1ksn: Difference between revisions
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|PDB= 1ksn |SIZE=350|CAPTION= <scene name='initialview01'>1ksn</scene>, resolution 2.1Å | |PDB= 1ksn |SIZE=350|CAPTION= <scene name='initialview01'>1ksn</scene>, resolution 2.1Å | ||
|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene> | |LIGAND= <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=FXV:METHYL-3-(4'-N-OXOPYRIDYLPHENOYL)-3-METHYL-2-(M-AMIDINOBENZYL)-PROPIONATE'>FXV</scene> | ||
|ACTIVITY= [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] | |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> | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY=[[1ezq|1EZQ]], [[1f0r|1F0R]], [[1f0s|1F0S]], [[1f0t|1F0T]], [[1f0u|1F0U]] | |||
|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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==Overview== | ==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. | 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== | ==About this Structure== | ||
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[[Category: Guilloteau, J P.]] | [[Category: Guilloteau, J P.]] | ||
[[Category: Maignan, S.]] | [[Category: Maignan, S.]] | ||
[[Category: hydrolase]] | [[Category: hydrolase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 21:53:00 2008'' | ||