2ank: Difference between revisions

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Bots, Bureaucrats, journal, Administrators
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OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,328,572 edits
No edit summary
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[[Image:2ank.jpg|left|200px]]
{{Seed}}
[[Image:2ank.png|left|200px]]


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{{STRUCTURE_2ank|  PDB=2ank  |  SCENE=  }}  
{{STRUCTURE_2ank|  PDB=2ank  |  SCENE=  }}  


'''orally active thrombin inhibitors in complex with thrombin and an exosite decapeptide'''
===orally active thrombin inhibitors in complex with thrombin and an exosite decapeptide===




==Overview==
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Synthesis and SAR of orally active thrombin inhibitors of the d-Phe-Pro-Arg type with focus on the P2-moiety are described. The unexpected increase in in vitro potency, oral bioavailability, and in vivo activity of inhibitors with dehydroproline as P2-isostere is discussed. Over a period of 24h the antithrombin activity of the most active inhibitors with IC(50)s in the nanomolar range was determined in dogs demonstrating high thrombin inhibitory activity in plasma and an appropriate duration of action after oral administration.
The line below this paragraph, {{ABSTRACT_PUBMED_16460939}}, adds the Publication Abstract to the page
(as it appears on PubMed at http://www.pubmed.gov), where 16460939 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16460939}}


==About this Structure==
==About this Structure==
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[[Category: Hydrolase]]
[[Category: Hydrolase]]
[[Category: Serine protease]]
[[Category: Serine protease]]
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 19:15:22 2008''
 
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:37:44 2008''
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