1yk8
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| , resolution 2.6Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | CTSK, CTSO, CTSO2 (Homo sapiens) | ||||||
| Activity: | Cathepsin K, with EC number 3.4.22.38 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Cathepsin K complexed with a cyanamide-based inhibitor
OverviewOverview
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.
DiseaseDisease
Known disease associated with this structure: Pycnodysostosis OMIM:[601105]
About this StructureAbout this Structure
1YK8 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.
ReferenceReference
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 Jr, Wright LL, Bioorg Med Chem Lett. 2005 Jun 15;15(12):3039-43. PMID:15896958
Page seeded by OCA on Thu Mar 20 15:23:57 2008