2b7d

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[[Image:2b7d.gif|left|200px]]
[[Image:2b7d.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2b7d |SIZE=350|CAPTION= <scene name='initialview01'>2b7d</scene>, resolution 2.24&Aring;
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The line below this paragraph, containing "STRUCTURE_2b7d", 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=C1B:(2R)-2-[5-(5-CARBAMIMIDOYL-1H-BENZOIMIDAZOL-2-YL)-6,2&#39;-DIHYDROXY-5&#39;-UREIDOMETHYL-BIPHENYL-3-YL]-SUCCINIC+ACID'>C1B</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/Coagulation_factor_VIIa Coagulation factor VIIa], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.21 3.4.21.21] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= F7 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]), F3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2b7d| PDB=2b7d | 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=2b7d FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2b7d OCA], [http://www.ebi.ac.uk/pdbsum/2b7d PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2b7d RCSB]</span>
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}}
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'''Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model'''
'''Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model'''
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[[Category: Young, W B.]]
[[Category: Young, W B.]]
[[Category: Yu, C.]]
[[Category: Yu, C.]]
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[[Category: short hydrogen bond]]
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[[Category: Short hydrogen bond]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 19:56:48 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:02:33 2008''
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Revision as of 16:56, 3 May 2008

Image:2b7d.gif

Template:STRUCTURE 2b7d

Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model


Contents

Overview

Highly selective and potent factor VIIa-tissue factor (fVIIa.TF) complex inhibitors were generated through structure-based design. The pharmacokinetic properties of an optimized analog (9) were characterized in several preclinical species, demonstrating pharmacokinetic characteristics suitable for once-a-day dosing in humans. Analog 9 inhibited platelet and fibrin deposition in a dose-dependent manner after intravenous administration in a baboon thrombosis model, and a pharmacodynamic concentration-response model was developed to describe the platelet deposition data. Results for heparin and enoxaparin (Lovenox) in the baboon model are also presented.

Disease

Known disease associated with this structure: Factor VII deficiency OMIM:[227500], Myocardial infarction, decreased susceptibility to OMIM:[227500]

About this Structure

2B7D is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Factor VIIa inhibitors: chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model., Young WB, Mordenti J, Torkelson S, Shrader WD, Kolesnikov A, Rai R, Liu L, Hu H, Leahy EM, Green MJ, Sprengeler PA, Katz BA, Yu C, Janc JW, Elrod KC, Marzec UM, Hanson SR, Bioorg Med Chem Lett. 2006 Apr 1;16(7):2037-41. Epub 2006 Jan 18. PMID:16412633 Page seeded by OCA on Sat May 3 19:56:48 2008

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OCA

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