Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities
We report here a novel class of cation transporters with extreme simplicity, opening a whole new dimension of scientific research for finding small molecule-based cation transporters for therapeutic applications. Comprising three modular components (a headgroup, a flexible alkyl chain-derived body,...
| Main Authors: | , , , , |
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| Other Authors: | |
| Format: | Journal Article |
| Language: | English |
| Published: |
2023
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| Subjects: | |
| Online Access: | https://hdl.handle.net/10356/171493 |
| _version_ | 1811685856464863232 |
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| author | Zhang, Hao Ye, Ruijuan Mu, Yuguang Li, Tianhu Zeng, Huaqiang |
| author2 | School of Biological Sciences |
| author_facet | School of Biological Sciences Zhang, Hao Ye, Ruijuan Mu, Yuguang Li, Tianhu Zeng, Huaqiang |
| author_sort | Zhang, Hao |
| collection | NTU |
| description | We report here a novel class of cation transporters with extreme simplicity, opening a whole new dimension of scientific research for finding small molecule-based cation transporters for therapeutic applications. Comprising three modular components (a headgroup, a flexible alkyl chain-derived body, and a crown ether-derived foot for ion binding), these transporters efficiently (EC50 = 0.18-0.41 mol % relative to lipid) and selectively (K+/Na+ selectivity = 7.0-9.5) move K+ ions across the membrane. Importantly, the most active (EC50 = 0.18-0.22 mol %) and highly selective series of transporters A12, B12, and C12 concurrently possess potent anticancer activities with IC50 values as low as 4.35 ± 0.91 and 6.00 ± 0.13 μM toward HeLa and PC3 cells, respectively. Notably, a mere replacement of the 18-crown-6 unit in the structure with 12-crown-4 or 15-crown-5 units completely annihilates the cation-transporting ability. |
| first_indexed | 2024-10-01T04:51:10Z |
| format | Journal Article |
| id | ntu-10356/171493 |
| institution | Nanyang Technological University |
| language | English |
| last_indexed | 2024-10-01T04:51:10Z |
| publishDate | 2023 |
| record_format | dspace |
| spelling | ntu-10356/1714932023-11-03T02:13:45Z Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities Zhang, Hao Ye, Ruijuan Mu, Yuguang Li, Tianhu Zeng, Huaqiang School of Biological Sciences Science::Biological sciences Supramolecular Chemistry Artificial Membrane Transporters We report here a novel class of cation transporters with extreme simplicity, opening a whole new dimension of scientific research for finding small molecule-based cation transporters for therapeutic applications. Comprising three modular components (a headgroup, a flexible alkyl chain-derived body, and a crown ether-derived foot for ion binding), these transporters efficiently (EC50 = 0.18-0.41 mol % relative to lipid) and selectively (K+/Na+ selectivity = 7.0-9.5) move K+ ions across the membrane. Importantly, the most active (EC50 = 0.18-0.22 mol %) and highly selective series of transporters A12, B12, and C12 concurrently possess potent anticancer activities with IC50 values as low as 4.35 ± 0.91 and 6.00 ± 0.13 μM toward HeLa and PC3 cells, respectively. Notably, a mere replacement of the 18-crown-6 unit in the structure with 12-crown-4 or 15-crown-5 units completely annihilates the cation-transporting ability. 2023-11-03T01:45:54Z 2023-11-03T01:45:54Z 2021 Journal Article Zhang, H., Ye, R., Mu, Y., Li, T. & Zeng, H. (2021). Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities. Nano Letters, 21(3), 1384-1391. https://dx.doi.org/10.1021/acs.nanolett.0c04134 1530-6984 https://hdl.handle.net/10356/171493 10.1021/acs.nanolett.0c04134 33464086 2-s2.0-85100254260 3 21 1384 1391 en Nano Letters © 2021 American Chemical Society. All rights reserved. |
| spellingShingle | Science::Biological sciences Supramolecular Chemistry Artificial Membrane Transporters Zhang, Hao Ye, Ruijuan Mu, Yuguang Li, Tianhu Zeng, Huaqiang Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title | Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title_full | Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title_fullStr | Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title_full_unstemmed | Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title_short | Small molecule-based highly active and selective K⁺ transporters with potent anticancer activities |
| title_sort | small molecule based highly active and selective k⁺ transporters with potent anticancer activities |
| topic | Science::Biological sciences Supramolecular Chemistry Artificial Membrane Transporters |
| url | https://hdl.handle.net/10356/171493 |
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