Author/Authors :
David N. Deaton، نويسنده , , Anne M. Hassell، نويسنده , , Robert B. McFadyen، نويسنده , , Aaron B. Miller، نويسنده , , Larry R. Miller، نويسنده , , Lisa M. Shewchuk، نويسنده , , Francis X. Tavares، نويسنده , , Derril H. Willard Jr.، نويسنده , , Lois L. Wright، نويسنده ,
Abstract :
Starting from a PDE IV inhibitor hit derived from high throughput screening of the compound collection, a key pyrrolidine cyanamide pharmacophore was identified. Modifications of the pyrrolidine ring produced enhancements in cathepsin K inhibition. An X-ray co-crystal structure of a cyanamide with cathepsin K confirmed the mode of inhibition.
Keywords :
Cathepsin K , Cyanamide , Cysteine protease inhibitor , Warhead
