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2auz

From Proteopedia

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[[Image:2auz.gif|left|200px]]
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{{STRUCTURE_2auz| PDB=2auz | SCENE= }}
{{STRUCTURE_2auz| PDB=2auz | SCENE= }}
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'''Cathepsin K complexed with a semicarbazone inhibitor'''
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===Cathepsin K complexed with a semicarbazone inhibitor===
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==Overview==
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Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
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(as it appears on PubMed at http://www.pubmed.gov), where 16290936 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16290936}}
==About this Structure==
==About this Structure==
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[[Category: Catk]]
[[Category: Catk]]
[[Category: Cysteine protease]]
[[Category: Cysteine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:30:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 12:12:09 2008''

Revision as of 09:12, 29 July 2008

Image:2auz.png

Template:STRUCTURE 2auz

Cathepsin K complexed with a semicarbazone inhibitor

Template:ABSTRACT PUBMED 16290936

About this Structure

2AUZ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?, Adkison KK, Barrett DG, Deaton DN, Gampe RT, Hassell AM, Long ST, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Wells-Knecht KJ, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2006 Feb 15;16(4):978-83. Epub 2005 Nov 15. PMID:16290936

Page seeded by OCA on Tue Jul 29 12:12:09 2008

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