1g37: Difference between revisions
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|PDB= 1g37 |SIZE=350|CAPTION= <scene name='initialview01'>1g37</scene>, resolution 2.0Å | |PDB= 1g37 |SIZE=350|CAPTION= <scene name='initialview01'>1g37</scene>, resolution 2.0Å | ||
|SITE= | |SITE= | ||
|LIGAND= <scene name='pdbligand=110:3-(4-AMINO-CYCLOHEXYL)-2-HYDROXY-3-[(4-OXO-2-PHENYLMETHANESULFONYL-1,2,3,4-TETRAHYDRO-PYRROLO[1,2-A]PYRAZINE-6-CARBONYL)-AMINO]-PROPIONIC ACID BUTYL ESTER'>110</scene> | |LIGAND= <scene name='pdbligand=110:3-(4-AMINO-CYCLOHEXYL)-2-HYDROXY-3-[(4-OXO-2-PHENYLMETHANESULFONYL-1,2,3,4-TETRAHYDRO-PYRROLO[1,2-A]PYRAZINE-6-CARBONYL)-AMINO]-PROPIONIC+ACID+BUTYL+ESTER'>110</scene> | ||
|ACTIVITY= [http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] </span> | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1g37 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1g37 OCA], [http://www.ebi.ac.uk/pdbsum/1g37 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1g37 RCSB]</span> | |||
}} | }} | ||
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==Overview== | ==Overview== | ||
Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model. | Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Tarazi, M.]] | [[Category: Tarazi, M.]] | ||
[[Category: Winocour, P D.]] | [[Category: Winocour, P D.]] | ||
[[Category: inhibitor]] | [[Category: inhibitor]] | ||
[[Category: protease]] | [[Category: protease]] | ||
[[Category: thrombin]] | [[Category: thrombin]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:35:35 2008'' |