刘梦,于彭城,徐寒梅.蛋白多肽类药物长效化技术研究进展[J].药学进展,2019,43(03):209-216.

  

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蛋白多肽类药物长效化技术研究进展

刘梦于  彭城  徐寒梅

中国药科大学江苏省合成多肽药物发现与评价工程研究中心

摘要：近年来,蛋白多肽类药物因在治疗疾病方面具有显著的优点,普遍受到研究者的青睐;另一方面,蛋白多肽类药物半衰期一般较短,影响患者用药顺应性。结合蛋白多肽类药物药动学特点,总结蛋白多肽类药物长效化方法的研究进展,主要包括氨基酸替代、定点修饰突变、通过基因手段与其他蛋白融合、糖基化、环化、与聚合物缀合、钉合肽,以及新剂型开发等方法,希望能对药物研发工作者有所帮助。
关键词： 蛋白多肽类药物;药动学特点;长效化技术;
专辑： 医药卫生科技
专题： 药学
分类号： R96


文章目录
1 蛋白多肽类药物药动学特点
    1.1 吸收
    1.2 分布
    1.3 代谢和消除
2 改善蛋白多肽类药物半衰期的方式
    2.1 氨基酸替代
    2.2 定点修饰突变
    2.3 通过基因手段与其他蛋白融合
    2.4 糖基化
    2.5 环化
    2.6 与聚合物缀合
        2.6.1 PEG化学修饰
        2.6.2 非结构化可生物降解蛋白缀合
        2.6.3 PAS缀合
        2.6.4 羟乙基化淀粉缀合
    2.7 钉合肽
    2.8 药物传递系统开发
3 结语



刘梦,于彭城,徐寒梅.蛋白多肽类药物长效化技术研究进展[J].药学进展,2019,43(03):209-216.
[ 作者介绍 ] 徐寒梅：中国药科大学教授，博士生导师，江苏省合成多肽药物发现与评价工程研究中心主任，国家药典委员会委员，中组部“万人计划”入选者。多年从事多肽药物的研究，带领团队自主设计合成了多个多肽药物、转让了 4 个 1 类多肽新药，有 2 个已经进入临床研究。近 5 年在国内外发表学术论文 80 余篇，SCI 论文 35 篇；主编及参编论著各 1 部，主编教材 1 部；申请发明专利及软件著作权共 35 项 ( 其中国际专利 5 项 )，获得授权 15 项。近年来，先后带领团队主持了：国家自然科学基金，国家“863”高科技发展计划，国家“十一五”、“十二五”、“十三五”重大新药创制科技重大专项多项，江苏省校企合作前瞻性研究等项目。2014 年获得江苏省医药科技奖一等奖（排名第一），曾获得科技部创新创业人才、南京市领军人才、科技创业家等称号。

 
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 刘梦,于彭城,徐寒梅.蛋白多肽类药物长效化技术研究进展[J].药学进展,2019,43(03):209-216.