1fpc
From Proteopedia
(New page: 200px<br /> <applet load="1fpc" size="450" color="white" frame="true" align="right" spinBox="true" caption="1fpc, resolution 2.3Å" /> '''ACTIVE SITE MIMETIC ...) |
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| - | [[Image:1fpc. | + | [[Image:1fpc.jpg|left|200px]]<br /><applet load="1fpc" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1fpc" size=" | + | |
caption="1fpc, resolution 2.3Å" /> | caption="1fpc, resolution 2.3Å" /> | ||
'''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN'''<br /> | '''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1FPC is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO3 and ANS as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] Full crystallographic information is available from [http:// | + | 1FPC is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO3:'>SO3</scene> and <scene name='pdbligand=ANS:'>ANS</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1FPC OCA]. |
==Reference== | ==Reference== | ||
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[[Category: complex (serine protease/inhibitor)]] | [[Category: complex (serine protease/inhibitor)]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri Feb 15 15:48:36 2008'' |
Revision as of 13:48, 15 February 2008
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ACTIVE SITE MIMETIC INHIBITION OF THROMBIN
Contents |
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.
Disease
Known diseases associated with this structure: Dysprothrombinemia OMIM:[176930], Hyperprothrombinemia OMIM:[176930], Hypoprothrombinemia OMIM:[176930]
About this Structure
1FPC is a Single protein structure of sequence from Homo sapiens with and as ligands. Active as Thrombin, with EC number 3.4.21.5 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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