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. 2005 Feb 1;15(3):761-4.
doi: 10.1016/j.bmcl.2004.11.011.

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

Craig W Lindsley  1 , Zhijian Zhao, William H Leister, Ronald G Robinson, Stanley F Barnett, Deborah Defeo-Jones, Raymond E Jones, George D Hartman, Joel R Huff, Hans E Huber, Mark E Duggan
Affiliations

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

Craig W Lindsley et al. Bioorg Med Chem Lett. .

Abstract

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.

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