An acid-labile dextran-bortezomib conjugate (Dex-BTZ), i.e., a macromolecularized 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-κB- and ERS-mediated apoptosis signaling pathways.
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Xu et al. (2015) studied this question.
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