Department of Chemistry and Center for NanoScience (CeNS), Ludwig-Maximilians-Universität München, Butenandtstrasse 5-13, D-81377 München, Germany.
Nano Lett. 2012 Jul 11;12(7):3417-23. doi: 10.1021/nl300395q. Epub 2012 Jun 5.
Therapeutic nanoparticles can be directed to cancer cells by incorporating selective targeting ligands. Here, we investigate the epidermal growth factor receptor (EGFR)-mediated endocytosis of gene carriers (polyplexes) either targeted with natural EGF or GE11, a short synthetic EGFR-binding peptide. Highly sensitive live-cell fluorescence microcopy with single particle resolution unraveled the existence of two different uptake mechanisms; EGF triggers accelerated nanoparticle endocytosis due to its dual active role in receptor binding and signaling activation. For GE11, an alternative EGFR signaling independent, actin-driven pathway is presented.
治疗性纳米颗粒可以通过整合选择性靶向配体来靶向癌细胞。在这里，我们研究了表皮生长因子受体（EGFR）介导的基因载体（多聚物）的内吞作用，这些基因载体要么与天然 EGF 结合，要么与短合成 EGFR 结合肽 GE11 结合。具有单颗粒分辨率的高灵敏度活细胞荧光显微镜揭示了两种不同的摄取机制的存在；由于 EGF 在受体结合和信号激活中的双重作用，EGF 触发了加速的纳米颗粒内吞作用。对于 GE11，则提出了一种替代的 EGFR 信号独立的、肌动蛋白驱动的途径。
