Non-ATP Competitive PLK 1 Polo-dox Domain Inhibitors as Anti-tumor Therapeutics

Description:

Reference #: 00881

The University of South Carolina is offering licensing opportunities for a PLK1 polo-box domain inhibitor that makes cancer treatment more effective by targeting cancer cells for destruction while alleviating the harmful therapeutic toxicity that occurs from the use of existing remedies.

Potential Applications:

This therapy opens new therapeutics for cancer treatment without the traditional effects of toxicity to healthy cells.

Advantages and Benefits:

  • Is non-ATP competitive
  • Selectively targets the polo-box domain of PLK1
  • Is not toxic to normal cells

Background:

Cancer is the leading cause of death worldwide, and the World Health Organization estimates that 12 million new cases will be diagnosed yearly. Polo-like kinase 1 (PLK1), which is made up of a kinase domain and a polo box domain (PBD), has been shown to be over-expressed in a number of tumors and has a prognostic value in cancer, making it a good therapeutic target for cancer treatment. Current kinase inhibitors on the market are almost exclusively ATP-competitive, inhibiting the ATP binding pocket of the kinase domain. These treatments effectively kill cancer cells, but with their success they bring unwanted side effects. Because the ATP binding pocket is highly conserved amongst the kinase family, these ATP-competitive inhibitors cannot discriminate amongst the kinases easily. Therefore, traditional kinase inhibitors can have undesirable toxicity to healthy cells.

Invention Description:

This new method inhibits the PBD domain of PLK1 to create a non-ATP competitive therapy to inhibit tumor growth. Unlike traditional therapies, which are ATP-competitive, this therapy selectively inhibits cancer cells without being toxic for normal cells.

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Fragment Ligated Inhibitors Selective for the Polo Box domain of PLK1 Utility United States 13/365,707 9,175,357 2/3/2012 11/3/2015    
For Information, Contact:
Technology Commercialization
University of South Carolina
technology@sc.edu
Inventors:
Campbell Mcinnes
Doaa Boshra Farag
Keywords:
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