Small Molecule Inhibitors of DYRK1A and Uses Thereof.

Technology #ua14-059

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Categories
Researchers
Christopher Hulme
Professor, Pharmacology & Toxicology
Yeng Jeng Shaw
Research Associate, Pharmacology & Toxicology
Travis Dunckley
Associate Investigator
Managed By
Rakhi Gibbons
Asst. Director, Life Sciences (520) 626-6695

 Title: Small molecule inhibitors of DYRK1A and uses thereof

Invention: The technology presented identifies a series of small molecule inhibitors of DYRK1A for the treatment of Alzheimer’s disease and other neurodegenerative and cognitive diseases.  In particular, the present invention provides design and synthesis methods for a collection of benzimidazole analogs tested in vivo for DYRK1A inhibition using Caliper EZ Reader technique.

Background: The underlying treatment of learning and/or memory disorders is a huge and significantly unmet medical need within the market. In particular, Alzheimer’s disease is a neurodegenerative pathology whose most evident symptom is progressive decline of cognitive functions. Current research suggests that overexpression of DYRK1A may be significant factor leading to cognitive deficits in people with Alzheimer’s disease (AD) and Down Syndrome and treatment options for these are extremely limited. In addition, several protein kinases have been implicated in neuronal development and, in particular, their overexpression and aberrant activation have been shown to play a significant role in the development of AD via tau phosphorylation. The present technology provides insight on small molecule inhibition of DYRK1A activity in the brain as an avenue for pharmaceutical intervention of mental impairment associated with AD and other neurodegenerative diseases

Applications:

  • Alzheimer’s disease therapeutics
  • Down syndrome therapeutics
  • Any therapeutic for neurodegenerative disorders related to DYRK1A activity
  • Any therapeutic for a variety of cancers related to DYRK1A activity
  • General cognitive enhancement

Advantages:

  • Target different and distinct DYRK kinases to address multiple therapeutic needs
  • Addresses unmet medical needs for patients suffering from diseases that significantly impair quality of life
  • DYRK1A inhibitors can also be considered as potential therapeutics for the treatment of developmental diseases such as Down syndrome, and neurodegenerative diseases such as Parkinson’s disease, and Huntington’s disease
  • DYRK1A can phosphorylate sirtuin, a key regulator of learning and memory

Licensing Manager: 

Rakhi Gibbons

rakhig@tla.arizona.edu

(520) 626-6695