Technology ID
TAB-4191

Renal Selective Unsaturated Englerin Analogues

E-Numbers
E-072-2014-0
Lead Inventor
Beutler, John (NCI)
Co-Inventors
Ransom, Tanya (NCI)
Echavarren, Antonio (Institute of Chemical Research of Catalonia (ICIQ))
Ratel, Frederic (Institute of Chemical Research of Catalonia (ICIQ))
Applications
Therapeutics
Therapeutic Areas
Oncology
Infectious Disease
Endocrinology
Development Stages
Discovery
Lead IC
NCI
ICs
NCI

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
Licensing Contact:
Hastings, Whitney
whitney.hastings2@nih.gov