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ID: ALA1141888

Journal: Bioorg Med Chem Lett

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

Authors: Lindsley CW, Zhao Z, Leister WH, Robinson RG, Barnett SF, Defeo-Jones D, Jones RE, Hartman GD, Huff JR, Huber HE, Duggan ME.

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.

CiteXplore: 15664853

DOI: 10.1016/j.bmcl.2004.11.011