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1w2k

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[[Category: vitamin k]]
[[Category: vitamin k]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 14:48:26 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 5 17:23:26 2007''

Revision as of 15:18, 5 November 2007

Image:1w2k.gif

1w2k, resolution 3.00Å

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TF7A_4380 COMPLEX

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.

About this Structure

1W2K is a Protein complex structure of sequences from Homo sapiens with FUC, BGC, CA, CAC and 380 as ligands. Active as Coagulation factor VIIa, with EC number 3.4.21.21 Structure known Active Site: AC1. 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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