Renal Selective Unsaturated Englerin Analogues

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: