Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments

Romain Mustière (1) , Patrice Vanelle (1, 2) , Nicolas Primas (2)

1 UNICAEN Santé - Université de Caen Normandie - UFR Santé
2 ICR - Institut de Chimie Radicalaire

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 Plasmodium kinome remains to be explored.

Mots clés: kinase inhibitor; Plasmodium; malaria; SAR; medicinal chemistry

Domaines: Chimie

Romain Mustière, Patrice Vanelle, Nicolas Primas. Plasmodial Kinase Inhibitors Targeting Malaria: Recent Developments. Molecules, 2020, 25, ⟨10.3390/molecules25245949⟩. ⟨hal-03246460⟩