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Use of Englerin A, a Small Molecule HSF1 Activator, for the Treatment of Diabetes, Obesity, and Other Diseases Associated with I

Posted Mar 22 2012 8:00pm

Description of Invention:
Insulin resistance is a causative factor for type 2 diabetes, obesity and a number of other conditions. This technology claims methods for treating diseases or conditions associated with insulin resistance using the small molecule epoxy-guaiane derivative englerin A and related compounds. The compounds are claimed separately in a related NIH technology.

The inventors have shown that englerin A, a compound originally isolated from the Phyllanthus plant and previously identified as an anti-cancer agent, can also be used to treat insulin resistance. Insulin resistance is associated with reduced gene expression and production of heat shock protein 70 (HSP70). Using a mouse with tumor model, the inventors discovered that administration of englerin A decreases blood glucose levels by activating transcription of HSF1, thereby increasing the expression and secretion of HSP70. Thus, englerin A and related compounds represent potential drugs for the treatment of a variety of conditions associated with insulin resistance.

Applications:
Treatment of diseases or conditions associated with insulin resistance, such as type 2 diabetes, obesity, inflammation, metabolic syndrome, polycystic ovary disease, arteriosclerosis, non-alcoholic fatty liver disease, reproductive abnormality of a female, and growth abnormality.

Advantages:
Use of small-molecule compounds targeting HSF1 represents a novel approach to the treatment of type 2 diabetes and other conditions caused by insulin resistance.

Development Status:
  • In vitro data available
  • In vivo data available (animal)


Inventors:
Leonard M Neckers (NCI)


Patent Status:
HHS, Reference No. E-042-2012/0
US, Application No. 61/584,526 filed 09 Jan 2012


Related Technologies:
US, Application No. 12/811,245 filed 29 Jul 2010, Reference No. E-064-2008/2 , and related international applications


Relevant Publication:
  1. Ratnayake R, et al. [ PMID 19061394 ]


Collaborative Research Opportunity:
The NCI Urologic Oncology Branch is seeking statements of capability or interest from parties interested in collaborative research to further develop, evaluate, or commercialize epoxyguaianes as anti-type 2 diabetes agents. For collaboration opportunities, please contact John Hewes, Ph.D. at hewesj@mail.nih.gov .


For Licensing Information Please Contact:
Tara Kirby Ph.D.
NIH Office of Technology Transfer
6011 Executive Blvd. Suite 325,
Rockville, MD 20852
United States
Email: tk200h@nih.gov
Phone: 301-435-4426
Fax: 301-402-0220


Ref No: 2390

Updated: 03/2012

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