2b7d

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{{STRUCTURE_2b7d| PDB=2b7d | SCENE= }}
{{STRUCTURE_2b7d| PDB=2b7d | SCENE= }}
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'''Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model'''
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===Factor VIIa Inhibitors: Chemical Optimization, Preclinical Pharmacokinetics, Pharmacodynamics, and Efficacy in a Baboon Thrombosis Model===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16412633 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16412633}}
==Disease==
==Disease==
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[[Category: Yu, C.]]
[[Category: Yu, C.]]
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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 Jul 28 01:58:28 2008''

Revision as of 22:58, 27 July 2008

Image:2b7d.png

Template:STRUCTURE 2b7d

Contents

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

Template:ABSTRACT PUBMED 16412633

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 Mon Jul 28 01:58:28 2008

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