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Pubmed ID :17576063
Publication Date : //

The discovery of carboline analogs as potent MAPKAP-K2 inhibitors.


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.

Authors : Wu Jiang-Ping , Wang Ji , Abeywardane Asitha , Andersen Denise , Emmanuel Michel , Gautschi Elda , Goldberg Daniel R , Kashem Mohammed A , Lukas Susan , Mao Wang , Martin Leslie , Morwick Tina , Moss Neil , Pargellis Christopher , Patel Usha R , Patnaude Lori , Peet Gregory W , Skow Donna , Snow Roger J , Ward Yancey , Werneburg Brian , White Andre ,

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