1g37: Difference between revisions

New page: left|200px<br /> <applet load="1g37" size="450" color="white" frame="true" align="right" spinBox="true" caption="1g37, resolution 2.0Å" /> '''CRYSTAL STRUCTURE OF...
 
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[[Image:1g37.gif|left|200px]]<br />
[[Image:1g37.gif|left|200px]]<br /><applet load="1g37" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="1g37" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="1g37, resolution 2.0&Aring;" />
caption="1g37, resolution 2.0&Aring;" />
'''CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE'''<br />
'''CRYSTAL STRUCTURE OF HUMAN ALPHA-THROMBIN COMPLEXED WITH BCH-10556 AND EXOSITE-DIRECTED PEPTIDE'''<br />


==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.


==Disease==
==Disease==
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==About this Structure==
==About this Structure==
1G37 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with 110 as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1G37 OCA].  
1G37 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=110:'>110</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1G37 OCA].  


==Reference==
==Reference==
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[[Category: Thrombin]]
[[Category: Thrombin]]
[[Category: Bachand, B.]]
[[Category: Bachand, B.]]
[[Category: Edmunds, J.J.]]
[[Category: Edmunds, J J.]]
[[Category: Leblond, L.]]
[[Category: Leblond, L.]]
[[Category: Siddiqui, M.A.]]
[[Category: Siddiqui, M A.]]
[[Category: St-Denis, Y.]]
[[Category: St-Denis, Y.]]
[[Category: Tarazi, M.]]
[[Category: Tarazi, M.]]
[[Category: Winocour, P.D.]]
[[Category: Winocour, P D.]]
[[Category: 110]]
[[Category: 110]]
[[Category: inhibitor]]
[[Category: inhibitor]]
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[[Category: thrombin]]
[[Category: thrombin]]


''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 17:00:05 2007''
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 12:45:32 2008''

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