LAUSR

Cancer‐targeting ligands used for nanomedicines have been limited mostly to antibodies, peptides, aptamers, and small molecules thus far. Here, a library of glycocalyx‐mimicking nanoparticles as a platform to enable screening and identification of cancer‐targeting nanomedicines is reported. Specifically, a library of 31 artificial glycopolymers composed of either homogeneous or heterogeneous display of five different sugar moieties (β‐glucose, β‐galactose, α‐mannose, β‐N‐acetyl glucosamine, and β‐N‐acetyl galactosamine) is converted to a library of glyconanoparticles (GlyNPs). GlyNPs optimal for targeting CT26, DU145, A549, and PC3 tumors are systematically screened and identified. The cypate‐conjugated GlyNP displaying α‐mannose and β‐N‐acetyl glucosamine show selective targeting and potent photothermal therapeutic efficacy against A549 human lung tumors. The docetaxel‐contained GlyNP displaying β‐glucose, β‐galactose, and α‐mannose demonstrate targeted chemotherapy against DU145 human prostate tumors. The results presented herein collectively demonstrate that the GlyNP library is a versatile platform enabling the identification of cancer‐targeting glyconanoparticles and suggest its potential applicability for targeting various diseased cells beyond cancer.