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[[Image:1kui.jpg|left|200px]]
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[[Image:1kui.png|left|200px]]


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{{STRUCTURE_1kui|  PDB=1kui  |  SCENE=  }}  
{{STRUCTURE_1kui|  PDB=1kui  |  SCENE=  }}  


'''Crystal Structure of a Taiwan Habu Venom Metalloproteinase complexed with pEQW.'''
===Crystal Structure of a Taiwan Habu Venom Metalloproteinase complexed with pEQW.===




==Overview==
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Venoms from crotalid and viperid snakes contain several peptide inhibitors which regulate the proteolytic activities of their snake-venom metalloproteinases (SVMPs) in a reversible manner under physiological conditions. In this report, we describe the high-resolution crystal structures of a SVMP, TM-3, from Taiwan habu (Trimeresurus mucrosquamatus) cocrystallized with the endogenous inhibitors pyroGlu-Asn-Trp (pENW), pyroGlu-Gln-Trp (pEQW) or pyroGlu-Lys-Trp (pEKW). The binding of inhibitors causes some of the residues around the inhibitor-binding environment of TM-3 to slightly move away from the active-site center, and displaces two metal-coordinated water molecules by the C-terminal carboxylic group of the inhibitors. This binding adopts a retro-manner principally stabilized by four possible hydrogen bonds. The Trp indole ring of the inhibitors is stacked against the imidazole of His143 in the S-1 site of the proteinase. Results from the study of synthetic inhibitor analogues showed the primary specificity of Trp residue of the inhibitors at the P-1 site, corroborating the stacking effect observed in our structures. Furthermore, we have made a detailed comparison of our structures with the binding modes of other inhibitors including batimastat, a hydroxamate inhibitor, and a barbiturate derivative. It suggests a close correlation between the inhibitory activity of an inhibitor and its ability to fill the S-1 pocket of the proteinase. Our work may provide insights into the rational design of small molecules that bind to this class of zinc-metalloproteinases.
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{{ABSTRACT_PUBMED_12071970}}


==About this Structure==
==About this Structure==
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[[Category: Alpha/beta protein]]
[[Category: Alpha/beta protein]]
[[Category: Retro-binding manner]]
[[Category: Retro-binding manner]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 23:10:59 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 2 11:01:37 2008''

Revision as of 08:01, 2 July 2008

File:1kui.png

Template:STRUCTURE 1kui

Crystal Structure of a Taiwan Habu Venom Metalloproteinase complexed with pEQW.

Template:ABSTRACT PUBMED 12071970

About this Structure

1KUI is a Single protein structure of sequence from Protobothrops mucrosquamatus. Full crystallographic information is available from OCA.

Reference

Determinants of the inhibition of a Taiwan habu venom metalloproteinase by its endogenous inhibitors revealed by X-ray crystallography and synthetic inhibitor analogues., Huang KF, Chiou SH, Ko TP, Wang AH, Eur J Biochem. 2002 Jun;269(12):3047-56. PMID:12071970

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