A novel approach to the development of new and effective cancer treatment options.
Background: The Mixed Lineage Leukemia 1 (MLL1) protein is a member of the SET1 family of proteins. Mutations of the MLL1 core complex leads to excessive di- and trimethylation of H3K4 which alters gene regulation. This has been linked to certain types of leukemia, solid tumors, and psychotropic disorders such as schizophrenia and bipolar disorders. The minimal complex required for di- and trimethylation of H3K4 includes MLL1 or SETd1a, WDR5, RbBP5, Ash2L and DPY-30. The protein WDR5 bridges the catalytic SET domain of SET1 family proteins and the regulatory components of RbBP5 and Ash2L. Currently, there are no approaches for inhibiting the formation of SET1 family core complexes for the treatment of leukemia and other disorders.
Technology Overview: This technology from Upstate Medical University provides peptide-based inhibitors of the SET1 family core complexes. These peptides can be used to inhibit the growth of cancer cells. These peptide inhibitors can inhibit the enzymatic activity of complexes of MLL1 and SETd1A. The peptide inhibitors may act by inhibiting the formation of, or by disrupting, MLL1 and SETd1A complexes. The peptide inhibitors may also enhance the activity of MLL3, which is a known tumor suppressor. The administration of a compound based on this approach can be used alone or combined with chemotherapy, radiation therapy, surgical removal of tumors, or combinations thereof, and/or with a diagnostic technique.
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Advantages: This technology provides a new approach for the development of compounds that could treat various forms of cancer. It may also be used for the development of treatments for psychotropic disorders.
Applications: The primary application for this technology is cancer treatment. It may also be used for the treatment of psychotropic disorders such as schizophrenia and bipolar disorders.
Intellectual Property Summary: This technology is covered by the patent US 10392423 B2, “Peptide-Based Inhibitors of MLL / SET1 Family Core Complexes.” https://patents.google.com/patent/US10392423B2/
Stage of Development: TRL 3 - Experimental proof of concept
Licensing Status This technology is available for licensing.
Licensing Potential This technology will be of value to any company or institution involved in treating cancer. This includes: • Pharmaceutical companies • Hospitals • Research centers