title: The rational design of a gemcitabine prodrug with AIE-based intracellular light-up characteristics for selective suppression of pancreatic cancer cells.
abstract: An enzyme and reduction-activatable gemcitabine prodrug (TPE-GEM-RGD) with aggregation-induced emission (AIE) properties was designed for targeted and image-guided cancer therapy. TPE-GEM-RGD was successfully used for intracellular light-up imaging and glutathione (GSH)-responsive release of gemcitabine to suppress pancreatic cancer cells.
authors.affiliation: MOE Key Laboratory of Macromolecule Synthesis and Functionalization of Ministry of Education, Department of Polymer Science and Engineering, Zhejiang University, Hangzhou, 310027, China. jinqiao@zju.edu.cn jijian@zju.edu.cn.
authors.forename: Haijie
authors.initials: H
authors.lastname: Han
authors.forename: Qiao
authors.initials: Q
authors.lastname: Jin
authors.forename: Yin
authors.initials: Y
authors.lastname: Wang
authors.forename: Yangjun
authors.initials: Y
authors.lastname: Chen
authors.forename: Jian
authors.initials: J
authors.lastname: Ji
mesh_terms: D000595:Amino Acid Sequence; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D019328:Buthionine Sulfoximine / Q000494:pharmacology; D002401:Cathepsin B / Q000037:antagonists & inhibitors / Q000378:metabolism; D045744:Cell Line, Tumor; D015853:Cysteine Proteinase Inhibitors / Q000494:pharmacology; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D004151:Dipeptides / Q000494:pharmacology; D004705:Endocytosis / Q000502:physiology; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000378:metabolism / Q000627:therapeutic use*; D005978:Glutathione / Q000031:analogs & derivatives / Q000037:antagonists & inhibitors / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000502:physiology; D010084:Oxidation-Reduction; D010190:Pancreatic Neoplasms / Q000188:drug therapy*; D011355:Prodrugs / Q000138:chemical synthesis* / Q000378:metabolism / Q000627:therapeutic use; D000093542:Gemcitabine
chemical_list: D000970:Antineoplastic Agents; D015853:Cysteine Proteinase Inhibitors; D004151:Dipeptides; D005456:Fluorescent Dyes; D039302:Integrin alphaVbeta3; D011355:Prodrugs; D003841:Deoxycytidine; C068250:N-(3-propylcarbamoyloxirane-2-carbonyl)-isoleucyl-proline; D019328:Buthionine Sulfoximine; C042431:S-ethyl glutathione; D002401:Cathepsin B; D005978:Glutathione; D000093542:Gemcitabine