2hbr

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[[Image:2hbr.gif|left|200px]]
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{{STRUCTURE_2hbr| PDB=2hbr | SCENE= }}
{{STRUCTURE_2hbr| PDB=2hbr | SCENE= }}
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'''Crystal structure of human caspase-1 (Arg286->Ala) in complex with 3-[2-(2-benzyloxycarbonylamino-3-methyl-butyrylamino)-propionylamino]-4-oxo-pentanoic acid (z-VAD-FMK)'''
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===Crystal structure of human caspase-1 (Arg286->Ala) in complex with 3-[2-(2-benzyloxycarbonylamino-3-methyl-butyrylamino)-propionylamino]-4-oxo-pentanoic acid (z-VAD-FMK)===
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==Overview==
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We present a common allosteric mechanism for control of inflammatory and apoptotic caspases. Highly specific thiol-containing inhibitors of the human inflammatory caspase-1 were identified by using disulfide trapping, a method for site-directed small-molecule discovery. These compounds became trapped by forming a disulfide bond with a cysteine residue in the cavity at the dimer interface approximately 15 A away from the active site. Mutational and structural analysis uncovered a linear circuit of functional residues that runs from one active site through the allosteric cavity and into the second active site. Kinetic analysis revealed robust positive cooperativity not seen in other endopeptidases. Recently, disulfide trapping identified a similar small-molecule site and allosteric transition in the apoptotic caspase-7 that shares only a 23% sequence identity with caspase-1. Together, these studies show a general small-molecule-binding site for functionally reversing the zymogen activation of caspases and suggest a common regulatory site for the allosteric control of inflammation and apoptosis.
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(as it appears on PubMed at http://www.pubmed.gov), where 16682620 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16682620}}
==About this Structure==
==About this Structure==
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[[Category: Allosteric circuit]]
[[Category: Allosteric circuit]]
[[Category: Caspase]]
[[Category: Caspase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 06:05:51 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:23:04 2008''

Revision as of 21:23, 27 July 2008

Image:2hbr.png

Template:STRUCTURE 2hbr

Crystal structure of human caspase-1 (Arg286->Ala) in complex with 3-[2-(2-benzyloxycarbonylamino-3-methyl-butyrylamino)-propionylamino]-4-oxo-pentanoic acid (z-VAD-FMK)

Template:ABSTRACT PUBMED 16682620

About this Structure

2HBR is a Protein complex structure of sequences from Homo sapiens. This structure supersedes the now removed PDB entry 2fqs. Full crystallographic information is available from OCA.

Reference

A common allosteric site and mechanism in caspases., Scheer JM, Romanowski MJ, Wells JA, Proc Natl Acad Sci U S A. 2006 May 16;103(20):7595-600. Epub 2006 May 8. PMID:16682620

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