Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

…, MP Glenn, SM Sebti, JQ Cheng, AD Hamilton

Index: Kayser, Katherine J.; Glenn, Matthew P.; Sebti, Said M.; Cheng, Jin Q.; Hamilton, Andrew D. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 7 p. 2068 - 2073

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Citation Number: 25

Abstract

Amplification, overexpression, and elevated activation of Akt have been detected in many human malignancies making it an important target for cancer therapy. The Akt substrate- binding site offers a large number of potential interactions to an appropriately designed small molecule and can form the basis for the development of selective inhibitors. Here, we report the progression of GSK3β substrate-mimetic inhibitors towards the development of ...