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2op3

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{{STRUCTURE_2op3| PDB=2op3 | SCENE= }}
{{STRUCTURE_2op3| PDB=2op3 | SCENE= }}
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'''The structure of cathepsin S with a novel 2-arylphenoxyacetaldehyde inhibitor derived by the Substrate Activity Screening (SAS) method'''
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===The structure of cathepsin S with a novel 2-arylphenoxyacetaldehyde inhibitor derived by the Substrate Activity Screening (SAS) method===
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==Overview==
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The substrate activity screening (SAS) method, a substrate-based fragment identification and optimization method for the development of enzyme inhibitors, was previously applied to cathepsin S to obtain a novel (2-arylphenoxy)acetaldehyde inhibitor, 2, with a 0.49 microM Ki value (Wood, W. J. L.; Patterson, A. W.; Tsuruoka, H.; Jain, R. K.; Ellman, J. A. J. Am. Chem. Soc. 2005, 127, 15521-15527). In this paper we disclose the X-ray structure of a complex between cathepsin S and inhibitor 2 which reveals an unprecedented binding mode. On the basis of this structure, additional 2-biaryloxy substrates with greatly increased cleavage efficiency were designed. Conversion of the optimized substrates to the corresponding aldehyde inhibitors yielded a low molecular weight (304 Daltons) and potent (9.6 nM) cathepsin S inhibitor that showed from 100- to &gt;1000-fold selectivity relative to cathepsins B, L, and K.
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{{ABSTRACT_PUBMED_17469812}}
==About this Structure==
==About this Structure==
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[[Category: Nonpeptidic]]
[[Category: Nonpeptidic]]
[[Category: Substrate activity screening]]
[[Category: Substrate activity screening]]
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Revision as of 00:03, 29 July 2008

Image:2op3.png

Template:STRUCTURE 2op3

The structure of cathepsin S with a novel 2-arylphenoxyacetaldehyde inhibitor derived by the Substrate Activity Screening (SAS) method

Template:ABSTRACT PUBMED 17469812

About this Structure

2OP3 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Characterization and optimization of selective, nonpeptidic inhibitors of cathepsin S with an unprecedented binding mode., Inagaki H, Tsuruoka H, Hornsby M, Lesley SA, Spraggon G, Ellman JA, J Med Chem. 2007 May 31;50(11):2693-9. Epub 2007 May 1. PMID:17469812

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