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1w2k

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Revision as of 08:18, 3 February 2008 by OCA (Talk | contribs)
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Image:1w2k.gif

1w2k, resolution 3.00Å

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TF7A_4380 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

1W2K 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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