Author/Authors :
David G. Barrett، نويسنده , , David N. Deaton، نويسنده , , Anne M. Hassell، نويسنده , , Robert B. McFadyen، نويسنده , , Aaron B. Miller، نويسنده , , Larry R. Miller، نويسنده , , J. Alan Payne، نويسنده , , Lisa M. Shewchuk، نويسنده , , Derril H. Willard Jr.، نويسنده , , Lois L. Wright، نويسنده ,
Abstract :
Conversion of the proline-derived cyanamide lead to an acyclic cyanamide capable of forming an additional hydrogen bond with cathepsin K resulted in a large increase in inhibitory activity. An X-ray structure of a co-crystal of a cyanamide with cathepsin K confirmed the enzyme interaction. Furthermore, a representative acyclic cyanamide inhibitor 6r was able to attenuate bone resorption in the rat calvarial model.
