2cji

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[[Image:2cji.gif|left|200px]]
[[Image:2cji.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2cji |SIZE=350|CAPTION= <scene name='initialview01'>2cji</scene>, resolution 2.10&Aring;
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The line below this paragraph, containing "STRUCTURE_2cji", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Gsk+Binding+Site+For+Chain+A'>AC1</scene>
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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=GSK:6-CHLORO-N-{(3S)-1-[(1S)-1-METHYL-2-(4-MORPHOLINYL)-2-OXO+ETHYL]-2-OXO-3-PYRROLIDINYL}-2-NAPHTHALENESULFONAMIDE'>GSK</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_2cji| PDB=2cji | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2cji FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2cji OCA], [http://www.ebi.ac.uk/pdbsum/2cji PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2cji RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX'''
'''CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX'''
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[[Category: Whitworth, C.]]
[[Category: Whitworth, C.]]
[[Category: Young, R J.]]
[[Category: Young, R J.]]
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[[Category: blood coagulation]]
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[[Category: Blood coagulation]]
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[[Category: calcium]]
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[[Category: Calcium]]
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[[Category: egf-like domain]]
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[[Category: Egf-like domain]]
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[[Category: gamma-carboxyglutamic acid]]
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[[Category: Gamma-carboxyglutamic acid]]
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[[Category: glycoprotein]]
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[[Category: Glycoprotein]]
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[[Category: hydrolase]]
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[[Category: Hydrolase]]
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[[Category: hydroxylation]]
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[[Category: Hydroxylation]]
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[[Category: polymorphism]]
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[[Category: Polymorphism]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: serine protease]]
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[[Category: Serine protease]]
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[[Category: zymogen]]
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[[Category: Zymogen]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 22:17:24 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:22:21 2008''
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Revision as of 19:17, 3 May 2008

Image:2cji.gif

Template:STRUCTURE 2cji

CRYSTAL STRUCTURE OF A HUMAN FACTOR XA INHIBITOR COMPLEX


Overview

A series of novel, non-basic 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group, was designed and synthesised. Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl derivative 24 was shown to be a potent, selective fXa inhibitor with good anticoagulant activity. Moreover, 24 possessed highly encouraging rat and dog pharmacokinetic profiles with excellent oral bioavailabilities in both species.

About this Structure

2CJI is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Design and synthesis of orally active pyrrolidin-2-one-based factor Xa inhibitors., Watson NS, Brown D, Campbell M, Chan C, Chaudry L, Convery MA, Fenwick R, Hamblin JN, Haslam C, Kelly HA, King NP, Kurtis CL, Leach AR, Manchee GR, Mason AM, Mitchell C, Patel C, Patel VK, Senger S, Shah GP, Weston HE, Whitworth C, Young RJ, Bioorg Med Chem Lett. 2006 Jul 15;16(14):3784-8. Epub 2006 May 11. PMID:16697194 Page seeded by OCA on Sat May 3 22:17:24 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

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