2ank

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[[Image:2ank.jpg|left|200px]]
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{{Seed}}
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[[Image:2ank.png|left|200px]]
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{{STRUCTURE_2ank| PDB=2ank | SCENE= }}
{{STRUCTURE_2ank| PDB=2ank | SCENE= }}
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'''orally active thrombin inhibitors in complex with thrombin and an exosite decapeptide'''
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===orally active thrombin inhibitors in complex with thrombin and an exosite decapeptide===
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==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.
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The line below this paragraph, {{ABSTRACT_PUBMED_16460939}}, adds the Publication Abstract to the page
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(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]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:15:22 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 07:37:44 2008''

Revision as of 04:37, 29 July 2008

Image:2ank.png

Template:STRUCTURE 2ank

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

Template:ABSTRACT PUBMED 16460939

About this Structure

2ANK is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety., Lange UE, Baucke D, Hornberger W, Mack H, Seitz W, Hoffken HW, Bioorg Med Chem Lett. 2006 May 15;16(10):2648-53. Epub 2006 Feb 3. PMID:16460939

Page seeded by OCA on Tue Jul 29 07:37:44 2008

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