1ksn

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[[Image:1ksn.gif|left|200px]]
[[Image:1ksn.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1ksn |SIZE=350|CAPTION= <scene name='initialview01'>1ksn</scene>, resolution 2.1&Aring;
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The line below this paragraph, containing "STRUCTURE_1ksn", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=FXV:METHYL-3-(4&#39;-N-OXOPYRIDYLPHENOYL)-3-METHYL-2-(M-AMIDINOBENZYL)-PROPIONATE'>FXV</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <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>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1ksn| PDB=1ksn | SCENE= }}
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|RELATEDENTRY=[[1ezq|1EZQ]], [[1f0r|1F0R]], [[1f0s|1F0S]], [[1f0t|1F0T]], [[1f0u|1F0U]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ksn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ksn OCA], [http://www.ebi.ac.uk/pdbsum/1ksn PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ksn RCSB]</span>
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}}
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'''Crystal Structure of Human Coagulation Factor XA Complexed with FXV673'''
'''Crystal Structure of Human Coagulation Factor XA Complexed with FXV673'''
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[[Category: Guilloteau, J P.]]
[[Category: Guilloteau, J P.]]
[[Category: Maignan, S.]]
[[Category: Maignan, S.]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 23:07:23 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:53:00 2008''
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Revision as of 20:07, 2 May 2008

Image:1ksn.gif

Template:STRUCTURE 1ksn

Crystal Structure of Human Coagulation Factor XA Complexed with FXV673


Overview

Further optimization of the beta-aminoester class of factor Xa (fXa) inhibitors is described culminating in the identification of 9c (FXV673), a potent and selective factor Xa inhibitor with excellent in vivo anticoagulant activity. An X-ray structure of FXV673 bound to human fXa is also presented. Based on its selectivity, potent in vivo activity and favorable pre-clinical safety profile, FXV673 was selected for further development and is currently undergoing clinical trials.

About this Structure

1KSN is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity., Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW, Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4. PMID:12039587 Page seeded by OCA on Fri May 2 23:07:23 2008

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