Title of article
Acyclic cyanamide-based inhibitors of cathepsin K
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
3039
To page
3043
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.
Keywords
Cyanamide , Cathepsin K , Cysteine protease inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795722
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