Discovery of Allosteric Non-Covalent KRAS Inhibitors

Description:

Activating mutations of KRAS are known to occur in about 25% of all human cancers. Currently, there are no drugs that can directly act on mutated KRAS to stop its cancer causing activities. As a result, KRAS-related cancers, which include some of the deadliest, such as pancreatic cancer, remain untreatable. Finding a direct inhibitor of KRAS remains a major challenge in the search for cancer therapy.

 

Technology:

Dr. Gorfe at the University of Texas Health Science Center Houston has used a structure based computational ligand design approach followed by biophysical and cell biological experiments to discover a novel compound that non-covalently binds to KRAS with nano-molar affinity. This compound abolishes interaction with Raf, and slightly decreases both intrinsic and SOS-mediated nucleotide exchange reactions. This compound semi-selctively inhibits KRAS signaling and KRAS-dependent proliferation of cancer cells.

 

 

Intellectual Property Status:

-Patent Application Pending

Patent Information:

The preceding is intended to be a non-confidential and limited description of a novel technology created at the University of Texas Health Science Center at Houston (UTHealth). This promotional material is not comprehensive in scope and should not replace company’s diligence in a thorough evaluation of the technology. Please contact the Office of Technology Management for more information regarding this technology.
For Information, Contact:
Hannah Nelson
Senior Technology License Associate
University of Texas Health Science Center At Houston
hannah.m.nelson@uth.tmc.edu
Inventors:
Keywords:
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