1w2k
From Proteopedia
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, resolution 3.00Å | |||||||
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Sites: | |||||||
Ligands: | , , , and | ||||||
Activity: | Coagulation factor VIIa, with EC number 3.4.21.21 | ||||||
Coordinates: | save as pdb, mmCIF, xml |
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. 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
Page seeded by OCA on Thu Mar 20 14:51:12 2008
Categories: Coagulation factor VIIa | Homo sapiens | Protein complex | Ackermann, J. | Arcy, A D. | Banner, D W. | Groebke-Zbinden, K. | Ji, Y. | Kirchhofer, D. | Tschopp, T B. | Wallbaum, S. | Weber, L. | 380 | BGC | CA | CAC | FUC | Blood coagulation | Calcium-binding | Co-factor | Coagulation | Enzyme complex | Gamma-carboxyglutamic acid | Glycoprotein | Hydrolase | Plasma | Serine protease | Vitamin k