1tu6

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[[Image:1tu6.gif|left|200px]]
[[Image:1tu6.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1tu6 |SIZE=350|CAPTION= <scene name='initialview01'>1tu6</scene>, resolution 1.75&Aring;
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The line below this paragraph, containing "STRUCTURE_1tu6", 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=FSP:[1-(4-FLUOROBENZYL)CYCLOBUTYL]METHYL+(1S)-1-[OXO(1H-PYRAZOL-5-YLAMINO)ACETYL]PENTYLCARBAMATE'>FSP</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</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_1tu6| PDB=1tu6 | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1tu6 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1tu6 OCA], [http://www.ebi.ac.uk/pdbsum/1tu6 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1tu6 RCSB]</span>
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}}
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'''Cathepsin K complexed with a ketoamide inhibitor'''
'''Cathepsin K complexed with a ketoamide inhibitor'''
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[[Category: Wells-Knecht, K J.]]
[[Category: Wells-Knecht, K J.]]
[[Category: Wright, L L.]]
[[Category: Wright, L L.]]
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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 10:22:08 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 00:01:06 2008''
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Revision as of 07:22, 3 May 2008

Image:1tu6.gif

Template:STRUCTURE 1tu6

Cathepsin K complexed with a ketoamide inhibitor


Overview

A series of ketoamides were synthesized and evaluated for inhibitory activity against cathepsin K. Exploration of the interactions between achiral P(2) substituents and the cysteine protease based on molecular modelling suggestions resulted in potent cathepsin K inhibitors that demonstrated high selectivity versus cathepsins B, H, and L. Subsequent modifications of the P(3), P(1), and P(1') moieties afforded orally bioavailable inhibitors.

About this Structure

1TU6 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potent and selective P2-P3 ketoamide inhibitors of cathepsin K with good pharmacokinetic properties via favorable P1', P1, and/or P3 substitutions., Barrett DG, Catalano JG, Deaton DN, Hassell AM, Long ST, Miller AB, Miller LR, Shewchuk LM, Wells-Knecht KJ, Willard DH Jr, Wright LL, Bioorg Med Chem Lett. 2004 Oct 4;14(19):4897-902. PMID:15341947 Page seeded by OCA on Sat May 3 10:22:08 2008

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OCA

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