1w2k: Difference between revisions
No edit summary |
No edit summary |
||
| Line 6: | Line 6: | ||
==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== | |||
Known diseases associated with this structure: Esophageal squamous cell carcinoma OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=606551 606551]], Factor VII deficiency OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]], Myocardial infarction, decreased susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=227500 227500]] | |||
==About this Structure== | ==About this Structure== | ||
| Line 41: | Line 44: | ||
[[Category: vitamin k]] | [[Category: vitamin k]] | ||
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 19:46:20 2007'' | ||
Revision as of 20:39, 12 November 2007
|
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 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.
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 Mon Nov 12 19:46:20 2007
Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)
OCA- Pages with broken file links
- 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