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从乙酰肝素快速两步合成米曲菌素:肝素的替代品。

Rapid two-step synthesis of mitrin from heparosan: a replacement for heparin.

作者信息

Kuberan Balagurunathan, Beeler David L, Lawrence Roger, Lech Miroslaw, Rosenberg Robert D

机构信息

Department of Biology, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA.

出版信息

J Am Chem Soc. 2003 Oct 15;125(41):12424-5. doi: 10.1021/ja036737g.

Abstract

We have engineered a two-step enzymatic synthesis of Mitrin which is a more potent and homogeneous anticoagulant than the current animal-derived heparin. This engineered heparin may have advantages of being free from animal-derived pathogens and may also have reduced side effects such as heparin induced thrombocytopenia. This approach can also be extended to tailor heparin-based drugs with improved therapeutic characteristics to treat other disorders or infections in which heparin-like molecules play a major role.

摘要

我们设计了一种两步酶促合成米曲菌素的方法,米曲菌素是一种比目前动物源性肝素更有效且更均一的抗凝剂。这种工程化肝素可能具有无动物源性病原体的优势,并且还可能减少诸如肝素诱导的血小板减少症等副作用。这种方法还可以扩展到定制具有改善治疗特性的基于肝素的药物,以治疗其他疾病或感染,其中肝素样分子起主要作用。

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