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1Endoplasmic reticulum targeted AIE bioprobe as a highly efficient inducer of immunogenic cell death显示文摘Focused oxidative stress of the specific organelles(e.g.,endoplasmic reticulum(ER)and mitochondrion)of cancer cells can boost the immunogenic cell death(ICD)effect for cancer immunotherapy.Herein,an ER-targeted bioprobe with aggregationinduced emission(AIE)characteristics(TPE-PR-FFKDEL)was rationally designed and synthesized by integrating a new AIE photosensitizer with ER targeting peptide,which has been demonstrated to be able to efficiently induce ER oxidative stress to evoke ICD.Compared with the photosensitizer hypericin that is well-known as an ER-targeted ICD inducer,TPE-PR-FFKDEL can lead to more robust emission of immunostimulatory damage-associated molecular patterns such as surface-exposed calreticulin,ATP secretion,and high-mobility group protein B1(HMGB1)and heat shock protein 70(HSP 70)expression.Furthermore,a range of immune responses are activated to protect mice from the attack of cancer cells in vivo.Jun Li Heqi Gao Ruihua Liu Chao Chen Sheng Zeng Qian Liu Dan Ding 2020Science China Chemistry2020,63,10:2
2Enabling AIEgens close assembly in tumor-overexpressed protein cluster for boosted image-guided cancer surgery显示文摘Development of efficient fluorescent probes that can realize precise fluorescence image-guided cancer surgery(FIGCS)with extremely high tumor-to-normal tissue(T/NT)ratio is urgently desirable.Herein,we report the design and synthesis of an aggregation-induced emission(AIE)-active,peptide-based fluorescence turn-on probe MPA-Ph-R-FFGYSAYPDSVPMMS(MPA-Ph-R-FFGYSA for short),which consists of a new near-infrared emissive AIE luminogen(AIEgen)MPA-Ph-R,a self-assembling peptide sequence“FFG”,and an“active”targeting peptide YSAYPDSVPMMS that can selectively bind to EphA2 protein cluster overexpressed in many cancers.As compared to the control probe MPA-Ph-R-YSA without“FFG”,MPA-Ph-R-FFGYSA exhibits much higher fluorescent brightness and sensitivity in both cellular and in vivo studies on EphA2 cluster detection/imaging,as“FFG”is beneficial to closer assembly of AIEgens in EphA2 cluster,leading to more effective restriction of the intramolecular motion of AIEgen.In vivo studies demonstrate that MPA-Ph-R-FFGYSA is a safe bioprobe and gives excellent performance in FIGCS with a rather high T/NT ratio of^13.4 upon intravenous administration into peritoneal carcinomatosis-bearing mice.This study provides a new strategy of utilizing the close assembly of tumor microenvironment-responsive AIE probes for boost FIGCS.Junxiao Gao Jun Li Daohe Wei Han Yang Yue Duan Yue Zhang Xiaoqun Gong Hanjie Wang Dan Ding Xiaoli Wu Jin Chang 2020Science China Chemistry2020,63,11:0
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