2c4f

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{{STRUCTURE_2c4f| PDB=2c4f | SCENE= }}
{{STRUCTURE_2c4f| PDB=2c4f | SCENE= }}
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'''CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121'''
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===CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16289811 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16289811}}
==About this Structure==
==About this Structure==
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[[Category: Serine protease]]
[[Category: Serine protease]]
[[Category: Transmembrane]]
[[Category: Transmembrane]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 08:08:17 2008''

Revision as of 05:08, 29 July 2008

Image:2c4f.png

Template:STRUCTURE 2c4f

CRYSTAL STRUCTURE OF FACTOR VII.STF COMPLEXED WITH PD0297121

Template:ABSTRACT PUBMED 16289811

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

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