2c4f
From Proteopedia
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[[Image:2c4f.jpg|left|200px]] | [[Image:2c4f.jpg|left|200px]] | ||
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| - | | | + | {{STRUCTURE_2c4f| PDB=2c4f | SCENE= }} |
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'''CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121''' | '''CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121''' | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2C4F is a [[Protein complex]] structure | + | 2C4F is a [[Protein complex]] structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2C4F OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Kohrt, J T.]] | [[Category: Kohrt, J T.]] | ||
[[Category: Zhang, E.]] | [[Category: Zhang, E.]] | ||
| - | [[Category: | + | [[Category: Blood coagulation]] |
| - | [[Category: | + | [[Category: Egf]] |
| - | [[Category: | + | [[Category: Egf-like domain]] |
| - | [[Category: | + | [[Category: Gla]] |
| - | [[Category: | + | [[Category: Glycoprotein]] |
| - | [[Category: | + | [[Category: Hydrolase]] |
| - | [[Category: | + | [[Category: Hydroxylation]] |
| - | [[Category: | + | [[Category: Lipoprotein]] |
| - | [[Category: | + | [[Category: Palmitate]] |
| - | [[Category: | + | [[Category: Protease]] |
| - | [[Category: | + | [[Category: Receptor enzyme]] |
| - | [[Category: | + | [[Category: Serine protease]] |
| - | [[Category: | + | [[Category: Transmembrane]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:14:08 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 18:14, 3 May 2008
CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121
Overview
The activated factor VII/tissue factor complex (FVIIa/TF) is known to play a key role in the formation of blood clots. Inhibition of this complex may lead to new antithrombotic drugs. A fluoropyridine-based series of FVIIa/TF inhibitors was discovered which utilized a diisopropylamino group for binding in the S2 and S3 binding pockets of the active site of the enzyme complex. In this series, an enhancement in binding affinity was observed by substitution at the 5-position of the hydroxybenzoic acid sidechain. An X-ray crystal structure indicates that amides at this position may increase inhibitor binding affinity through interactions with the S1'/S2' pocket.
About this Structure
2C4F is a Protein complex structure. Full crystallographic information is available from OCA.
Reference
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2., Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Narasimhan LS, Zhang E, Rapundalo ST, Saiya-Cork K, Leadley RJ, Edmunds JJ, Bioorg Med Chem Lett. 2006 Feb 15;16(4):1060-4. Epub 2005 Nov 11. PMID:16289811 Page seeded by OCA on Sat May 3 21:14:08 2008
