Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors

Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors
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DOI:
10.1016/j.bmcl.2004.11.011
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发表时间:
2005-02-01
影响因子:
2.7
通讯作者:
Duggan, ME
Duggan, ME
中科院分区:
医学4区
文献类型:
--
作者:
Lindsley, CW;Zhao, ZJ;Duggan, ME

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This letter describes the development of two series of potent and selective allosteric Akt kinase inhibitors that display an unprecedented level of selectivity for either Akt1, Akt2 or both Akt1/Akt2. An iterative analog library synthesis approach quickly provided a highly selective Akt1/Akt2 inhibitor that induces apoptosis in tumor cells and inhibits Akt phosphorylation in vivo. (C) 2004 Elsevier Ltd. All rights reserved.