1z71: Difference between revisions

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[[Image:1z71.gif|left|200px]]
{{Seed}}
[[Image:1z71.png|left|200px]]


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{{STRUCTURE_1z71|  PDB=1z71  |  SCENE=  }}  
{{STRUCTURE_1z71|  PDB=1z71  |  SCENE=  }}  


'''thrombin and P2 pyridine N-oxide inhibitor complex structure'''
===thrombin and P2 pyridine N-oxide inhibitor complex structure===




==Overview==
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In this study, we have demonstrated that the critical hydrogen bonding motif of the established 3-aminopyrazinone thrombin inhibitors can be effectively mimicked by a 2-aminopyridine N-oxide. As this peptidomimetic core is more resistant toward oxidative metabolism, it also overcomes the metabolic liability associated with the pyrazinones. An optimization study of the P(1) benzylamide delivered the potent thrombin inhibitor 21 (K(i) = 3.2 nM, 2xaPTT = 360 nM), which exhibited good plasma levels and half-life after oral dosing in the dog (C(max) = 2.6 microM, t(1/2) = 4.5 h).
The line below this paragraph, {{ABSTRACT_PUBMED_15911253}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 15911253 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15911253}}


==About this Structure==
==About this Structure==
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[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
[[Category: Thrombin inhibitor complex]]
[[Category: Thrombin inhibitor complex]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 17:15:27 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 23:47:02 2008''
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