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Acyclic cyanamide-based inhibitors of cathepsin K.

Barrett DG, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Willard DH, Wright LL
Bioorg Med Chem Lett 15 3039-43 (2005)
Cited: 12 times
EuropePMC logo PMID: 15896958

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.

Reviews citing this publication (2)

  1. Biochemical properties and regulation of cathepsin K activity. Lecaille F, Brömme D, Lalmanach G. Biochimie 90 208-226 (2008)
  2. Cryo-EM: A new dawn in thyroid biology. Coscia F, Taler-Verčič A. Mol Cell Endocrinol 531 111309 (2021)

Articles citing this publication (10)



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