1zgi

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[[Image:1zgi.jpg|left|200px]]
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{{Seed}}
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[[Image:1zgi.png|left|200px]]
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{{STRUCTURE_1zgi| PDB=1zgi | SCENE= }}
{{STRUCTURE_1zgi| PDB=1zgi | SCENE= }}
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'''thrombin in complex with an oxazolopyridine inhibitor 21'''
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===thrombin in complex with an oxazolopyridine inhibitor 21===
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==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.
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The line below this paragraph, {{ABSTRACT_PUBMED_16137886}}, adds the Publication Abstract to the page
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(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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 17:35:43 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 09:54:35 2008''

Revision as of 06:54, 29 July 2008

Image:1zgi.png

Template:STRUCTURE 1zgi

thrombin in complex with an oxazolopyridine inhibitor 21

Template:ABSTRACT PUBMED 16137886

About this Structure

1ZGI is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Development of an oxazolopyridine series of dual thrombin/factor Xa inhibitors via structure-guided lead optimization., Deng JZ, McMasters DR, Rabbat PM, Williams PD, Coburn CA, Yan Y, Kuo LC, Lewis SD, Lucas BJ, Krueger JA, Strulovici B, Vacca JP, Lyle TA, Burgey CS, Bioorg Med Chem Lett. 2005 Oct 15;15(20):4411-6. PMID:16137886

Page seeded by OCA on Tue Jul 29 09:54:35 2008

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