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[1]易享炎,何天同,曹臻,等.Bcl-XL蛋白拮抗剂分子设计的研究进展[J].生物加工过程,2018,16(06):70-79.[doi:10.3969/j.issn.1672-3678.2018.06.013]
 YI Xiangyan,HE Tiantong,CAO Zhen,et al.Advances in molecular design of Bcl-XL protein antagonists[J].Chinese Journal of Bioprocess Engineering,2018,16(06):70-79.[doi:10.3969/j.issn.1672-3678.2018.06.013]
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Bcl-XL蛋白拮抗剂分子设计的研究进展()
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《生物加工过程》[ISSN:1672-3678/CN:32-1706/Q]

卷:
16
期数:
2018年06期
页码:
70-79
栏目:
出版日期:
2018-11-30

文章信息/Info

Title:
Advances in molecular design of Bcl-XL protein antagonists
文章编号:
1672-3678(2018)06-0070-10
作者:
易享炎何天同曹臻张婉玲付豪亮汪丽泽于杨黄和杨雅琼黄菲
南京工业大学 药学院,江苏 南京 211800
Author(s):
YI XiangyanHE TiantongCAO ZhenZHANG WanlingFU HaoliangWANG LizeYU YangHUANG HeYANG YaqiongHUANG Fei
School of Pharmaceutical Sciences,Nanjing Tech University,Nanjing 211800,China
关键词:
Bcl-XL 分子设计 苯甲酰脲骨架 磺酰胺骨架 苯并噻唑骨架 生物医学
分类号:
R914.2
DOI:
10.3969/j.issn.1672-3678.2018.06.013
文献标志码:
A
摘要:
Bcl-XL是Bcl-2家族蛋白重要的成员之一。作为细胞凋亡的关键效应因子,已成为目前最具吸引力的癌症治疗靶点之一。在介绍Bcl-2家族蛋白调控细胞凋亡机制的基础上,对近5年报道的新型Bcl-XL蛋白拮抗剂的分子设计历程进行综述,着重阐述基于全新药物设计方法、高通量筛选、X线单晶衍射技术、计算机辅助药物设计以及衍生化修饰设计出的3类结构新颖、活性显著和靶向性优良的小分子肽模拟物。研究表明:苯甲酰脲类对Bcl-XL蛋白具有极强的靶向性; 磺酰胺类对Bcl-XL蛋白的抑制活性可以达到纳摩尔水平; 苯并噻唑类具有极佳的生物利用度。这3类分子骨架的设计代表了现代抗癌药物分子设计中三大发展方向,该研究将会对未来抗癌药物的研发提供借鉴,同时还对3类化合物作为Bcl-XL蛋白拮抗剂的发展进行了展望。

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备注/Memo

备注/Memo:
收稿日期:2017-11-29修回日期:2017-12-26
基金项目:江苏高校优秀科技创新团队计划(苏教科[2015]4号文); 江苏省先进生物制造创新中心(XTC1810、XTE1850)
作者简介:易享炎(1993—),男,江苏连云港人,硕士研究生,研究方向:药物化学; 杨雅琼(联系人),讲师,E-mail:yangyq@njtech.edu.cn; 黄菲(联系人),讲师,E-mail: huangfei@njtech.edu.cn
引文格式:易享炎,何天同,曹臻,等.Bcl-XL蛋白拮抗剂分子设计的研究进展[J].生物加工过程,2018,16(6):70-79.
YI Xiangyan,HE Tiantong,CAO Zhen,et al.Advances in molecular design of Bcl-XL protein antagonists[J].Chin J Bioprocess Eng,2018,16(6):70-79..
更新日期/Last Update: 2018-11-30