Renal Selective Unsaturated Englerin Analogues


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: Competitive Advantages:
  • Renal cancer therapeutic
  • HIV therapeutic
 
  • PKC theta associated with a number of immune disorders, cancers, and HIV
  • Reduced toxicity compared to parent Englerin A compounds


Development Stage:
Basic (Target Identification)

Related Invention(s):
E-064-2008
E-090-2014
E-140-2017


Inventors:

John Beutler (NCI)  ➽ more inventions...

Antonio Echavarren (NCI)  ➽ more inventions...

Federic Ratel ()  ➽ more inventions...

Tanya Random ()  ➽ more inventions...


Intellectual Property:
Application No. 62/146,805
Application No. PCT/US2016/027262
Application No. 2016247920
Application No. 16718144.5
Application No. 2017-554513
Application No. 15/564,353

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

Collaboration Opportunity:

Licensing and research collaboration


Licensing Contact:
John Hewes, Ph.D.
Email: John.Hewes@nih.gov
Phone: 240-276-5515

OTT Reference No: E-072-2014
Updated: Aug 1, 2018