1sb1: Difference between revisions

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[[Image:1sb1.gif|left|200px]]
{{Seed}}
[[Image:1sb1.png|left|200px]]


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{{STRUCTURE_1sb1|  PDB=1sb1  |  SCENE=  }}  
{{STRUCTURE_1sb1|  PDB=1sb1  |  SCENE=  }}  


'''Novel Non-Covalent Thrombin Inhibitors Incorporating P1 4,5,6,7-Tetrahydrobenzothiazole Arginine Side Chain Mimetics'''
===Novel Non-Covalent Thrombin Inhibitors Incorporating P1 4,5,6,7-Tetrahydrobenzothiazole Arginine Side Chain Mimetics===




==Overview==
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The design, synthesis and biological activity of a series of novel non-covalent D-Phe-Pro-Arg motif-based thrombin inhibitors incorporating 4,5,6,7-tetrahydrobenzothiazol-2-amine as a novel arginine surrogate are described. Compound 9, the most potent in the series of thrombin inhibitors, exhibited an in vitro K(i) of 128 nM and 342-fold selectivity against trypsin. The binding mode of this novel class of thrombin inhibitors in the enzyme active site, based on the X-ray crystal structure of compound 9 co-crystallized with human alpha-thrombin, is discussed.
The line below this paragraph, {{ABSTRACT_PUBMED_15051174}}, adds the Publication Abstract to the page
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{{ABSTRACT_PUBMED_15051174}}


==About this Structure==
==About this Structure==
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[[Category: Serine protease inhibitor]]
[[Category: Serine protease inhibitor]]
[[Category: Thrombin]]
[[Category: Thrombin]]
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