresses. Once we are comfortable with our activator series, we will focus on developing our inhibitor series."