2. Academic Validation
  3. Design of small molecule ketoamide-based inhibitors of cathepsin K

Design of small molecule ketoamide-based inhibitors of cathepsin K

  • Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22. doi: 10.1016/j.bmcl.2003.11.029.
John G Catalano 1,  David N Deaton,  Stacey T Long,  Robert B McFadyen,  Larry R Miller,  J Alan Payne,  Kevin J Wells-Knecht,  Lois L Wright
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA.
PMID: 14741275 DOI: 10.1016/j.bmcl.2003.11.029
Abstract

A novel series of ketoamide-based inhibitors of Cathepsin K has been identified. Modifications to P(2) and P(3) elements were crucial to enhancing inhibitory activity. Although not optimized, a selected inhibitor was effective in attenuating type I collagen hydrolysis in a surrogate assay of bone resorption.

Figures
Products