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压力循环二硫化物通过与转移素受体反应使细胞吸收成为可能
Daniel Abegg1, Giulio Gasparini1, Dominic G Hoch1
1School of Chemistry and Biochemistry, National Centre of Competence in Research (NCCR) Chemical Biology, University of Geneva , CH-1211 Geneva, Switzerland.
Journal of the American Chemical Society
|December 22, 2016
概括
一种新的酸标签 (AspA标签) 能够有效地吸收未受保护的. 这种方法将送到癌细胞,通过转移素受体向诱导细胞灭绝.
科学领域:
- 生物化学
- 分子生物学
- 细胞生物学
背景情况:
- 如何有效地将治疗性化物输入细胞仍然是一个挑战.
- 不受保护的通常具有不良的稳定性和有限的细胞透.
- 有针对性的输送系统对于提高治疗效果和减少非目标效应至关重要.
研究的目的:
- 开发一种新的,高效的细胞输送方法.
- 研究被标记为酸的的吸收机制.
- 用这种传递系统来诱导癌细胞的亡.
主要方法:
- 一个酸残留物 (AspA标签) 附着在上.
- 使用BH3域诱导癌细胞的AspA标记.
- 化学蛋白质学用于识别AspA标签的分子目标.
- 研究AspA标记与转移素受体之间的相互作用.
主要成果:
- AspA标签确保了未受保护的的有效细胞吸收和细胞内分布.
- AspA标记的BH3域成功诱导了癌细胞的亡.
- 在转移素受体上,AspA部分与556/558的共价键形成被确定为吸收机制.
- 证实了转移素受体介导的内细胞吸收AspA标记的有效载荷.
结论:
- AspA标签是一种小型,无毒,高效的输送系统.
- 该标签利用转移素受体进行向细胞进入.
- 这种方法对包括癌症治疗在内的各种生命科学应用具有重大前景.
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