TF7A_4380 COMPLEX

File:1w2k.gif


PDB ID 1w2k

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, resolution 3.00Å
Sites:
Ligands: , , , and
Activity: Coagulation factor VIIa, with EC number 3.4.21.21
Coordinates: save as pdb, mmCIF, xml



OverviewOverview

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.

DiseaseDisease

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 StructureAbout this Structure

1W2K is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

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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