2anm

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[[Image:2anm.gif|left|200px]]
[[Image:2anm.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2anm |SIZE=350|CAPTION= <scene name='initialview01'>2anm</scene>, resolution 2.40&Aring;
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The line below this paragraph, containing "STRUCTURE_2anm", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=CDO:2-((R)-1-((S)-2-(N-(6-CARBAMIMIDOYLPYRIDIN-3-YL)METHYLCARBAMOYL)-2H-PYRROL-1(5H)-YL)-3-CYCLOHEXYL-1-OXOPROPAN-2-YLAMINO)ACETIC+ACID'>CDO</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Thrombin Thrombin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.5 3.4.21.5] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2anm| PDB=2anm | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2anm FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2anm OCA], [http://www.ebi.ac.uk/pdbsum/2anm PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2anm RCSB]</span>
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}}
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'''Ternary complex of an orally active thrombin inhibitor with human thrombin and a c-terminal hirudin derived exo-sit inhibitor'''
'''Ternary complex of an orally active thrombin inhibitor with human thrombin and a c-terminal hirudin derived exo-sit inhibitor'''
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[[Category: Mack, H.]]
[[Category: Mack, H.]]
[[Category: Seitz, W.]]
[[Category: Seitz, W.]]
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[[Category: blood clotting]]
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[[Category: Blood clotting]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:15:26 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:54:59 2008''
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Revision as of 16:15, 3 May 2008

Image:2anm.gif

Template:STRUCTURE 2anm

Ternary complex of an orally active thrombin inhibitor with human thrombin and a c-terminal hirudin derived exo-sit inhibitor


Overview

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.

About this Structure

2ANM 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 Sat May 3 19:15:26 2008

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OCA

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