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肝素及其相关产品的制备与合成研究进展。

Advances in the preparation and synthesis of heparin and related products.

机构信息

Department of Chemistry & Chemical Biology, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, NY, USA; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, Ankara, Turkey.

Department of Chemistry & Chemical Biology, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, NY, USA; Department of Chemical and Biological Engineering, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, NY, USA; Department of Biological Sciences, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, NY, USA.

出版信息

Drug Discov Today. 2020 Dec;25(12):2095-2109. doi: 10.1016/j.drudis.2020.09.011. Epub 2020 Sep 16.

Abstract

Heparin is a naturally occurring glycosaminoglycan from livestock, principally porcine intestine, and is clinically used as an anticoagulant drug. A limitation to heparin production is that it depends on a single animal species and potential problems have been associated with animal-derived heparin. The contamination crisis in 2008 led to a search for new animal sources and the investigation of non-animal sources of heparin. Over the past 5 years, new animal sources, chemical, and chemoenzymatic methods have been introduced to prepare heparin-based drugs. In this review, we describe advances in the preparation and synthesis of heparin and related products.

摘要

肝素是一种天然存在的糖胺聚糖,主要来自猪的肠道,临床上用作抗凝药物。肝素生产的一个限制因素是它依赖于单一的动物物种,并且与动物来源的肝素有关的潜在问题。2008 年的污染危机导致人们寻找新的动物来源,并研究肝素的非动物来源。在过去的 5 年中,已经引入了新的动物来源、化学和化学酶方法来制备肝素类药物。在这篇综述中,我们描述了肝素及其相关产品的制备和合成方面的进展。

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本文引用的文献

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Programmable One-Pot Synthesis of Heparin Pentasaccharide Fondaparinux.肝素五糖磺达肝癸钠的可编程一锅法合成
Org Lett. 2020 Jun 19;22(12):4638-4642. doi: 10.1021/acs.orglett.0c01386. Epub 2020 Jun 4.
4
Chemoenzymatic Synthesis of Glycosaminoglycans.糖胺聚糖的酶促化学合成。
Acc Chem Res. 2020 Feb 18;53(2):335-346. doi: 10.1021/acs.accounts.9b00420. Epub 2019 Nov 12.
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Chemoenzymatic synthesis of ultralow and low-molecular weight heparins.酶化学法合成超低分子量肝素和低分子量肝素。
Biochim Biophys Acta Proteins Proteom. 2020 Feb;1868(2):140301. doi: 10.1016/j.bbapap.2019.140301. Epub 2019 Oct 31.
6
Porcine Mucosal Heparin Shortage Crisis! What Are the Options?猪黏膜肝素短缺危机!有哪些应对方案?
Clin Appl Thromb Hemost. 2019 Jan-Dec;25:1076029619878786. doi: 10.1177/1076029619878786.

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