Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments

Recent progress in reducing malaria cases and ensuing deaths is threatened by factors like mutations that induce resistance to artemisinin derivatives. Multiple drugs are currently in clinical trials for malaria treatment, including some with novel mechanisms of action. One of these, MMV390048, is a...

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Main Authors: Romain Mustière, Patrice Vanelle, Nicolas Primas
Format: Article
Language:English
Published: MDPI AG 2020-12-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/25/24/5949
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author Romain Mustière
Patrice Vanelle
Nicolas Primas
author_facet Romain Mustière
Patrice Vanelle
Nicolas Primas
author_sort Romain Mustière
collection DOAJ
description Recent progress in reducing malaria cases and ensuing deaths is threatened by factors like mutations that induce resistance to artemisinin derivatives. Multiple drugs are currently in clinical trials for malaria treatment, including some with novel mechanisms of action. One of these, MMV390048, is a plasmodial kinase inhibitor. This review lists the recently developed molecules which target plasmodial kinases. A systematic review of the literature was performed using CAPLUS and MEDLINE databases from 2005 to 2020. It covers a total of 60 articles and describes about one hundred compounds targeting 22 plasmodial kinases. This work highlights the strong potential of compounds targeting plasmodial kinases for future drug therapies. However, the majority of the <i>Plasmodium</i> kinome remains to be explored.
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spelling doaj.art-a4d77204dbf2470ab8a6407337625c082023-11-21T00:58:27ZengMDPI AGMolecules1420-30492020-12-012524594910.3390/molecules25245949Plasmodial Kinase Inhibitors Targeting Malaria: Recent DevelopmentsRomain Mustière0Patrice Vanelle1Nicolas Primas2Aix Marseille Univ, CNRS, ICR UMR 7273, Equipe Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 13385 Marseille CEDEX 05, FranceAix Marseille Univ, CNRS, ICR UMR 7273, Equipe Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 13385 Marseille CEDEX 05, FranceAix Marseille Univ, CNRS, ICR UMR 7273, Equipe Pharmaco-Chimie Radicalaire, Faculté de Pharmacie, 13385 Marseille CEDEX 05, FranceRecent progress in reducing malaria cases and ensuing deaths is threatened by factors like mutations that induce resistance to artemisinin derivatives. Multiple drugs are currently in clinical trials for malaria treatment, including some with novel mechanisms of action. One of these, MMV390048, is a plasmodial kinase inhibitor. This review lists the recently developed molecules which target plasmodial kinases. A systematic review of the literature was performed using CAPLUS and MEDLINE databases from 2005 to 2020. It covers a total of 60 articles and describes about one hundred compounds targeting 22 plasmodial kinases. This work highlights the strong potential of compounds targeting plasmodial kinases for future drug therapies. However, the majority of the <i>Plasmodium</i> kinome remains to be explored.https://www.mdpi.com/1420-3049/25/24/5949kinase inhibitor<i>Plasmodium</i>malariaSARmedicinal chemistry
spellingShingle Romain Mustière
Patrice Vanelle
Nicolas Primas
Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
Molecules
kinase inhibitor
<i>Plasmodium</i>
malaria
SAR
medicinal chemistry
title Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
title_full Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
title_fullStr Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
title_full_unstemmed Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
title_short Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments
title_sort plasmodial kinase inhibitors targeting malaria recent developments
topic kinase inhibitor
<i>Plasmodium</i>
malaria
SAR
medicinal chemistry
url https://www.mdpi.com/1420-3049/25/24/5949
work_keys_str_mv AT romainmustiere plasmodialkinaseinhibitorstargetingmalariarecentdevelopments
AT patricevanelle plasmodialkinaseinhibitorstargetingmalariarecentdevelopments
AT nicolasprimas plasmodialkinaseinhibitorstargetingmalariarecentdevelopments