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MDM2‐Associated Clusterization‐Triggered Emission and Apoptosis Induction Effectuated by a Theranostic Spiropolymer
Author(s) -
Liu Pai,
Fu Weiqiang,
Verwilst Peter,
Won Miae,
Shin Jinwoo,
Cai Zhengxu,
Tong Bin,
Shi Jianbing,
Dong Yuping,
Kim Jong Seung
Publication year - 2020
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201916524
Subject(s) - apoptosis , cytotoxicity , mdm2 , docking (animal) , heteroatom , biocompatibility , microbiology and biotechnology , chemistry , cancer cell , biophysics , nanotechnology , biochemistry , materials science , biology , cancer , in vitro , genetics , medicine , ring (chemistry) , nursing , organic chemistry
Heteroatom‐containing spiropolymers were constructed in a facile manner by a catalyst‐free multicomponent spiropolymerization route. P1a2b as the most potent of these spiropolymers, demonstrates cluster‐triggered emission resulting from strong interactions with the MDM2 protein. By preventing the anti‐apoptotic p53/MDM2 interaction, P1a2b triggers apoptosis in cancerous cells, while demonstrating a good biocompatibility and non‐toxicity in non‐cancerous cells. The combined results from solution and cell‐based cluster‐triggered emission studies, docking, protein expression experiments and cytotoxicity data strongly support the MDM2‐binding hypothesis and indicate a potential application as a fluorescent cancer marker as well as therapeutic for this spiropolymer.