2b7d

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Revision as of 18:52, 12 November 2007

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spinqualitylabelsall models 2b7d, resolution 2.24Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

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

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

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 diseases associated with this structure: Esophageal squamous cell carcinoma OMIM:[606551], 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 with C1B as ligand. Active as Coagulation factor VIIa, with EC number 3.4.21.21 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

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