Human thrombin complexed with fragment-based small molecules occupying the S1 pocket

Neumann, Thomas; Junker, Hans‐Dieter; Keil, Oliver; Burkert, Klaus; Ottleben, Holger; Gamer, Jürgen; Sekul, Renate; Deppe, H.; Feurer, Achim; Tomandl, Dirk; Metz, Günther

doi:10.2210/pdb2bvr/pdb

2006

DOI: 10.2210/pdb2bvr/pdb

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Human thrombin complexed with fragment-based small molecules occupying the S1 pocket

Thomas Neumann¹,

Hans‐Dieter Junker²,

Oliver Keil³

et al.

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Direct thrombin inhibitors – a survey of recent developments

Schwienhorst¹

2006

Cell. Mol. Life Sci.

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Thrombin is a plasma serine protease that plays a key role in coagulation and hemostasis but also in thromboembolic diseases. Direct thrombin inhibitors could, therefore, be beneficial for future anticoagulant therapy in the prophylaxis of venous and arterial thrombosis as well as myocardial infarction. However, development of direct thrombin inhibitors has brought researchers more heartache than success. The most recent setback came this year when AstraZeneca withdrew Ximelagatran, the first orally bioavailable direct thrombin inhibitor that had received regulatory approval (France, 2003), after reports of serious hepatoxicity in a fraction of patients. This review describes the status of direct thrombin inhibitors, focusing on drug candidates that are at present in clinical trials. In addition, some more recent research strategies in the design of novel direct thrombin inhibitors are discussed, which may very well contribute to future developments of potent anticoagulants.

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Direct thrombin inhibitors – a survey of recent developments

Schwienhorst¹

2006

Cell. Mol. Life Sci.

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Recent Developments in Fragment-Based Drug Discovery

Congreve¹,

Chessari²,

Tisi³

et al. 2008

J. Med. Chem.

574

516

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Crystallization to obtain protein–ligand complexes for structure-aided drug design

Danley¹

2006

Acta Crystallogr D Biol Crystallogr

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Human thrombin complexed with fragment-based small molecules occupying the S1 pocket

Cited by 5 publications

References 0 publications

Direct thrombin inhibitors – a survey of recent developments

Direct thrombin inhibitors – a survey of recent developments

Recent Developments in Fragment-Based Drug Discovery

Crystallization to obtain protein–ligand complexes for structure-aided drug design

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