Abstract
The drawbacks and limitations of existing anticoagulant therapy which may result in serious adverse effects and a high mortality rate, have given rise to many anticoagulant development programmes in the last decade, focusing mainly at development of thrombin and FXa low-molecular weight inhibitors. A detailed understanding of blood coagulation pathways, functioning of the serine proteases thrombin, FXa, FVIIa and FIXa and elucidation of their crystal structures resulted in many potent compounds, among which some have entered the clinical phase or have been approved for use in clinical practice. Recently, the focus of anticoagulant research turned to inhibition of the TF:FVIIa complex, with some promising clinical candidates on the horizon. This article provides an overview of the current development status of serine protease inhibitors as anticoagulants, including new trends such as dual coagulation factor inhibitors.
Keywords: Anticoagulants, thrombin, FXa and TF, FVIIa inhibitors
Current Pharmaceutical Design
Title: Recent Advances in Serine Protease Inhibitors as Anticoagulant Agents
Volume: 13 Issue: 3
Author(s): Andrej Prezelj, Petra Stefanic Anderluh, Luka Peternel and Uros Urleb
Affiliation:
Keywords: Anticoagulants, thrombin, FXa and TF, FVIIa inhibitors
Abstract: The drawbacks and limitations of existing anticoagulant therapy which may result in serious adverse effects and a high mortality rate, have given rise to many anticoagulant development programmes in the last decade, focusing mainly at development of thrombin and FXa low-molecular weight inhibitors. A detailed understanding of blood coagulation pathways, functioning of the serine proteases thrombin, FXa, FVIIa and FIXa and elucidation of their crystal structures resulted in many potent compounds, among which some have entered the clinical phase or have been approved for use in clinical practice. Recently, the focus of anticoagulant research turned to inhibition of the TF:FVIIa complex, with some promising clinical candidates on the horizon. This article provides an overview of the current development status of serine protease inhibitors as anticoagulants, including new trends such as dual coagulation factor inhibitors.
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Cite this article as:
Prezelj Andrej, Stefanic Anderluh Petra, Peternel Luka and Urleb Uros, Recent Advances in Serine Protease Inhibitors as Anticoagulant Agents, Current Pharmaceutical Design 2007; 13 (3) . https://dx.doi.org/10.2174/138161207779313605
DOI https://dx.doi.org/10.2174/138161207779313605 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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