Technology Bundle ID
TAB-2224

Selective 12-Human Lipoxygenase Inhibitors for the Treatment of Diabetes and Clotting

Applications
Diagnostics
Linked ID
E-134-2010-0
Lead Inventors
David Maloney (NCATS)
Co-Inventors
Ajit Jadhav (NCATS)
Anton Simeonov (NCATS)
Jerry Nadler (Eastern Virginia Medical School)
Michael Holinstat (Thomas Jefferson University)
Theodore Holman (University of California, Santa Cruz)
Development Status
Pre-clinical
Therapeutic Areas
Cardiology
ICs
NCATS
This invention discloses small molecule inhibitors of human 12-lipoxygenase (12-hLO). 12-lipoxygenase expression, activation, and lipid metabolites have been implicated in type 1 and type 2 diabetes, cardiovascular disease, hypertension, Alzheimer’s, and Parkinson’s disease. The development of 12-hLO inhibitors may be a potent intracellular approach to decreasing the ability of platelets to form large clots in response to vessel injury or activation of the coagulation pathway. Thus, 12-hLO inhibition has the potential to attenuate platelet-mediated clot formation caused by diabetes and/or cardiovascular disease and significantly decrease the occurrence of myocardial infarction and death. Moreover, Type 1 and Type 2 diabetes are serious disorders that can lead to major complications and reduced lifespan. An unmet medical need is to identify new ways to protect beta cells in these metabolic disorders. A selective 12-hLO inhibitor could provide a new therapeutic approach to prevent or treat either form of diabetes.
Commercial Applications
  • Therapeutic developments (blood clots; Type 1 and Type 2 diabetes, cardiovascular disease, and neurodegenerative diseases)
  • Inflammatory responses
Competitive Advantages
  • Small molecule (series of analogs can be derived in search of improved performances and/or different functions)
  • Selective inhibitor of human 12-lipoxygenase

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