Acyclic cyanamide-based inhibitors of cathepsin K.

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Barrett DG, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Willard DH Jr, Wright LL

Acyclic cyanamide-based inhibitors of cathepsin K.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43.

PubMed ID
15896958 [ View in PubMed
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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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
CyanamideCathepsin KProteinHumans
Unknown
Not AvailableDetails