Technologies
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WARF: P100028US02

BACE1 Inhibitors Reduce β-Amyloid Production, Provide Potential Treatment for Alzheimer’s Disease


INVENTORS -

Luigi Puglielli

The Wisconsin Alumni Research Foundation (WARF) is seeking commercial partners interested in developing inhibitors of the enzyme BACE1 that may be useful in the treatment of Alzheimer’s disease.
OVERVIEWAlzheimer’s disease is the most common form of dementia, affecting an estimated 27 million people worldwide. This disease has a large economic impact with estimated direct and indirect costs of $148 billion annually in the United States.

Plaques composed of aggregated β-amyloid peptide, which accumulate in the brains of patients with Alzheimer’s disease, play a key role in the pathogenesis of the disease. β-amyloid is formed when the enzyme BACE1 cleaves the β-amyloid precursor protein. Because BACE1 is the rate-limiting step in β-amyloid formation, it is considered a potential therapeutic target. A UW–Madison researcher previously showed that BACE1 is transiently acetylated by the acetyltransferases ATase1 and ATase2, a modification important to its role in β-amyloid production.
THE INVENTIONThe UW–Madison researcher now has identified two compounds that can downregulate BACE1 levels and the rate of β-amyloid production and thus may be potential therapeutics for Alzheimer’s disease. These compounds inhibit the activity of ATase1 and ATase2.
APPLICATIONS
  • Prevention or treatment of Alzheimer’s disease
KEY BENEFITS
  • Successfully tested in cellular systems and an animal model of Alzheimer’s disease
  • May delay the onset or progression of symptoms of Alzheimer’s disease
ADDITIONAL INFORMATION
For More Information About the Inventors
Related Intellectual Property
Publications
  • Ding Y., Ko M.H., Pehar M., Kotch F., Peters N.R., Luo Y., Salamat S.M. and Puglielli L. 2012. Biochemical Inhibition of the Acetyltransferases ATase1 and ATase2 Reduces β-secretase (BACE1) Levels and Aβ Generation. J. Biol. Chem. 287, 8424-8433.
Contact Information
For current licensing status, please contact Rafael Diaz at rdiaz@warf.org or 608-960-9847.
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UW–Madison has the integrative capabilities to complete many key components of the drug development cycle, from discovery through clinical trials. As one of the top research universities in the world, and one of the two best-funded universities for research in the country, UW–Madison offers state-of-the-art facilities unmatched by most public universities.

These include the Small Molecule Screening Facility at the UW Comprehensive Cancer Center; the Zeeh Pharmaceutical Experiment Station, which provides consulting and laboratory services for developing formulations and studying solubility, stability and more; the Waisman Clinical Biomanufacturing Facility; the Wisconsin Institute for Medical Research, which provides UW–Madison with a complete translational research facility; and the innovative, interdisciplinary Wisconsin Institutes for Discovery, home to the private, nonprofit Morgridge Institute for Research and its public twin, WID, part of the university's graduate school. The highly qualified experts at these facilities are ready to work with you to create a library of candidates for drug development.