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.
- 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
John Beutler (NCI), Antonio Echavarren, Federic Ratel, Tanya Random (NCI)
Lopez-Suarez L, et al. Synthesis and Biological Evaluation of New (-)-Englerin Analogues. [PMID: 27005578]
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