1w2k
From Proteopedia
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==Overview== | ==Overview== | ||
- | Proof of concept experiments have shown that tissue factor/factor VIIa | + | 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== | ==Disease== | ||
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[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Ackermann, J.]] | [[Category: Ackermann, J.]] | ||
- | [[Category: Arcy, A | + | [[Category: Arcy, A D.]] |
- | [[Category: Banner, D | + | [[Category: Banner, D W.]] |
[[Category: Groebke-Zbinden, K.]] | [[Category: Groebke-Zbinden, K.]] | ||
[[Category: Ji, Y.]] | [[Category: Ji, Y.]] | ||
[[Category: Kirchhofer, D.]] | [[Category: Kirchhofer, D.]] | ||
- | [[Category: Tschopp, T | + | [[Category: Tschopp, T B.]] |
[[Category: Wallbaum, S.]] | [[Category: Wallbaum, S.]] | ||
[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
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[[Category: vitamin k]] | [[Category: vitamin k]] | ||
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:39:45 2008'' |
Revision as of 13:39, 21 February 2008
|
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
Page seeded by OCA on Thu Feb 21 15:39:45 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