1ksn
From Proteopedia
(New page: 200px<br /> <applet load="1ksn" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ksn, resolution 2.1Å" /> '''Crystal Structure of...) |
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| - | [[Image:1ksn.gif|left|200px]]<br /> | + | [[Image:1ksn.gif|left|200px]]<br /><applet load="1ksn" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="1ksn" size=" | + | |
caption="1ksn, resolution 2.1Å" /> | caption="1ksn, resolution 2.1Å" /> | ||
'''Crystal Structure of Human Coagulation Factor XA Complexed with FXV673'''<br /> | '''Crystal Structure of Human Coagulation Factor XA Complexed with FXV673'''<br /> | ||
==Overview== | ==Overview== | ||
| - | Further optimization of the beta-aminoester class of factor Xa (fXa) | + | 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. |
==Disease== | ==Disease== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 1KSN is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with CA and FXV as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http:// | + | 1KSN is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=CA:'>CA</scene> and <scene name='pdbligand=FXV:'>FXV</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1KSN OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| - | [[Category: Guilloteau, J | + | [[Category: Guilloteau, J P.]] |
[[Category: Maignan, S.]] | [[Category: Maignan, S.]] | ||
[[Category: CA]] | [[Category: CA]] | ||
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[[Category: hydrolase]] | [[Category: hydrolase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:39:03 2008'' |
Revision as of 11:39, 21 February 2008
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Crystal Structure of Human Coagulation Factor XA Complexed with FXV673
Contents |
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.
Disease
Known disease associated with this structure: Factor X deficiency OMIM:[227600]
About this Structure
1KSN is a Protein complex structure of sequences from Homo sapiens with and as ligands. Active as Coagulation factor Xa, with EC number 3.4.21.6 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 Thu Feb 21 13:39:03 2008
