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首页> 外文会议>NATO Advanced Study Institute on Experimental and Computational Approaches to Structure-Based Drug Design May 9-19, 1996 Erice, Sicily, Italy >Structure-based design of novel heparin-like anticoagulants
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Structure-based design of novel heparin-like anticoagulants

机译：新型肝素样抗凝剂的基于结构的设计

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摘要

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：天然产物肝素已被证明是抗血栓形成剂研究的重要线索。通过合成肝素片段的系统修饰，发现了新的衍生物。其中之一是抗凝血酶III结合五糖1的合成对应物，目前正在临床测试中。最近，许多血液凝结蛋白的结构阐明引发了抗凝研究的新突破。关键的抗凝血酶III-肝素-凝血酶复合物的分子模型激发了新型抗凝剂的设计和合成。可以以合理的方式调节其抗凝血特性，从而获得具有前所未有特性的化合物。肝素的故事说明了药物开发中分子建模和基于结构的设计的弱点和优势。

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