Simplified analogs of bryostatin with anticancer activity display greater potency for translocation of PKCdelta-GFP

Chemistry & Biology
Jeremy L BaryzaPaul A Wender

Abstract

Structurally simplified analogs of bryostatin 1, a marine natural product in clinical trials for the treatment of cancer, have been shown to be up to 50 times more potent than bryostatin 1 at inducing the translocation of PKCdelta-GFP from the cytosol of rat basophilic leukemia (RBL) cells. The end distribution of the protein is similar for all three compounds, despite a significant difference in translocation kinetics. The potency of the compounds for inducing the translocation response appears to be only qualitatively related to their binding affinity for PKC, highlighting the importance of using binding affinity in conjunction with real-time measurements of protein localization for the pharmacological profiling of biologically active agents.

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Citations

Jul 19, 2011·Journal of the American Chemical Society·Amos B SmithQunli Xu
Mar 19, 2011·Proceedings of the National Academy of Sciences of the United States of America·Paul A WenderVishal A Verma
Nov 1, 2005·Proceedings of the National Academy of Sciences of the United States of America·Daniel L AlkonThomas J Nelson
Jun 7, 2005·Expert Opinion on Therapeutic Targets·Patrick M Martin, Isa M Hussaini
Apr 1, 2010·Chemistry, an Asian Journal·Karl J Hale, Soraya Manaviazar
Dec 24, 2005·Nature Chemical Biology·Alexander V StatsukSergey A Kozmin
Nov 16, 2010·Angewandte Chemie·Alex M Szpilman, Erick M Carreira
Mar 7, 2006·The Journal of Immunology : Official Journal of the American Association of Immunologists·Jelena TomicDavid E Spaner
Apr 1, 2011·Israel Journal of Chemistry·Paul A WenderAdam J Schrier

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