含酪氨酸硫酸化修饰的抗凝血蛋白Triabin及其半化学合成方法

By using Fmoc peptide solid-phase synthesis and E. coli recombinant expression technology, tyrosine sulfate-modified Triabin protein was successfully prepared, solving the synthesis problem in the existing technology, improving synthesis efficiency and stability, enhancing anticoagulant activity, and laying the foundation for clinical application.

CN122103315BActive Publication Date: 2026-07-17SOUTH CHINA UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTH CHINA UNIV OF TECH
Filing Date
2026-04-28
Publication Date
2026-07-17

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Abstract

本发明提供了含酪氨酸硫酸化修饰的抗凝血蛋白Triabin及其半化学合成方法。本发明根据距离引入硫酸化酪氨酸位点最近的一个半胱氨酸将Triabin划分为片段1和片段2，硫酸化酪氨酸位点位于片段1中，硫酸化酪氨酸位点靠近片段1的C端；运用多肽固相合成技术合成片段1多肽树脂，经裂解、脱保护、萃取、纯化后得到C端为酰胺的片段1，结合大肠杆菌重组表达技术得到C端为酰肼的片段2，将C端为酰肼的片段2硫酯转化，通过自然化学连接反应与新戊基脱除反应得到全长线性蛋白，经重折叠反应得到含酪氨酸硫酸化修饰的抗凝血蛋白Triabin。含酪氨酸硫酸化修饰的抗凝血蛋白Triabin具有强于野生型Triabin的抗凝活性。
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