1rwk: Difference between revisions

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[[Image:1rwk.gif|left|200px]]
{{Seed}}
[[Image:1rwk.png|left|200px]]


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{{STRUCTURE_1rwk|  PDB=1rwk  |  SCENE=  }}  
{{STRUCTURE_1rwk|  PDB=1rwk  |  SCENE=  }}  


'''Crystal structure of human caspase-1 in complex with 3-(2-mercapto-acetylamino)-4-oxo-pentanoic acid'''
===Crystal structure of human caspase-1 in complex with 3-(2-mercapto-acetylamino)-4-oxo-pentanoic acid===




==Overview==
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Caspase-1 is a key endopeptidase responsible for the post-translational processing of the IL-1beta and IL-18 cytokines and small-molecule inhibitors that modulate the activity of this enzyme are predicted to be important therapeutic treatments for many inflammatory diseases. A fragment-assembly approach, accompanied by structural analysis, was employed to generate caspase-1 inhibitors. With the aid of Tethering with extenders (small molecules that bind to the active-site cysteine and contain a free thiol), two novel fragments that bound to the active site and made a disulfide bond with the extender were identified by mass spectrometry. Direct linking of each fragment to the extender generated submicromolar reversible inhibitors that significantly reduced secretion of IL-1beta but not IL-6 from human peripheral blood mononuclear cells. Thus, Tethering with extenders facilitated rapid identification and synthesis of caspase-1 inhibitors with cell-based activity and subsequent structural analyses provided insights into the enzyme's ability to accommodate different inhibitor-binding modes in the active site.
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{{ABSTRACT_PUBMED_16511067}}


==About this Structure==
==About this Structure==
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[[Category: Romanowski, M J.]]
[[Category: Romanowski, M J.]]
[[Category: Protein-small molecule inhibitor complex]]
[[Category: Protein-small molecule inhibitor complex]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 07:59:28 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:18:50 2008''

Revision as of 04:18, 29 July 2008

File:1rwk.png

Template:STRUCTURE 1rwk

Crystal structure of human caspase-1 in complex with 3-(2-mercapto-acetylamino)-4-oxo-pentanoic acid

Template:ABSTRACT PUBMED 16511067

About this Structure

1RWK is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Structural analysis of caspase-1 inhibitors derived from Tethering., O'Brien T, Fahr BT, Sopko MM, Lam JW, Waal ND, Raimundo BC, Purkey HE, Pham P, Romanowski MJ, Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005 May 1;61(Pt, 5):451-8. Epub 2005 Apr 9. PMID:16511067

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