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Multifunctional AuI-based AIEgens: Manipulating Molecular Structures and Boosting Specific Cancer Cell Imaging and Theranostics
Authors:Jing Zhang  Dr Hang Zou  Jinping Lei  Benzhao He  Xuewen He  Dr Herman H Y Sung  Dr Ryan T K Kwok  Dr Jacky W Y Lam  Prof Lei Zheng  Prof Ben Zhong Tang
Institution:1. Department of Chemistry, Hong Kong Branch of Chinese National Engineering, Research Center for Tissue Restoration and Reconstruction, Institute for Advanced Study, Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China

These authors contributed equally to this work.;2. Department of Laboratory Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515 China

These authors contributed equally to this work.;3. School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006 China

These authors contributed equally to this work.;4. Department of Chemistry, Hong Kong Branch of Chinese National Engineering, Research Center for Tissue Restoration and Reconstruction, Institute for Advanced Study, Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China;5. Department of Chemistry, Hong Kong Branch of Chinese National Engineering, Research Center for Tissue Restoration and Reconstruction, Institute for Advanced Study, Department of Chemical and Biological Engineering, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, China

HKUST-Shenzhen Research Institute, No. 9 Yuexing 1st RD, South Area, Hi-tech Park, Nanshan, Shenzhen, 518057 China;6. Department of Laboratory Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515 China

Abstract:Gold(I) N-heterocyclic carbene (AuI-NHC) complexes have emerged as potential anticancer agents owing to their high cytotoxicity and stability. Integration of their above unique functions with customized aggregation-induced emission (AIE) luminogens to achieve specific bioimaging and efficient theranostics to cancer is highly desirable but is rarely studied. Now, a series of novel AuI-NHC compounds were developed with AIE characteristics. A complex with a PPh3 ligand was selected out as it could achieve both prominent specific imaging of various cancer cells and efficient inhibition of their growth with negligible toxic effects on normal cells due to the targeting binding and strong inhibition towards thioredoxin reductase. This complex could also act as a powerful radiosensitizer to boost the anticancer efficacy with performance superior to that of popularly used auranofin. It holds great potential as a specific and effective theranostic drug in cancer diagnosis and precise therapy.
Keywords:Aggregationsinduzierte Emission  Gold(I)-Komplexe  Radiosensibilisatoren  Spezifische Biobildgebung  Thioredoxin-Reduktase
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