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

Posted Feb 16 2011 7:00pm

Description of Invention:
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.

  • Therapeutic developments (blood clots; Type 1 and Type 2 diabetes, cardiovascular disease, and neurodegenerative diseases)
  • Inflammatory responses

  • Small molecule (series of analogs can be derived in search of improved performances and/or different functions)
  • Selective inhibitor of human 12-lipoxygenase

Development Status:
Pre-clinical; no animal data

David J Maloney (NHGRI)
Theodore Holman (University of California, San Diego)
Jerry L Nadler (Eastern Virginia Medical School)
Michael Holinstat (Thomas Jefferson University)
Anton M Simeonov (NHGRI)
Ajit P Jadhav (NHGRI)

Patent Status:
HHS, Reference No. E-134-2010/0
US, Application No. 61/345,708 filed 18 May 2010

Licensing Status:
Available for licensing.

Internal Medicine
Internal Medicine - Diagnostics

For Licensing Information Please Contact:
Steven Standley Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Phone: 301-435-4074
Fax: 301-402-0220

Ref No: 2224

Updated: 02/2011

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