首页|Tumor microenvironment-activatable neuropeptide-drug conjugates enhanced tumor penetration and inhibition via multiple delivery pathways and calcium deposition
Tumor microenvironment-activatable neuropeptide-drug conjugates enhanced tumor penetration and inhibition via multiple delivery pathways and calcium deposition
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Peptide-drug conjugates have achieved considerable development and application as a novel strategy for targeted delivery of anticancer drugs.Bioactive peptides induced calcium deposition can irreversibly assist inhibition of tumors.However,active regulation of calcium level through signal transduction of bioactive substances has not been reported yet.In this study,novel neuropeptide-doxorubicin conju-gates(NP-DOX)with lysosome-specific acid response were described for neuropeptide Y1 receptor(Y1R)-overexpressed triple-negative breast cancer.The delivery mechanism of NP-DOX was clarified that diverse pathways were involved,including intracellular and intercellular transport.Importantly,up-regulation of Y1R-mediated intracellular calcium level via second messenger inositol triphosphate was presented in NP-DOX treated MDA-MB-231 cells.In vivo antitumor efficacy demonstrated that NP-DOX showed less organ toxicity and enhanced tumor inhibition benefited from its controlled release and Y1R-mediated calcium deposition,compared with free DOX.This bioconjugate is a proof-of-concept confirming that neuropeptide-mediated control of signaling responses in neuropeptide-drug conjugates enables great po-tential for further applications in tumor chemotherapy.
Neuropeptide-drug conjugateTumor penetrationCalcium depositionTumor inhibitionTriple-negative breast cancer
Yi Cao、Xiaojiao Ge、Yuanyuan Wei、Lulu He、Aiguo Wu、Juan Li
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Ningbo Key Laboratory of Biomedical Imaging Probe Materials and Technology,Zhejiang International Cooperation Base of Biomedical Materials Technology and Application,Chinese Academy of Sciences(CAS)Key Laboratory of Magnetic Materials and Devices,Ningbo Cixi Institute of Biomedical Engineering,Zhejiang Engineering Research Center for Biomedical Materials,Ningbo Institute of Materials Technology and Engineering,Chinese Academy of Sciences,Ningbo 315201,China
University of Chinese Academy of Sciences,Beijing
Advanced Energy Science and Technology Guangdong L
Key Research and Development Pro-gram of Zhejiang Province国家自然科学基金国家自然科学基金国家自然科学基金Science and Technology Bureau of Ningbo CityScience and Technology Bureau of Ningbo CityExcellent Member of Youth Innovation Promotion Association Foundation of CAS
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