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

Pai Liu, Weiqiang Fu, Peter Verwilst, Miae Won, Jinwoo Shin, Zhengxu Cai*, Bin Tong, Jianbing Shi, Yuping Dong, Jong Seung Kim

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

53 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)8435-8439
Number of pages5
JournalAngewandte Chemie - International Edition
Volume59
Issue number22
DOIs
Publication statusPublished - 25 May 2020

Keywords

  • MDM2 inhibitor
  • cell apoptosis
  • clusterization-triggered emission
  • spiropolymerization
  • theranostics

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