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1w0y

From Proteopedia

Revision as of 13:39, 21 February 2008 by OCA (Talk | contribs)
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Image:1w0y.gif

1w0y, resolution 2.50Å

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TF7A_3771 COMPLEX

Contents

Overview

Proof of concept experiments have shown that tissue factor/factor VIIa inhibitors have antithrombotic activity without enhancing bleeding propensity. Starting from lead compounds generated by a biased combinatorial approach, phenylglycine amide tissue factor/factor VIIa inhibitors with low nanomolar affinity and good selectivity against other serine proteases of the coagulation cascade were designed, using the guidance of X-ray structural analysis and molecular modelling.

Disease

Known diseases associated with this structure: Esophageal squamous cell carcinoma OMIM:[606551], Factor VII deficiency OMIM:[227500], Myocardial infarction, decreased susceptibility to OMIM:[227500]

About this Structure

1W0Y is a Protein complex structure of sequences from Homo sapiens with , , , and as ligands. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Known structural/functional Site: . Full crystallographic information is available from OCA.

Reference

Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors., Groebke Zbinden K, Banner DW, Ackermann J, D'Arcy A, Kirchhofer D, Ji YH, Tschopp TB, Wallbaum S, Weber L, Bioorg Med Chem Lett. 2005 Feb 1;15(3):817-22. PMID:15664864

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