Treating Cancer Using Synthetic Peptide Inhibitors Derived from BRAF Protein

Braftide is a synthetic peptide inhibitor that works via a novel dual mechanism of action to inhibit BRAF, a protein that is responsible for cell proliferation, differentiation, and migration.  This protein is an integral part of the MAP kinase / ERK signaling pathway. Mutations in BRAF have been identified in melanoma, colorectal cancer, non-Hodgkins lymphoma, thyroid carcinoma, hairy cell leukemia, and non-small cell lung cancer.  The most common mutation in the BRAF gene is the V600E mutation, which is found to be promoting a multitude of cancers including non-small cell lung cancer.

Dr. Wang and the University of the Sciences investigators believe a reduction in BRAF kinase activity could be used as an adjunct therapy in treating certain types of cancer.

Inventors envision Braftide being used as a combination therapy with current FDA-approved ATP- competitive inhibitors like Dabrafenib and Vemurafenib. These drugs can paradoxically activate the MAPK pathway at lower concentration, which remains a primary drawback. Braftide can help in mitigating this activation and in improving the potency of Dabrafenib/ Vemurafenib.

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