定制糖聚合物作为抗凝血肝素模拟物。
Tailored glycopolymers as anticoagulant heparin mimetics.
机构信息
Division of Chemistry and Chemical Engineering and Howard Hughes Medical Institute, California Institute of Technology, 1200 E. California Blvd, Pasadena, CA 91125 (USA).
出版信息
Angew Chem Int Ed Engl. 2013 Nov 4;52(45):11796-9. doi: 10.1002/anie.201306968. Epub 2013 Oct 9.
Abstract
Heparin and its low molecular weight derivatives are clinical therapeutics used to treat and prevent blood clots, but are prone to side effects and contamination. Here we describe the design and expedient synthesis of heparin-based glycopolymers that are potent and potentially safer mimetics of heparin. The mimetics exhibited strong activity against proteases in the coagulation cascade and prolonged blood clot times in human plasma with efficacies similar to those of clinical anticoagulants.
摘要
肝素及其低分子量衍生物是用于治疗和预防血栓形成的临床治疗药物，但容易产生副作用和污染。在这里，我们描述了基于肝素的糖聚合物的设计和方便合成，这些糖聚合物是肝素的有效且潜在更安全的模拟物。这些模拟物对凝血级联中的蛋白酶表现出很强的活性，并延长了人血浆中的血栓形成时间，其功效与临床抗凝剂相似。
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