Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics |
| |
Authors: | Kayser Katherine J Glenn Matthew P Sebti Said M Cheng Jin Q Hamilton Andrew D |
| |
Institution: | Department of Chemistry, Yale University, PO Box 208107, New Haven, CT 06520, USA. |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|