Biological effects and activity optimization of small-molecule, drug-like synthetic anion transporters
Copyright © 2019 Elsevier Masson SAS. All rights reserved..
The balance of normal anion concentrations in cells provides basis for maintaining cellular morphology and function. Disrupting the homeostasis of cellular anions and lysosomal pH, in particular with high selectivity for cancer cells over normal cells may serve as a promising approach for the treatment of cancers. Small-molecule organic compounds with transmembrane anion transport activity, namely synthetic anion transporters are able to destroy the homeostasis of cellular anions, in particular chloride anions to trigger cell death and thus may be developed as a new class of anti-tumor drugs. This paper reviews the latest advance in the investigation into the in vitro anion transport, promising anti-tumor activity and probable mechanism of biological action of synthetic anion transporters. The strategies for optimizing the biological activity of synthetic anion transporters and improving the selectivity for cancer cells over normal cells are also discussed.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:184 |
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| Enthalten in: |
European journal of medicinal chemistry - 184(2019) vom: 15. Dez., Seite 111782 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Yu, Xi-Hui [VerfasserIn] |
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| Links: |
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| Themen: |
Activity optimization |
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| Anmerkungen: |
Date Completed 18.02.2020 Date Revised 18.02.2020 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.ejmech.2019.111782 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM302410171 |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2019 Elsevier Masson SAS. All rights reserved. | ||
| 520 | |a The balance of normal anion concentrations in cells provides basis for maintaining cellular morphology and function. Disrupting the homeostasis of cellular anions and lysosomal pH, in particular with high selectivity for cancer cells over normal cells may serve as a promising approach for the treatment of cancers. Small-molecule organic compounds with transmembrane anion transport activity, namely synthetic anion transporters are able to destroy the homeostasis of cellular anions, in particular chloride anions to trigger cell death and thus may be developed as a new class of anti-tumor drugs. This paper reviews the latest advance in the investigation into the in vitro anion transport, promising anti-tumor activity and probable mechanism of biological action of synthetic anion transporters. The strategies for optimizing the biological activity of synthetic anion transporters and improving the selectivity for cancer cells over normal cells are also discussed | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a Activity optimization | |
| 650 | 4 | |a Anion homeostasis | |
| 650 | 4 | |a Anion transporter | |
| 650 | 4 | |a Bioactivity | |
| 650 | 4 | |a Mechanism of biological action | |
| 650 | 7 | |a Antineoplastic Agents |2 NLM | |
| 650 | 7 | |a Organic Anion Transporters |2 NLM | |
| 650 | 7 | |a Small Molecule Libraries |2 NLM | |
| 700 | 1 | |a Hong, Xiao-Qiao |e verfasserin |4 aut | |
| 700 | 1 | |a Mao, Qin-Chao |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Wen-Hua |e verfasserin |4 aut | |
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