2c4f: Difference between revisions
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==Overview== | ==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. | 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. | ||
==Disease== | |||
Known diseases associated with this structure: Esophageal squamous cell carcinoma OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=606551 606551]], Factor VII deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]], Myocardial infarction, decreased susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]] | |||
==About this Structure== | ==About this Structure== | ||
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[[Category: transmembrane]] | [[Category: transmembrane]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:10:30 2007'' | ||
