1w2k: Difference between revisions
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|PDB= 1w2k |SIZE=350|CAPTION= <scene name='initialview01'>1w2k</scene>, resolution 3.00Å | |PDB= 1w2k |SIZE=350|CAPTION= <scene name='initialview01'>1w2k</scene>, resolution 3.00Å | ||
|SITE= <scene name='pdbsite=AC1:Bgc+Binding+Site+For+Chain+L'>AC1</scene> | |SITE= <scene name='pdbsite=AC1:Bgc+Binding+Site+For+Chain+L'>AC1</scene> | ||
|LIGAND= <scene name='pdbligand= | |LIGAND= <scene name='pdbligand=380:(2R)-2-({4-[AMINO(IMINO)METHYL]PHENYL}AMINO)-N-BENZYL-2-(3,4-DIMETHOXYPHENYL)ACETAMIDE'>380</scene>, <scene name='pdbligand=BGC:BETA-D-GLUCOSE'>BGC</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CAC:CACODYLATE+ION'>CAC</scene>, <scene name='pdbligand=CGU:GAMMA-CARBOXY-GLUTAMIC+ACID'>CGU</scene>, <scene name='pdbligand=FUC:ALPHA-L-FUCOSE'>FUC</scene> | ||
|ACTIVITY= [http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] </span> | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1w2k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1w2k OCA], [http://www.ebi.ac.uk/pdbsum/1w2k PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1w2k RCSB]</span> | |||
}} | }} | ||
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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. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Wallbaum, S.]] | [[Category: Wallbaum, S.]] | ||
[[Category: Weber, L.]] | [[Category: Weber, L.]] | ||
[[Category: blood coagulation]] | [[Category: blood coagulation]] | ||
[[Category: calcium-binding]] | [[Category: calcium-binding]] | ||
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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 Mon Mar 31 00:30:16 2008'' | ||