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However, enhancing ligand\u2010receptor selectivity and precisely controlling subsequent cellular behavior remain significant challenges. In this study, we developed a receptor\u2010mediated cascade amplification strategy via glycopeptides (GPs) to regulate the dynamic self\u2010assembly of artificial ligands, enhancing ligand\u2010receptor selectivity. By designing the assembly sequences, we control the antagonistic relationship between dynamic nanostructures and receptor\u2010mediated internalization. Our findings show that in fast cascade amplification, rapid fiber network formation inhibits internalization, while in slow amplification, receptor aggregation enhances internalization, promoting cellular uptake. This precise regulation further impacts the spatial distribution and function of receptor, ultimately controlling cellular phenotypes. Based on real\u2010world needs, we applied the cascade amplification strategy to enhance the efficacy of PD\u2010L1 tumor immunotherapy. 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