1zgi: Difference between revisions

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[[Image:1zgi.jpg|left|200px]]
{{Seed}}
[[Image:1zgi.png|left|200px]]


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{{STRUCTURE_1zgi|  PDB=1zgi  |  SCENE=  }}  
{{STRUCTURE_1zgi|  PDB=1zgi  |  SCENE=  }}  


'''thrombin in complex with an oxazolopyridine inhibitor 21'''
===thrombin in complex with an oxazolopyridine inhibitor 21===




==Overview==
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Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolopyridines. A modification intended to attenuate plasma protein binding (i.e., conversion of the P3 pyridine to a piperidine) conferred significant factor Xa activity to this series. Ultimately, these dual thrombin/factor Xa inhibitors demonstrated excellent in vitro and in vivo anticoagulant efficacy.
The line below this paragraph, {{ABSTRACT_PUBMED_16137886}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 16137886 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16137886}}


==About this Structure==
==About this Structure==
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[[Category: Thrombin]]
[[Category: Thrombin]]
[[Category: Thrombin inhibitor complex]]
[[Category: Thrombin inhibitor complex]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 17:35:43 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:54:35 2008''
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