BERKELEY, CA (UroToday.com) - One of the advantages of englerin A (EA) is its potent cytotoxicity against renal cell carcinoma (RCC) that is independent of the von Hippel-Lindau (VHL) tumor suppressor gene. This indicates that EA can be an effective therapy for RCC that is VHL competent or deficient, and therefore applicable to a broader patient group.
Our very recent results from metabolomics experiments indicate that EA disrupts the cellular metabolism of RCC causing cell stress, and ultimately cell death. This attribute of EA most likely is the basis for its selective cytotoxicity to RCC. The selectivity of EA for RCC is highly unique in that no other cancer type appears to be nearly as sensitive to the cytotoxicity of EA as RCC. In addition its potent selectivity, EA also appears to have some suitable drug properties. Our calculations indicated that EA has properties that conform to the Lipinski’s rule of five, and, as such, is predicted to have a lower attrition rate during clinical trials and hence have an increased chance of reaching the market, if developed.
In conclusion, we anticipate that EA has enormous potential as a treatment strategy for RCC -- not only in humans, but also in companion animals.
Ayse Batova, PhD as part of Beyond the Abstract on UroToday.com. This initiative offers a method of publishing for the professional urology community. Authors are given an opportunity to expand on the circumstances, limitations etc... of their research by referencing the published abstract.
Department of Pediatrics, Hematology/Oncology University of California San Diego