title: 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.
authors: Key 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.
authors: Weiguo
authors: W
authors: Xu
authors: Jianxun
authors: J
authors: Ding
authors: Lingyu
authors: L
authors: Li
authors: Chunsheng
authors: C
authors: Xiao
authors: Xiuli
authors: X
authors: Zhuang
authors: Xuesi
authors: X
authors: Chen
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D001897:Boronic Acids / Q000737:chemistry*; D000069286:Bortezomib / Q000737:chemistry* / Q000494:pharmacology*; D015687:Cell Hypoxia / Q000187:drug effects; D045744:Cell Line, Tumor; D003911:Dextrans / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D065546:Drug Liberation; D004951:Esterification; D006801:Humans; D006863:Hydrogen-Ion Concentration; D051379:Mice; D015398:Signal Transduction / Q000187:drug effects; D015854:Up-Regulation / Q000187:drug effects*
chemical_list: D000970:Antineoplastic Agents; D001897:Boronic Acids; D003911:Dextrans; D004337:Drug Carriers; D000069286:Bortezomib