3hat
From Proteopedia
(New page: 200px<br /> <applet load="3hat" size="450" color="white" frame="true" align="right" spinBox="true" caption="3hat, resolution 2.5Å" /> '''ACTIVE SITE MIMETIC ...) |
|||
| Line 1: | Line 1: | ||
| - | [[Image:3hat. | + | [[Image:3hat.jpg|left|200px]]<br /><applet load="3hat" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="3hat" size=" | + | |
caption="3hat, resolution 2.5Å" /> | caption="3hat, resolution 2.5Å" /> | ||
'''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN'''<br /> | '''ACTIVE SITE MIMETIC INHIBITION OF THROMBIN'''<br /> | ||
| Line 11: | Line 10: | ||
==About this Structure== | ==About this Structure== | ||
| - | 3HAT 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 as [http://en.wikipedia.org/wiki/ligand ligand]. This structure superseeds the now removed PDB entry 2HAT. 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:// | + | 3HAT 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> as [http://en.wikipedia.org/wiki/ligand ligand]. This structure superseeds the now removed PDB entry 2HAT. 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=3HAT OCA]. |
==Reference== | ==Reference== | ||
| Line 23: | Line 22: | ||
[[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 17:43:19 2008'' |
Revision as of 15:43, 15 February 2008
|
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
3HAT is a Single protein structure of sequence from Homo sapiens with as ligand. This structure superseeds the now removed PDB entry 2HAT. 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
Page seeded by OCA on Fri Feb 15 17:43:19 2008
