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Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter
Malaria remains a major international health challenge. Resistance to a number of existing drugs and evidence of the emergence of artemisinin resistance has emphasized the need for new antimalarials. A new approach has been the preparation of dual-function compounds that include a chloroquine-like a...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Future Medicine Ltd
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7099626/ https://www.ncbi.nlm.nih.gov/pubmed/23534360 http://dx.doi.org/10.2217/fmb.13.18 |
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author | Egan, Timothy J Kuter, David |
author_facet | Egan, Timothy J Kuter, David |
author_sort | Egan, Timothy J |
collection | PubMed |
description | Malaria remains a major international health challenge. Resistance to a number of existing drugs and evidence of the emergence of artemisinin resistance has emphasized the need for new antimalarials. A new approach has been the preparation of dual-function compounds that include a chloroquine-like antimalarial group and a group that resembles a chloroquine chemosensitizer. This article reviews the recent discovery of such dual-function antimalarials that are proposed to target both hemozoin formation and the chloroquine resistance transporter, PfCRT. These are discussed in relation to the mechanism of action of 4-aminoquinolines, chloroquine resistance and resistance reversal. |
format | Online Article Text |
id | pubmed-7099626 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Future Medicine Ltd |
record_format | MEDLINE/PubMed |
spelling | pubmed-70996262020-03-27 Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter Egan, Timothy J Kuter, David Future Microbiol Review Malaria remains a major international health challenge. Resistance to a number of existing drugs and evidence of the emergence of artemisinin resistance has emphasized the need for new antimalarials. A new approach has been the preparation of dual-function compounds that include a chloroquine-like antimalarial group and a group that resembles a chloroquine chemosensitizer. This article reviews the recent discovery of such dual-function antimalarials that are proposed to target both hemozoin formation and the chloroquine resistance transporter, PfCRT. These are discussed in relation to the mechanism of action of 4-aminoquinolines, chloroquine resistance and resistance reversal. Future Medicine Ltd 2013-04 2013-03-27 /pmc/articles/PMC7099626/ /pubmed/23534360 http://dx.doi.org/10.2217/fmb.13.18 Text en © 2013 Future Medicine Ltd This work is licensed under the Creative Commons Attribution 4.0 License (http://creativecommons.org/licenses/by/4.0/) |
spellingShingle | Review Egan, Timothy J Kuter, David Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title | Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title_full | Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title_fullStr | Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title_full_unstemmed | Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title_short | Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
title_sort | dual-functioning antimalarials that inhibit the chloroquine-resistance transporter |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7099626/ https://www.ncbi.nlm.nih.gov/pubmed/23534360 http://dx.doi.org/10.2217/fmb.13.18 |
work_keys_str_mv | AT egantimothyj dualfunctioningantimalarialsthatinhibitthechloroquineresistancetransporter AT kuterdavid dualfunctioningantimalarialsthatinhibitthechloroquineresistancetransporter |