2aux

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[[Image:2aux.gif|left|200px]]
[[Image:2aux.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2aux |SIZE=350|CAPTION= <scene name='initialview01'>2aux</scene>, resolution 2.4&Aring;
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The line below this paragraph, containing "STRUCTURE_2aux", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CT1:(1R)-2-METHYL-1-(PHENYLMETHYL)PROPYL[(1S)-1-FORMYLPENTYL]CARBAMATE'>CT1</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Cathepsin_K Cathepsin K], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.22.38 3.4.22.38] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= CTSK, CTSO, CTSO2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2aux| PDB=2aux | SCENE= }}
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|RELATEDENTRY=[[2auz|2AUZ]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2aux FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2aux OCA], [http://www.ebi.ac.uk/pdbsum/2aux PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2aux RCSB]</span>
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}}
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'''Cathepsin K complexed with a semicarbazone inhibitor'''
'''Cathepsin K complexed with a semicarbazone inhibitor'''
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[[Category: Miller, L R.]]
[[Category: Miller, L R.]]
[[Category: Shewchuk, L M.]]
[[Category: Shewchuk, L M.]]
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[[Category: catk]]
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[[Category: Catk]]
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[[Category: cysteine protease]]
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[[Category: Cysteine protease]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:30:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:57:35 2008''
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Revision as of 16:30, 3 May 2008

Image:2aux.gif

Template:STRUCTURE 2aux

Cathepsin K complexed with a semicarbazone inhibitor


Overview

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.

About this Structure

2AUX 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 Sat May 3 19:30:22 2008

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OCA

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