Journal
CHEMICAL COMMUNICATIONS
Volume 51, Issue 31, Pages 6812-6815Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c5cc01371b
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Funding
- National Natural Science Foundation of China [51303174, 51273196, 51203153, 51233004, 51390484, 51321062]
- Scientific Development Program of Jilin Province [20140520050JH]
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An acid-labile dextran-bortezomib conjugate (Dex-BTZ), i.e., a macro-molecularized proteasome inhibitor, is synthesized by a boron esterification reaction. The prodrug exhibits intracellular acidity-accelerated BTZ release, and up-regulated inhibition efficacies toward hypoxic tumor in vitro and in vivo through both NF-kappa B- and ERS-mediated apoptosis signaling pathways.
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