Preparation of Imidazole Pyrimidine Analogues as NEK2 Inhibitors for the Treatment of Cancer

Technology #ua16-229

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Researchers
Haiyong Han
Associate Investigator
Ichiro Nakano
Wenhao Hu
Professor, Chemistry
Brendan Frett
Postdoctoral Research Associate I, Pharmacology and Toxicology
Hong Yu Li
Associate Professor, Pharmacology and Toxicology
Managed By
Rakhi Gibbons
Asst. Director, Life Sciences (520) 626-6695

Title: Preparation of Imidazole Pyrimidine Analogues as NEK2 Inhibitors for the Treatment of Cancer

 

Invention: The invention is new kinds of imidazole pyrimidine analogues that inhibit NEK2 protein kinase and their use in cancer treatment. Initial results have demonstrated their efficacy in inhibiting proliferation of brain tumor stem cells and pancreatic cell lines.

 

Background: The protein kinase NEK2 plays an essential role in the regulation of cell division. NEK2 is frequently over-expressed in a wide variety of cancers, where it is associated with tumorigenesis, tumor progression and contributes to drug resistance. NEK2 is therefore a promising therapeutic target for cancer treatment and great efforts have been made to develop NEK2 inhibitors. However, NEK2 inhibitors are still at an early stage of development, and up to now, no NEK2 inhibitor has been reported to undergo clinical trial.

 

Applications:

  • Cancer treatment
  • Treatment of chemo-resistant cancers like advanced resistant pancreas cancer
  • Potential for combination therapy

 

Advantages:

  • A small molecule synthesized by common chemistry
  • First-in-class NEK2 inhibitors
  • Cancer cells that are resistant to other chemotherapy are sensitive to NEK2 inhibition
  • Inhibits cell proliferation of cancer cells

 

Licensing Manager:

Rakhi Gibbons

RakhiG@tla.arizona.edu

(520) 626-6695