Antimalarials: Review of Plasmepsins as Drug Targets and HIV Protease Inhibitors Interactions

Author(s): Whelton A. Miller III, Joshua Teye, Angela O. Achieng, Reagan M. Mogire, Hoseah Akala, John M. Ong'echa, Brijesh Rathi, Ravi Durvasula, Prakasha Kempaiah*, Samuel K. Kwofie*

Journal Name: Current Topics in Medicinal Chemistry

Volume 18 , Issue 23 , 2018

Become EABM
Become Reviewer
Call for Editor

Graphical Abstract:


Malaria is a major global health concern with the majority of cases reported in regions of South-East Asia, Eastern Mediterranean, Western Pacific, the Americas, and Sub-Saharan Africa. The World Health Organization (WHO) estimated 216 million worldwide reported cases of malaria in 2016. It is an infection of the red blood cells by parasites of the genus Plasmodium with most severe and common forms caused by Plasmodium falciparum (P. falciparum or Pf) and Plasmodium vivax (P. vivax or Pv). Emerging parasite resistance to available antimalarial drugs poses great challenges to treatment. Currently, the first line of defense includes artemisinin combination therapies (ACTs), increasingly becoming less effective and challenging to combat new occurrences of drug-resistant parasites. This necessitates the urgent need for novel antimalarials that target new molecular pathways with a different mechanism of action from the traditional antimalarials. Several new inhibitors and potential drug targets of the parasites have been reported over the years. This review focuses on the malarial aspartic proteases known as plasmepsins (Plms) as novel drug targets and antimalarials targeting Plms. It further discusses inhibitors of hemoglobin-degrading plasmepsins Plm I, Plm II, Plm IV and Histo-aspartic proteases (HAP), as well as HIV protease inhibitors of plasmepsins.

Keywords: Malaria, Antimalarials, P. falciparum, Plasmepsin, HIV Protease Inhibitors, P. vivax drug targets.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2018
Page: [2022 - 2028]
Pages: 7
DOI: 10.2174/1568026619666181130133548
Price: $65

Article Metrics

PDF: 40