The discovery of carboline analogs as potent MAPKAP-K2 inhibitors
详细信息 查看全文
- 作者：Jiang-Ping Wu ; Ji Wang ; Asitha Abeywardane ; Denise Andersen ; Michel Emmanuel ; Elda Gautschi ; Daniel R. Goldberg ; Mohammed A. Kashem ; Susan Lukas ; Wang Mao ; Leslie Martin ; Tina Morwick ; Neil Moss ; Chri
- 关键词：MAPKAP-K2 ; MK2 ; MK2a ; Carboline
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 August 2007
- 年：2007
- 卷：17
- 期：16
- 页码：4664-4669
- 全文大小：269 K
文摘
The discovery of a series of potent, carboline-based MK2 inhibitors is described. These compounds inhibit MK2 with IC50s as low as 10 nM, as measured in a DELFIA assay. An X-ray crystal structure reveals that they bind in a region near the p-loop and the hinge region of MK2a.