Acid-labile boronate-bridged dextran–bortezomib conjugate with up-regulated hypoxic tumor suppression

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.