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

Research output: Contribution to journalArticlepeer-review

43 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 - 2020 May 25

Bibliographical note

Funding Information:
This work was financially supported by the National Natural Science Foundation of China (Grants 21490574, 21474009, 21975021, 51803009), and a CRI project (No. 2018R1A3B1052702, J.S.K.) of the National Research Foundation of Korea (NRF) and the Basic Science Research Program (2017R1D1A1B03030062, M.W.) funded by the Ministry of Education.

Publisher Copyright:
© 2020 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim

Keywords

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

ASJC Scopus subject areas

  • Catalysis
  • General Chemistry

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