作者: Adrian V. Fuchs , Niklas Kotman , Julien Andrieu , Volker Mailänder , Clemens K. Weiss
DOI: 10.1039/C3NR00706E
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摘要: A solid-phase synthesis based approach towards protease cleavable polystyrene–peptide–polystyrene triblock copolymers and their formulation to nanoparticulate systems is presented. These nanoparticles are suitable for the optical detection of an enzyme have potential application as a drug delivery system. Two different peptide sequences, one cleaved by trypsin (GFF), other hepsin (RQLRVVGG), overexpressed in early stages prostate cancer, used central part triblock. For fluorophore–quencher pair introduced around cleavage sequence. The solid phase conduced such that two identical sequences synthesized from branching point. Eventually, carboxy-terminated polystyrene into synthesizer coupled amino-termini branched Upon cleavage, fragment released copolymer, which has use applications. Conducting whole on avoids solubility issues post-synthetic purification steps. Due hydrophobic PS-chains, copolymer can easily be formulated form using nanoprecipitation process. Incubation with respective enzymes leads significant increase fluorescence incorporated fluorophore, thereby indicating sequence decomposition particles.