MDM2‐Associated Clusterization‐Triggered Emission and Apoptosis Induction Effectuated by a Theranostic Spiropolymer

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 an...

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Veröffentlicht in:Angewandte Chemie International Edition 2020-05, Vol.59 (22), p.8435-8439
Hauptverfasser: Liu, Pai, Fu, Weiqiang, Verwilst, Peter, Won, Miae, Shin, Jinwoo, Cai, Zhengxu, Tong, Bin, Shi, Jianbing, Dong, Yuping, Kim, Jong Seung
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Sprache:eng
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Zusammenfassung: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. A spiropolymer (P1a2b, see picture) 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 non‐toxicity in non‐cancerous cells.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201916524