View source for 2uwp

==FACTOR XA INHIBITOR COMPLEX==
<StructureSection load='2uwp' size='340' side='right' caption='[[2uwp]], [[Resolution|resolution]] 1.75&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[2uwp]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2UWP OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2UWP FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=894:2-(5-CHLORO-2-THIENYL)-N-{(3S)-1-[(1S)-1-METHYL-2-MORPHOLIN-4-YL-2-OXOETHYL]-2-OXOPYRROLIDIN-3-YL}ETHANESULFONAMIDE'>894</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1c5m|1c5m]], [[1ezq|1ezq]], [[1f0r|1f0r]], [[1f0s|1f0s]], [[1fax|1fax]], [[1fjs|1fjs]], [[1fxy|1fxy]], [[1g2l|1g2l]], [[1g2m|1g2m]], [[1hcg|1hcg]], [[1ioe|1ioe]], [[1iqe|1iqe]], [[1iqf|1iqf]], [[1iqg|1iqg]], [[1iqh|1iqh]], [[1iqi|1iqi]], [[1iqj|1iqj]], [[1iqk|1iqk]], [[1iql|1iql]], [[1iqm|1iqm]], [[1iqn|1iqn]], [[1ksn|1ksn]], [[1kye|1kye]], [[1lpg|1lpg]], [[1lpk|1lpk]], [[1lpz|1lpz]], [[1lqd|1lqd]], [[1mq5|1mq5]], [[1mq6|1mq6]], [[1msx|1msx]], [[1nfu|1nfu]], [[1nfw|1nfw]], [[1nfx|1nfx]], [[1nfy|1nfy]], [[1nl8|1nl8]], [[1p0s|1p0s]], [[1v3x|1v3x]], [[1wu1|1wu1]], [[1xka|1xka]], [[1xkb|1xkb]], [[1z6e|1z6e]], [[2bmg|2bmg]], [[2boh|2boh]], [[2bok|2bok]], [[2bq6|2bq6]], [[2bq7|2bq7]], [[2bqw|2bqw]], [[2cji|2cji]], [[2fzz|2fzz]], [[2g00|2g00]], [[2gd4|2gd4]], [[2j2u|2j2u]], [[2j34|2j34]], [[2j38|2j38]], [[2j4i|2j4i]], [[2j94|2j94]], [[2j95|2j95]], [[2uwl|2uwl]], [[2uwo|2uwo]]</td></tr>
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Coagulation_factor_Xa Coagulation factor Xa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.6 3.4.21.6] </span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2uwp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2uwp OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2uwp RCSB], [http://www.ebi.ac.uk/pdbsum/2uwp PDBsum]</span></td></tr>
</table>
== Disease ==
[[http://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN]] Defects in F10 are the cause of factor X deficiency (FA10D) [MIM:[http://omim.org/entry/227600 227600]]. A hemorrhagic disease with variable presentation. Affected individuals can manifest prolonged nasal and mucosal hemorrhage, menorrhagia, hematuria, and occasionally hemarthrosis. Some patients do not have clinical bleeding diathesis.<ref>PMID:2790181</ref> <ref>PMID:1973167</ref> <ref>PMID:1985698</ref> <ref>PMID:7669671</ref> <ref>PMID:8529633</ref> <ref>PMID:7860069</ref> <ref>PMID:8845463</ref> <ref>PMID:8910490</ref> <ref>PMID:10468877</ref> <ref>PMID:10746568</ref> <ref>PMID:10739379</ref> <ref>PMID:11248282</ref> <ref>PMID:11728527</ref> <ref>PMID:12945883</ref> <ref>PMID:15650540</ref> <ref>PMID:17393015</ref> <ref>PMID:19135706</ref>  
== Function ==
[[http://www.uniprot.org/uniprot/FA10_HUMAN FA10_HUMAN]] Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting. 
== Evolutionary Conservation ==
[[Image:Consurf_key_small.gif|200px|right]]
Check<jmol>
  <jmolCheckbox>
    <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/uw/2uwp_consurf.spt"</scriptWhenChecked>
    <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
    <text>to colour the structure by Evolutionary Conservation</text>
  </jmolCheckbox>
</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
<div style="clear:both"></div>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhibitor (E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-o xoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide and these observed activity changes have been rationalised using structural studies.

Selective and dual action orally active inhibitors of thrombin and factor Xa.,Young RJ, Brown D, Burns-Kurtis CL, Chan C, Convery MA, Hubbard JA, Kelly HA, Pateman AJ, Patikis A, Senger S, Shah GP, Toomey JR, Watson NS, Zhou P Bioorg Med Chem Lett. 2007 May 15;17(10):2927-30. Epub 2007 Mar 30. PMID:17420122<ref>PMID:17420122</ref>

From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>

==See Also==
*[[Factor Xa|Factor Xa]]
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Coagulation factor Xa]]
[[Category: Homo sapiens]]
[[Category: Brown, D]]
[[Category: Burns-Kurtis, C L]]
[[Category: Chan, C]]
[[Category: Convery, M A]]
[[Category: Hubbard, J A]]
[[Category: Kelly, H A]]
[[Category: Pateman, A J]]
[[Category: Patikis, A]]
[[Category: Senger, S]]
[[Category: Shah, G P]]
[[Category: Thorpe, J H]]
[[Category: Toomey, J R]]
[[Category: Watson, N S]]
[[Category: Young, R J]]
[[Category: Zhou, P]]
[[Category: Blood coagulation]]
[[Category: Cleavage on pair of basic residue]]
[[Category: Complex]]
[[Category: Egf-like domain]]
[[Category: Gamma- carboxyglutamic acid]]
[[Category: Glycoprotein]]
[[Category: Hydrolase]]
[[Category: Hydroxylation]]
[[Category: Protease]]
[[Category: Serine protease]]
[[Category: Target hopping]]
[[Category: Zymogen]]