Literature DB >> 15380186

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

Jeremy L Baryza1, Stacey E Brenner, Madeleine L Craske, Tobias Meyer, Paul 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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Year:  2004        PMID： 15380186     DOI： 10.1016/j.chembiol.2004.06.014

Source DB:  PubMed          Journal:  Chem Biol        ISSN： 1074-5521


  7 in total

1.  Translating Nature's Library: The Bryostatins and Function-Oriented Synthesis.

Authors:  Paul A Wender; Brian A Loy; Adam J Schrier
Journal:  Isr J Chem       Date:  2011-03-24       Impact factor: 3.333

2.  Design, synthesis, and evaluation of potent bryostatin analogs that modulate PKC translocation selectivity.

Authors:  Paul A Wender; Jeremy L Baryza; Stacey E Brenner; Brian A DeChristopher; Brian A Loy; Adam J Schrier; Vishal A Verma
Journal:  Proc Natl Acad Sci U S A       Date:  2011-03-17       Impact factor: 11.205

3.  Protein synthesis required for long-term memory is induced by PKC activation on days before associative learning.

Authors:  Daniel L Alkon; Herman Epstein; Alan Kuzirian; M Catherine Bennett; Thomas J Nelson
Journal:  Proc Natl Acad Sci U S A       Date:  2005-10-28       Impact factor: 11.205

4.  Function Oriented Synthesis: Preparation and Initial Biological Evaluation of New A-Ring-Modified Bryologs.

Authors:  Paul A Wender; Jenny Reuber
Journal:  Tetrahedron       Date:  2011-12-23       Impact factor: 2.457

5.  Design, synthesis, and biological evaluation of diminutive forms of (+)-spongistatin 1: lessons learned.

Authors:  Amos B Smith; Christina A Risatti; Onur Atasoylu; Clay S Bennett; Junke Liu; Hongsheng Cheng; Karen TenDyke; Qunli Xu
Journal:  J Am Chem Soc       Date:  2011-08-12       Impact factor: 15.419

6.  Evaluation of Chromane-Based Bryostatin Analogues Prepared via Hydrogen-Mediated C-C Bond Formation: Potency Does Not Confer Bryostatin-like Biology.

Authors:  John M Ketcham; Ivan Volchkov; Te-Yu Chen; Peter M Blumberg; Noemi Kedei; Nancy E Lewin; Michael J Krische
Journal:  J Am Chem Soc       Date:  2016-09-27       Impact factor: 15.419

7.  Synthesis of seco-B-ring bryostatin analogue WN-1 via C-C bond-forming hydrogenation: critical contribution of the B-ring in determining bryostatin-like and phorbol 12-myristate 13-acetate-like properties.

Authors:  Ian P Andrews; John M Ketcham; Peter M Blumberg; Noemi Kedei; Nancy E Lewin; Megan L Peach; Michael J Krische
Journal:  J Am Chem Soc       Date:  2014-09-10       Impact factor: 15.419
  7 in total

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