A novel anti-cancer therapy to target the Proviral Integration of the Moloney murine leukemia virus (PIM) kinases is available for licensing and co-development.

PIM kinases are overexpressed in many solid cancers, which is predictive of poor survival in multiple cancer types. NIH inventors have developed multiple PIM kinase-targeting proteolysis-targeting chimeras (PROTACs) that cause PIM1 degradation in a prostate cancer cell model and increased chemo-sensitization. These compounds target pro-tumorigenic functions of the PIM kinases, which provides superior catalytic inhibition. This also prevents the onset of resistance due to increased expression of PIM kinases.

There are many competitive advantages of this novel anti-cancer therapy:

• Compound target pro-tumorigenic functions of the PIM kinases that are not linked to kinase activity
• Prevention of the onset of resistance due to increased expression of PIM kinases that occurs from catalytic inhibition
• Increased chemo-sensitivity.
• Compared to small molecule inhibitors, PROTACs:
  • Show promise overcoming tumor resistance.
  • Address and degrade undruggable target.
  • Offer novel, rapid, and reversible chemical knockout capabilities.

If you are interested in this technology, please view the PIM-Targeted PROTACs abstract for more information.