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Taurine Boosts Intracellular Delivery of Functional Molecules

技術優勢: · Covalent conjugation of taurine is abroadlyapplicable approach to boost the intracellulardelivery of bioactivemolecular and therapeuticagents· The taurine motif ensurestransportation and thesubsequent intracellular nanofibrils formationunderenzymatic catalysis can efficiently reducethe molecular diffusion outside ofcells, providing anew mechanism that eradicates drug resistance.· This method avoids the possibilityof immuneresponse and toxicity caused by CPPs· The natural and non-proteinogenicamino acid,taurine, is widely available, accessible, and itsmolecularmodification facile

技術應用: · As an effective method to delivertherapeutic agents, genes, proteins, and siRNA through otherwise imperviouscellular membranes into targeted cells· A fluorophore may also be conjugated toallowfor intracellular imaging studies

詳細技術說明: Taurine modified D-peptide conjugates significantly enhances cellular uptake of therapeutic molecules for disease diagnosis and treatment.

*Abstract: Internalization of functional moleculesis the basis for intracellular delivery of therapeutic agents for the treatmentand diagnosis of diseases. Unfortunately, the delivery of biologically activemolecules into cells is prevented by the non-permeable plasma cell membrane.Cell penetrating proteins (CPPs) are traditionally used to facilitate thecellular uptake of various cargo, but CPPs are limited by their susceptibilityto metabolic degradation, dependency on cell lines, and poor cellularcompatibility.
The present invention relieson the covalent conjugation of taurine to a D-peptidic hydrogel precursor toovercome the limitations of non-permeable cell membranes and CPPs.Taurine-promoted cellular uptake boosts intracellular delivery by 10X andeliminates immune response, poor stability, and toxicity caused by CPPs. Thisis novel strategy for targeted intracellular enzyme instructed self-assembly ofhydrogels for cancer treatment and may serve as an effective method to delivertherapeutic agents, genes, proteins, and siRNA through otherwise imperviouscellular membranes into targeted cells.

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