Structure-based design of novel heparin-like anticoagulants

机译：基于结构的新型肝素样抗凝剂设计

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The natural product heparin has turned out to be an important lead for the research on antithrombotics. By systematic modification of synthetic heparin fragments new derivatives were discovered. One of them, the synthetic counterpart of the antithrombin III binding pentasaccharide 1, is now being tested clinically. Recently, the structure elucidation of a number of blood coagulation proteins initiated a new breakthrough in the anticoagulant research. Molecular modelling of the cruical antithrombin III - heparin - thrombin complex inspired the design and synthesis of a novel class of anticoagulants. Their anticoagulant properties can be adjusted in a rational way leading to compounds with unprecedented characteristics. The heparin story illustrates the weaknesses and strengths of molecular modelling and structure-based design in drug discovery.

机译：天然产物肝素已致原因是对抗血栓管学研究的重要铅。通过系统改性合成肝素片段，发现了新的衍生物。其中一个是临床上测试抗凝血酶III结合戊二糖1的合成对应物。最近，许多血液凝固蛋白的结构阐明在抗凝研究中启动了新的突破。 Cruical抗胰蛋白酶III - 肝素 - 凝血酶复合物的分子建模启发了一种新型抗凝血剂的设计和合成。它们的抗凝血性能可以以理性的方式调整，导致具有前所未有的特征的化合物。肝素故事说明了药物发现中分子建模和基于结构的设计的弱点和优势。

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《NATO advanced study institute on experimental and computational approaches to structure-based drug design》|1998年||共11页
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Peter D. J. Grootenhuis; Constant A. A. van Boeckel; NATO;
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中图分类药物基础科学;
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4. Structure-based design of novel heparin-like anticoagulants [C] . Peter D. J. Grootenhuis, Constant A. A. van Boeckel, NATO NATO advanced study institute on experimental and computational approaches to structure-based drug design . 1998

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Structure-based design of novel heparin-like anticoagulants

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