Modifications of the GSK3β substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics
- 作者：Katherine J. Kayser ; Matthew P. Glenn ; Said M. Sebti ; Jin Q. Cheng ; Andrew D. Hamilton
- 关键词：Protein kinase B ; Akt ; Cancer ; Peptidomimetics ; Substrate-mimetic
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：1 April 2007
- 卷：17
- 期：7
- 页码：2068-2073
- 文件大小：1058 K
摘要
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 a potent, small molecule substrate-mimetic inhibitor of Akt.