3hat
From Proteopedia
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[[Image:3hat.jpg|left|200px]] | [[Image:3hat.jpg|left|200px]] | ||
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'''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN''' | '''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN''' | ||
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==About this Structure== | ==About this Structure== | ||
| - | 3HAT is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry | + | 3HAT is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=2hat 2hat]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3HAT OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Mathews, I I.]] | [[Category: Mathews, I I.]] | ||
[[Category: Tulinsky, A.]] | [[Category: Tulinsky, A.]] | ||
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 22:03:32 2008'' | |
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Revision as of 19:03, 4 May 2008
ACTIVE SITE MIMETIC INHIBITION OF THROMBIN
Overview
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.
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 Page seeded by OCA on Sun May 4 22:03:32 2008
