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Renal Selective Unsaturated Englerin Analogues

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Summary
Researchers at the National Cancer Institute (NCI) have developed a number of analogs of the natural product englerin A, an inhibitor of renal cancer cell growth. Englerin A is thought to exert its anticancer effects by activating protein kinase C (PKC) theta, and exert cytotoxic effects through activation of transient receptor potential cation (TRPC) channels. The invention englerin analogues provide promising treatment strategies for various cancers, diabetes, and HIV, and other diseases associated with the PKC theta and/or TRPC ion channel proteins. Researchers at the NCI seek licensing and/or co-development research collaborations for englerin A analogue compounds.
NIH Reference Number
E-072-2014
Product Type
  • Therapeutics
Keywords
  • small molecule, Renal Cancer, Diabetes, HIV, Beutler
Collaboration Opportunity
This invention is available for licensing and co-development.
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Description of Technology

Englerin A, a natural product, has shown growth-inhibiting activity against renal cancer cell lines. The compound is an agonist of protein kinase C (PCK) theta, which results in cell cytotoxicity, insulin inhibition, and selective activation of viral replication in T cells.  Englerin A derivatives are promising treatment strategies for any diseases associated with PKC theta and/or ion channel proteins.

Researchers at the National Cancer Institute have developed a series of Englerin A analogs for the treatment of renal cancer. The new derivatives are less toxic than the parent compound and have shown effective inhibition of growth in vitro.

Potential Commercial Applications
  • Renal cancer therapeutic
  • HIV therapeutic
Competitive Advantages
  • PKC theta associated with a number of immune disorders, cancers, and HIV
  • Reduced toxicity compared to parent Englerin A compounds
Inventor(s)

John Beutler (NCI), Antonio Echavarren, Federic Ratel, Tanya Random (NCI)

Development Stage
  • Basic (Target Identification)
Publications

Lopez-Suarez L, et al. Synthesis and Biological Evaluation of New (-)-Englerin Analogues.  [PMID: 27005578]

Patent Status
  • U.S. Provisional: U.S. Provisional Patent Application Number 62/146,805, Filed 13 Apr 2015
  • U.S. Patent Filed: U.S. Patent Application Number PCT/US2016/027262, Filed 13 Apr 2016
  • Foreign Filed: - Patent Application 2016247920, Filed 27 Sep 2017
  • Foreign Filed: - Patent Application , Filed 12 Oct 2017
  • Foreign Filed: - Patent Application 16718144.5, Filed 11 Oct 2017
  • Foreign Filed: - Patent Application 2017-554513, Filed 12 Oct 2017
  • U.S. Patent Filed: U.S. Patent Application Number 15/564,353, Filed 04 Oct 2017
Related Technologies
Therapeutic Area
  • Cancer/Neoplasm
  • Infectious Diseases
  • Hormonal Systems, Endocrine, and Metabolic Diseases
Updated
Wednesday, August 1, 2018