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Acid-labile boronate-bridged dextran-bortezomib conjugate with up-regulated hypoxic tumor suppression
Weiguo Xu1, Jianxun Ding, Lingyu Li
1Key Laboratory of Polymer Ecomaterials, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, P. R. China. jxding@ciac.ac.cn xschen@ciac.ac.cn.
Abstract:
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.

