This technology is a demonstration of a therapeutic strategy to modify the activity of kinases that drive the progression of cancer.
The inhibition of specific kinases or kinase families has proven to be an effective therapeutic strategy to prevent cancer growth. Most existing kinase inhibitors function as competitive inhibitors at the kinase active site. The development of alternative methods of altering kinase activity holds promise for the treatment of multiple diseases including, but not limited, to cancer.
This technology identifies amino acid modifications which can regulate the activity of certain protein kinases, in particular CMGC (cyclin-dependent) kinases, which control the cell cycle and are dysregulated in most cancers. By modulating the prolyl hydroxylation status of CMGC kinases, kinase activity can be inhibited or activated. This technology is applicable to dual-specificity tyrosine-phosphorylation-regulated kinases (DYRKs), MAPK, GSK3, HIPK, or CDK kinases. As such, these allosteric modulators can be developed as inhibitors or activators of kinase activity to treat cancer.
This technology has been validated in human cell lines.
IR CU20395
Licensing Contact: Kristin Neuman