乳糖功能化卡博西兰糖基基基因分离剂是高强度的多价值连接物,用于 Galectin-9 结合:增加对 Galectins 的 Glycan 亲和力与聚合行为相关
Monika Müllerová1, Michaela Hovorková2,3, Táňa Závodná4
1Institute of Chemical Process Fundamentals, Czech Academy of Sciences, Rozvojová 135, 165 02 Prague, Czech Republic.
Biomacromolecules
|September 8, 2023
概括
具有多个乳糖单元的碳西兰糖基基因分离体显示出显著增强的结合亲和力与素,特别是Gal-9. 与单个乳糖分子相比,这种多价值呈现显著增强了抑制作用.
科学领域:
- 生物化学 生物化学
- 葡萄糖生物学 葡萄糖生物学
- 纳米技术纳米技术
背景情况:
- 盖लेक्ट因是糖甘结合蛋白质,对生物调节至关重要.
- 了解加勒-配体相互作用是开发向疗法的关键.
- 碳烯树状体提供可调节的纳米支架,用于呈现碳水化合物连接体.
研究的目的:
- 为了合成乳糖功能化的碳基糖基基因组分离剂 (Lac-CS-DDMs).
- 为了研究这些甘氨基基的亲和力对双重类型的 galectins.
- 为了证明多价值联结体呈现对加勒素抑制的影响.
主要方法:
- 合成两种类型的乳糖功能化碳酸甘氨基基基基因组.
- 与酶相关的免疫吸收试验 (ELISA) 用于测量加列的结合亲和力.
- 动态光散射 (DLS) 用于分析聚合物形成.
主要成果:
- 拉克-CS-DDMs表现出强烈的,树突效应驱动的亲和力对双重类型的质素,特别是Gal-9.
- 一种第三代含有32个乳糖单位的甘氨基二烯酸获得了对Gal-9的纳米分子亲和力 (IC50 = 970 nM),比单价乳糖提高了1400倍.
- 通过DLS观察到,与稳定的加勒/Lac-CS-DDM聚合物的形成相关的亲和力增加.
结论:
- 通过卡博西兰树脂体,通过乳糖等简单配体的多价呈现显著增强了结合亲和力和阻碍力对抗 galectins.
- 这些甘氨基基基因表现为有前途的治疗药物,准了加列介导的过程.
- 这些发现凸显了多价值在设计有效的基于糖甘的抑制剂中的关键作用.
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