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

doi:10.1002/anie.201916524

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 journal › Article › peer-review

54 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 language	English
Pages (from-to)	8435-8439
Number of pages	5
Journal	Angewandte Chemie - International Edition
Volume	59
Issue number	22
DOIs	https://doi.org/10.1002/anie.201916524
Publication status	Published - 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

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/anie.201916524

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title = "MDM2-Associated Clusterization-Triggered Emission and Apoptosis Induction Effectuated by a Theranostic Spiropolymer",

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.",

keywords = "MDM2 inhibitor, cell apoptosis, clusterization-triggered emission, spiropolymerization, theranostics",

author = "Pai Liu and Weiqiang Fu and Peter Verwilst and Miae Won and Jinwoo Shin and Zhengxu Cai and Bin Tong and Jianbing Shi and Yuping Dong and Kim, {Jong Seung}",

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doi = "10.1002/anie.201916524",

language = "English",

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AU - Liu, Pai

AU - Fu, Weiqiang

AU - Verwilst, Peter

AU - Won, Miae

AU - Shin, Jinwoo

AU - Cai, Zhengxu

AU - Tong, Bin

AU - Shi, Jianbing

AU - Dong, Yuping

AU - Kim, Jong Seung

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PY - 2020/5/25

Y1 - 2020/5/25

N2 - 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.

AB - 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.

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

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

UN SDGs

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