Enabling AIEgens close assembly in tumor-overexpressed protein cluster for boosted image-guided cancer surgery
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abling AIEgens close assembly in tumor-overexpressed protein cluster for boosted image-guided cancer surgery 1
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Junxiao Gao , Jun Li , Daohe Wei , Han Yang , Yue Duan , Yue Zhang , Xiaoqun Gong , 1 2 1* 1* Hanjie Wang , Dan Ding , Xiaoli Wu & Jin Chang 1
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School of Life Sciences, Tianjin University, Tianjin 300072, China; Key Laboratory of Bioactive Materials, Ministry of Education, College of Life Sciences, Nankai University, Tianjin 300071, China Received June 30, 2020; accepted July 15, 2020; published online October 20, 2020
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 selfassembling 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-RFFGYSA 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 microenvironmentresponsive AIE probes for boost FIGCS. aggregation-induced emission luminogen, fluorescent probe, self-assembling peptide, fluorescence image-guided cancer surgery, tumor-to-normal tissue ratio Citation:
Gao J, Li J, Wei D, Yang H, Duan Y, Zhang Y, Gong X, Wang H, Ding D, Wu X, Chang J. Enabling AIEgens close assembly in tumor-overexpressed protein cluster for boosted image-guided cancer surgery. Sci China Chem, 2020, 63, https://doi.org/10.1007/s11426-020-9829-x
1 Introduction In recent years, fluorescence image-guided cancer surgery (FIGCS) has received great attention in both research and clinic as it has been demonstrated as a powerful tool to boost the cancer surgery outcomes by virtue of helping surgeon differentiate the margins between tumors and normal tissues as well as detect and remove the residue/microsized tumors during operation [1–6]. Fluorescent probes in particular those with emission in the near-infrared (NIR, >650 nm) region play a key role in the process of FIGCS and highly *Corresponding authors (email: [email protected]; [email protected])
emissive probes with specific tumor-targeting capability are always considerably desirable [7–10]. To date, several kinds
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