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

被引：22

作者：

Baryza, JL

Brenner, SE

Craske, ML

Meyer, T

Wender, PA ^{[1
]}

机构：

[1] Stanford Univ, Sch Med, Dept Chem, Stanford, CA 94305 USA

[2] Stanford Univ, Sch Med, Dept Mol Pharmacol, Stanford, CA 94305 USA

来源：

CHEMISTRY & BIOLOGY | 2004年 / 11卷 / 09期

关键词：

D O I：

10.1016/j.chembiol.2004.06.014

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1261 / 1267

页数：7

共 23 条

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