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  3. Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics

  • Bioorg Med Chem Lett. 2007 Apr 1;17(7):2068-73. doi: 10.1016/j.bmcl.2007.01.004.
Katherine J Kayser 1,  Matthew P Glenn,  Said M Sebti,  Jin Q Cheng,  Andrew D Hamilton
Affiliations

Affiliation

  • 1 Department of Chemistry, Yale University, PO Box 208107, New Haven, CT 06520, USA.
PMID: 17276059 DOI: 10.1016/j.bmcl.2007.01.004
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 GSK3beta substrate-mimetic inhibitors towards the development of a potent, small molecule substrate-mimetic inhibitor of Akt.

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