Ultrasound activatable antiangiogenic sonosensitizer for VEGFR associated glioblastoma tumor models  

作　　者：Subin Son Chuangli Zhang Miae Won Paramesh Jangili Minhyeok Choi Jiasheng Wu Jong Seung Kim 

机构地区：[1]Department of Chemistry,Korea University,Seoul,Korea [2]Key Laboratory of Photochemical Conversion and Optoelectronic,Technical Institute of Physics and Chemistry,Chinese Academy of Sciences,Beijing,China

出　　处：《Aggregate》2021年第4期137-143,共7页聚集体（英文）

基　　金：National Research Foundation ofKorea,Grant/Award Numbers:2018R1A3B1052702,2019M3E5D1A01068998;Basic Science Research Program,Grant/Award Number:2020R1A6A3A01100551;Ministry ofEducation,andNationalNatural Science Foundation of China,Grant/Award Number:21673265。

摘　　要：Angiogenic signaling pathway is a major contributing factor in cancer recurrence and progression,which can cause significantly reduced treatment outcomes,especially in the oxygen-dependent photo-and sonodynamic therapies.VEGF and its receptor(VEGFR)play a crucial role in angiogenesis progression;precisely,upregulated VEGF signaling ismainly associated with angiogenesis progression in many types of cancers.Herein,we report a sunitinib-conjugated sonosensitizer(TK-RB:tyrosine kinase-rose bengal)to enhance the anticancer efficacy through VEGF inhibitionmediated antiangiogenesis in conjunction with cellular/tumor damage by ROS generated under ultrasound irradiation.TK-RB reveals good selectivity and cytotoxicity toward VEGFR-positive cells(U87MG)over VEGFR-negative cells(MCF-7).The fluorescent imaging analysis in vivo/ex vivo and the tumor growth investigation in nude mice with U87MG glioblastoma tumor xenografts demonstrate that rose bengal having tyrosine kinase inhibitor(TK-RB)provides an enhanced antitumor effect.The current strategy will make a great contribution to optimizing anticancer performance by utilizing sonodynamic therapy together with antiangiogenics in several different malignancies.

关 键 词：ANTIANGIOGENESIS GLIOBLASTOMA sonodynamic therapy VEGFR blockage 

分 类 号：R73[医药卫生—肿瘤]