GALA peptide improves the potency of nanobody–drug conjugates by lipid-induced helix formation

Autor: Zhengshuang Xu, Xiao Chun Guo, Yong Juan Zhao, Hon Cheung Lee, Ya Jie Chen, Jian Yuan Yang, Qi Wen Deng, Li Wang, Ting Li
Rok vydání: 2021
Předmět:
Zdroj: Chemical Communications. 57:1434-1437
ISSN: 1364-548X
1359-7345
DOI: 10.1039/d0cc07706b
Popis: A novel nanobody-drug conjugate (NDC) was constructed by incorporating an amphipathic peptide, GALA, which improved the cytotoxicity by one to two orders of magnitude. Mechanistic studies demonstrate that tethering to lipids induces GALA to form a helix, which dramatically enhances endocytosis. Our work provides a general strategy not only for improving the anti-cancer efficacy of protein-drug conjugates but also for increasing the efficiency of other types of endocytosis-dependent cell delivery.
Databáze: OpenAIRE