1w2k: Difference between revisions

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==Overview==
==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.
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.D.]]
[[Category: Arcy, A D.]]
[[Category: Banner, D.W.]]
[[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.B.]]
[[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 Sun Feb 3 10:18:30 2008''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:39:45 2008''

Revision as of 16:39, 21 February 2008

File:1w2k.gif


1w2k, resolution 3.00Å

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TF7A_4380 COMPLEX

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 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.

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

Page seeded by OCA on Thu Feb 21 15:39:45 2008

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