Medical device company Qualigen Inc revealed on Thursday that it has entered into a Sponsored Research Agreement (SRA) with University of Louisville (UofL) for development of several small-molecule RAS Inhibitor drug candidates.
Pursuant to the SRA, Qualigen assumed funding responsibility for this RAS programme from 1 April 2019 through 30 September 2020.
RAS is the most common oncogene in human cancer, Qualigen said. Activating mutations in one of the three human RAS gene isoforms (KRAS, HRAS, or NRAS) are present in about one-quarter of all cancers. The mutant KRAS is found in 98% of all pancreatic ductal adenocarcinomas, 52% of all colon cancers and 32% of all lung adenocarcinoma, resulting in more than 120,000 deaths every year in the US.
The technology was reportedly developed at UofL with key support from several programmes, including UofL's ExCITE, a National Institutes of Health Research Evaluation and Commercialization Hub (REACH).
RAS is a G-protein that works as a switch, toggling between "on" and "off" when bound to guanosine nucleotides, GTP or GDP. The RAS mutations found in cancer cause this protein to be turned on most of the time. Most drug targets are proteins that have a well-defined "pocket" that can be targeted by small molecules. RAS lacks such pockets and thus is more difficult to target directly, but the UofL team has been able to develop small molecules that are protein-protein interaction (PPI) inhibitors which block the binding of RAS to its effector proteins.
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