Renal Selective Unsaturated Englerin Analogues

Description:

Abstract:

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.

Competitive Advantages:

  • PKC theta associated with a number of immune disorders, cancers, and HIV
  • Reduced toxicity compared to parent Englerin A compounds

Commercial Applications:

  • Renal cancer therapeutic
  • HIV therapeutic
Patent Information:
For Information, Contact:
Whitney Hastings
NIH Technology Transfer
240-276-5530
whitney.hastings2@nih.gov
Inventors:
John Beutler
Tanya Ransom
Antonio Echavarren
Frederic Ratel
Keywords:
Beutler
DIABETES
HIV
renal cancer
small molecule
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