Please use this identifier to cite or link to this item: https://hdl.handle.net/10356/180337
Title: Concentration-driven evolution of adaptive artificial ion channels or nanopores with specific anticancer activities
Authors: Chen, Zhiqing
Xie, Xiaopan
Jia, Chunyan
Zhong, Qishuo
Zhang, Qiuping
Luo, Daoxin
Cao, Yin
Mu, Yuguang
Ren, Changliang
Keywords: Medicine, Health and Life Sciences
Issue Date: 2024
Source: Chen, Z., Xie, X., Jia, C., Zhong, Q., Zhang, Q., Luo, D., Cao, Y., Mu, Y. & Ren, C. (2024). Concentration-driven evolution of adaptive artificial ion channels or nanopores with specific anticancer activities. Angewandte Chemie (International Ed. in English), 63(17), e202318811-. https://dx.doi.org/10.1002/anie.202318811
Journal: Angewandte Chemie (International ed. in English)
Abstract: In nature, ceramides are a class of sphingolipids possessing a unique ability to self-assemble into protein-permeable channels with intriguing concentration-dependent adaptive channel cavities. However, within the realm of artificial ion channels, this interesting phenomenon is scarcely represented. Herein, we report on a novel class of adaptive artificial channels, Pn-TPPs, based on PEGylated cholic acids bearing triphenylphosphonium (TPP) groups as anion binding motifs. Interestingly, the molecules self-assemble into chloride ion channels at low concentrations while transforming into small molecule-permeable nanopores at high concentrations. Moreover, the TPP groups endow the molecules with mitochondria-targeting properties, enabling them to selectively drill holes on the mitochondrial membrane of cancer cells and subsequently trigger the caspase 9 apoptotic pathway. The anticancer efficacies of Pn-TPPs correlate with their abilities to form nanopores. Significantly, the most active ensembles formed by P5-TPP exhibits impressive anticancer activity against human liver cancer cells, with an IC50 value of 3.8 μM. While demonstrating similar anticancer performance to doxorubicin, P5-TPP exhibits a selectivity index surpassing that of doxorubicin by a factor of 16.8.
URI: https://hdl.handle.net/10356/180337
ISSN: 1433-7851
DOI: 10.1002/anie.202318811
Schools: School of Biological Sciences 
Rights: © 2024 Wiley-VCH GmbH. All rights reserved.
Fulltext Permission: none
Fulltext Availability: No Fulltext
Appears in Collections:SBS Journal Articles

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