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Tailoring the ligand shell for the control of cellular uptake and optical properties of nanocrystals
摘要： In this short review, the main challenges in the use of hydrophobic nanoparticles in biomedical application are addressed. It is shown how to overcome the different issues by the use of a polymeric encapsulation system, based on an amphiphilic polyisoprene-block-poly(ethylene glycol) diblock copolymer. On the basis of this simple molecule, the development of a versatile and powerful phase transfer strategy is summarized, focusing on the main advantages like the adjustable size, the retained properties, the excellent shielding and the diverse functionalization properties of the encapsulated nanoparticles. Finally, the extraordinary properties of these encapsulated nanoparticles in terms of toxicity and specificity in a broad in vitro test is demonstrated.
关键词： quantum dots,biolable,poylmeric micelles,cellular uptake,fluorescence quenching
更新于2025-09-10 09:29:36
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Modulating the cellular uptake of fluorescently tagged substrates of prostate-specific antigen before and after enzymatic activation
摘要： A series of peptides based on the prostate-specific antigen (PSA) specific sequence histidine-serine-serine-lysine-leucine-glutamine were functionalised with an anthraquinone fluorophore at the C-terminal residue side chain using the copper(I) catalyzed azide-alkyne cycloaddition reaction. The effect of incorporating a negatively charged N-terminal tetra-glutamic acid group to the substrate and the effect of masking the negatively charged C-terminal carboxylic acid functionality of the substrate was investigated using confocal fluorescence microscopy in two cell lines (DLD-1 and LnCaP). The addition of a tetra-glutamic acid group to the N-terminus of the intact sequence was shown to reduce cellular uptake of the intact substrate prior to activation by PSA. In contrast, masking the C-terminal carboxylic acid group of the substrate as a methyl ester was shown to improve cellular uptake of the peptide fragment after activation by PSA. The synthesized C-terminal methyl ester substrates with the anthraquinone attached to the side chain were confirmed to be cleaved by PSA in LC-MS analysis, and the cytotoxicity of the substrates was shown to increase in the presence of PSA, consistent with cleavage and uptake of the C-terminal fragment. The results indicate that C- and N- terminal functionalisation of peptide substrates targeting PSA can be used to modulate the cellular uptake of peptides before and after enzymatic activation, and may thus be an important consideration in the design of tumour activated prodrugs.
关键词： peptide substrates,cellular uptake,tumour activated prodrugs,prostate-specific antigen,anthraquinone fluorophore
更新于2025-09-04 15:30:14