3hat

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[[Image:3hat.jpg|left|200px]]
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{{STRUCTURE_3hat| PDB=3hat | SCENE= }}
{{STRUCTURE_3hat| PDB=3hat | SCENE= }}
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'''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN'''
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===ACTIVE SITE MIMETIC INHIBITION OF THROMBIN===
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==Overview==
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The structures of two mimetic inhibitor complexes of human alpha-thrombin have been determined by X-ray crystallography. One mimics a beta-turn with a bicyclic ring system; the other mimics two different active-site binding modes. The beta-turn mimetic is used to approximate a turn found in the conformation of fibrinopeptide A, which is catalytically released by thrombin in the activation of fibrinogen to fibrin. The binding of the second mimetic is a hybrid between normal substrate and the abnormal binding of the potent natural leech inhibitor hirudin. The binding of the beta-turn mimetic is tenuous, because it is like a substrate, while that of the substrate-hirudin hybrid is that of a tenacious inhibitor (which it is). Structurally retrospect modifications for rational design and improvement of both mimetic inhibitors are proposed.
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The line below this paragraph, {{ABSTRACT_PUBMED_15299843}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15299843 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15299843}}
==About this Structure==
==About this Structure==
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[[Category: Mathews, I I.]]
[[Category: Mathews, I I.]]
[[Category: Tulinsky, A.]]
[[Category: Tulinsky, A.]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 22:03:32 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jul 3 12:48:22 2008''

Revision as of 09:48, 3 July 2008

Image:3hat.png

Template:STRUCTURE 3hat

ACTIVE SITE MIMETIC INHIBITION OF THROMBIN

Template:ABSTRACT PUBMED 15299843

About this Structure

3HAT is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 2hat. Full crystallographic information is available from OCA.

Reference

Active-site mimetic inhibition of thrombin., Mathews II, Tulinsky A, Acta Crystallogr D Biol Crystallogr. 1995 Jul 1;51(Pt 4):550-9. PMID:15299843

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