Heterocyclic α-helix mimetics for targeting protein–protein interactions

详细信息	查看全文 | 推荐本文 |

• 作者：Shannon M. Biros ; Lionel Moisan ; Enrique Mann ; Alex ; re Carella ; Dayong Zhai ; John C. Reed ; Julius Rebek Jr.
• 关键词：α ; -helix mimetic ; Pyridzaine ; Bak/Bcl-X_L ; Protein– ; protein interaction ; Diels– ; Alder
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 August 2007
• 卷：17
• 期：16
• 页码：4641-4645
• 文件大小：878 K

摘要

The design and synthesis of α-helix peptidomimetics using inverse electron demand Diels–Alder reactions is described. The potency of the resulting pyridazine-based library to disrupt the Bak/Bcl-X_L interaction was tested using an in vitro fluorescence polarization assay.