1g37

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[[Image:1g37.gif|left|200px]]
[[Image:1g37.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1g37 |SIZE=350|CAPTION= <scene name='initialview01'>1g37</scene>, resolution 2.0&Aring;
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The line below this paragraph, containing "STRUCTURE_1g37", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|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>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|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>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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|DOMAIN=
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{{STRUCTURE_1g37| PDB=1g37 | SCENE= }}
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|RELATEDENTRY=
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|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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}}
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'''CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE'''
'''CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE'''
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[[Category: Tarazi, M.]]
[[Category: Tarazi, M.]]
[[Category: Winocour, P D.]]
[[Category: Winocour, P D.]]
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[[Category: inhibitor]]
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[[Category: Inhibitor]]
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[[Category: protease]]
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[[Category: Protease]]
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[[Category: thrombin]]
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[[Category: Thrombin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Fri May 2 17:04:54 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 20:35:35 2008''
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Revision as of 14:04, 2 May 2008

Image:1g37.gif

Template:STRUCTURE 1g37

CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE


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.

About this Structure

1G37 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Potent and selective bicyclic lactam inhibitors of thrombin. Part 4: transition state inhibitors., Bachand B, Tarazi M, St-Denis Y, Edmunds JJ, Winocour PD, Leblond L, Siddiqui MA, Bioorg Med Chem Lett. 2001 Feb 12;11(3):287-90. PMID:11212093 Page seeded by OCA on Fri May 2 17:04:54 2008

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OCA

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