P12 - Selective Targeting of Prostate Cancer using the Warburg Effect

presented by

Sergey Dyshlovoy
Department of Internal Medicine II (Oncology Center), University Medical Center Hamburg-Eppendorf ; Martini-Klinik at the University Medical Center Hamburg-Eppendorf

Cancer cells consume larger amounts of glucose in comparison to non-malignant cells, a phenomenon known as the Warburg effect. In prostate cancer increased expression of glucose transporters (e.g. GLUT-1) has been found. For this reason, we decided to take advantage of this phenomenon to specifically target prostate cancer cells. Therefore, we have chemically conjugated the active molecule (1,4-naphthaquinone derivative) with glucose in order to increase its specifically and selectivity towards prostate cancer cells. To date, several “generations” of these compounds were synthesized and tested stepwise. Compounds belonging to the latest generation were found to have the best biomedical properties showing highest selectivity towards cancer cells. This resulted in promising activity and safety in vivo, with improved stability in the blood. Using proteomics followed by the bioinformatical analysis of the data and further experimental validation mitochondria have been shown to be a primary target of these compounds in cancer cells.

Contact: s.dyshlovoy@uke.de


  • In vitro and in vivo investigations of novel 1,4-napthoquinone sulphomethylene carbohydrate conjugates in prostate cancer    .     Busenbender T., Dyshlovoy S., Kaune S., Boeckelmann L., Lange T., Schumacher U., Pelageev D.N., Sabutskii Yu.E., Borisova K., Anufriev V.Ph., Graefen M., Bokemeyer C., von Amsberg G. Journal of Clinical Oncology. 2021. V. 39. No. 6_suppl. P. 104-104. doi: 10.1200/JCO.2021.39.6_suppl.104

    Inspired by Sea Urchins: Warburg Effect Mediated Selectivity of Novel Synthetic Non-Glycoside 1,4-Naphthoquinone-6S-Glucose Conjugates in Prostate Cancer. Dyshlovoy SA, Pelageev DN, Hauschild J, Sabutskii YE, Khmelevskaya EA, Krisp C, Kaune M, Venz S, Borisova KL, Busenbender T, Denisenko VA, Schlüter H, Bokemeyer C, Graefen M, Polonik SG, Anufriev VP, Amsberg GV.Mar Drugs. 2020 May 11;18(5):251. doi: 10.3390/md18050251.PMID: 32403427

    Successful Targeting of the Warburg Effect in Prostate Cancer by Glucose-Conjugated 1,4-Naphthoquinones. Dyshlovoy SA, Pelageev DN, Hauschild J, Borisova KL, Kaune M, Krisp C, Venz S, Sabutskii YE, Khmelevskaya EA, Busenbender T, Denisenko VA, Pokhilo ND, Atopkina LN, Graefen M, Schlüter H, Stonik VA, Bokemeyer C, Anufriev VP, von Amsberg G.Cancers (Basel). 2019 Oct 30;11(11):1690. doi: 10.3390/cancers11111690.PMID: 31671612