Jiangsu Key Laboratory of Translational Research and Therapy for Neuro-Psycho-Diseases and College of Pharmaceutical Sciences , Soochow University , Suzhou , Jiangsu 215021 , China.
Center for Biotechnology and Interdisciplinary Studies , Rensselaer Polytechnic Institute , 110 8th Street , Troy , New York 12180 , United States.
J Med Chem. 2019 Jan 24;62(2):1067-1073. doi: 10.1021/acs.jmedchem.8b01551. Epub 2019 Jan 14.
Heparin is a polypharmacological agent with anticoagulant activity. Periodate oxidation of the nonsulfated glucuronic acid residue results in non-anticoagulant heparin derivative (NACH) of reduced molecular weight. Similar treatment of a low molecular weight heparin, dalteparin, also removes its anticoagulant activity, affording a second heparin derivative (D-NACH). A full structural characterization of these two derivatives reveals their structural differences. SPR studies display their ability to bind to several important heparin-binding proteins, suggesting potential new therapeutic applications.
肝素是一种具有抗凝活性的多药效药物。过碘酸盐氧化非硫酸化葡萄糖醛酸残基可导致分子量降低的非抗凝肝素衍生物（NACH）。类似地处理低分子量肝素达肝素，也会去除其抗凝活性，得到第二种肝素衍生物（D-NACH）。对这两种衍生物的完整结构特征分析揭示了它们的结构差异。SPR 研究显示它们能够与几种重要的肝素结合蛋白结合，这表明它们可能具有新的治疗应用。
