Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity

…, RG Robinson, SF Barnett, D Defeo-Jones…

文献索引：Zhao, Zhijian; Robinson, Ronald G.; Barnett, Stanley F.; Defeo-Jones, Deborah; Jones, Raymond E.; Hartman, George D.; Huber, Hans E.; Duggan, Mark E.; Lindsley, Craig W. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 49 - 53

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被引用次数: 49

摘要

Recent reports from our laboratories disclosed a series of novel, allosteric Akt kinase inhibitors that displayed high levels of Akt isozyme selectivity and PH-domain dependent inhibition. 4 Significantly, these allosteric inhibitors were postulated to lock Akt into a closed conformation which not only inhibited the activity of the kinase, but also prevented the activation (phosphorylation) of Akt. 4 and 5 This was observed both in vitro and in vivo with the dual ...