1tu6: Difference between revisions

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[[Image:1tu6.gif|left|200px]]
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{{STRUCTURE_1tu6|  PDB=1tu6  |  SCENE=  }}  
{{STRUCTURE_1tu6|  PDB=1tu6  |  SCENE=  }}  


'''Cathepsin K complexed with a ketoamide inhibitor'''
===Cathepsin K complexed with a ketoamide inhibitor===




==Overview==
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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.
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{{ABSTRACT_PUBMED_15341947}}


==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 Sun Jul 27 19:30:42 2008''

Revision as of 19:30, 27 July 2008

File:1tu6.png

Template:STRUCTURE 1tu6

Cathepsin K complexed with a ketoamide inhibitorCathepsin K complexed with a ketoamide inhibitor

Template:ABSTRACT PUBMED 15341947

About this StructureAbout this Structure

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

ReferenceReference

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

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