Targeting protein kinases in the malaria parasite: update of an antimalarial drug target

Zhang, Veronica M., Chavchich, Marina and Waters, Norman C. (2012) Targeting protein kinases in the malaria parasite: update of an antimalarial drug target. Current Topics in Medicinal Chemistry, 12 5: 456-472. doi:10.2174/156802612799362922

Attached Files (Some files may be inaccessible until you login with your UQ eSpace credentials)
Name Description MIMEType Size Downloads

Author Zhang, Veronica M.
Chavchich, Marina
Waters, Norman C.
Title Targeting protein kinases in the malaria parasite: update of an antimalarial drug target
Journal name Current Topics in Medicinal Chemistry   Check publisher's open access policy
ISSN 1568-0266
Publication date 2012-03
Sub-type Article (original research)
DOI 10.2174/156802612799362922
Volume 12
Issue 5
Start page 456
End page 472
Total pages 17
Editor Allen B. Reitz
Rhoda W. Joseph
Marvin J. Meyers
Place of publication Bussum, Netherlands
Publisher Bentham Science Publishers
Collection year 2013
Language eng
Formatted abstract
Millions of deaths each year are attributed to malaria worldwide. Transmitted through the bite of an Anopheles mosquito, infection and subsequent death from the Plasmodium species, most notably P. falciparum, can readily spread through a susceptible population. A malaria vaccine does not exist and resistance to virtually every antimalarial drug predicts that mortality and morbidity associated with this disease will increase. With only a few antimalarial drugs currently in the pipeline, new therapeutic options and novel chemotypes are desperately needed. Hit-to-Lead diversity may successfully provide novel inhibitory scaffolds when essential enzymes are targeted, for example, the plasmodial protein kinases. Throughout the entire life cycle of the malaria parasite, protein kinases are essential for growth and development. Ongoing efforts continue to characterize these kinases, while simultaneously pursuing them as antimalarial drug targets. A collection of structural data, inhibitory profiles and target validation has set the foundation and support for targeting the malarial kinome. Pursuing protein kinases as cancer drug targets has generated a wealth of information on the inhibitory strategies that can be useful for antimalarial drug discovery. In this review, progress on selected protein kinases is described. As the search for novel antimalarials continues, an understanding of the phosphor-regulatory pathways will not only validate protein kinase targets, but also will identify novel chemotypes to thwart malaria drug resistance.
Keyword Antimalarial agents
Drug development
Kinase family
Plasmodium falciparum
Plasmodiual protein kinases
Protein kinases
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2013 Collection
School of Chemistry and Molecular Biosciences
Version Filter Type
Citation counts: TR Web of Science Citation Count  Cited 19 times in Thomson Reuters Web of Science Article | Citations
Scopus Citation Count Cited 22 times in Scopus Article | Citations
Google Scholar Search Google Scholar
Created: Fri, 16 Mar 2012, 09:23:06 EST by Lucy O'Brien on behalf of School of Chemistry & Molecular Biosciences