Targeting malaria parasite invasion of red blood cells as an antimalarial strategy

AL Burns, MG Dans, JM Balbin… - FEMS microbiology …, 2019 - academic.oup.com
Plasmodium spp. parasites that cause malaria disease remain a significant global-health
burden. With the spread of parasites resistant to artemisinin combination therapies in …

Parasite and host kinases as targets for antimalarials

HW Ong, J Adderley, AB Tobin… - Expert Opinion on …, 2023 - Taylor & Francis
ABSTRACT Introduction The deployment of Artemisinin-based combination therapies and
transmission control measures led to a decrease in the global malaria burden over the …

Ca2+ signals critical for egress and gametogenesis in malaria parasites depend on a multipass membrane protein that interacts with PKG

AC Balestra, K Koussis, N Klages, SA Howell… - Science …, 2021 - science.org
Calcium signaling regulated by the cGMP-dependent protein kinase (PKG) controls key life
cycle transitions in the malaria parasite. However, how calcium is mobilized from …

Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities

LB Arendse, S Wyllie, K Chibale… - ACS Infectious …, 2021 - ACS Publications
Protein and phosphoinositide kinases have been successfully exploited as drug targets in
various disease areas, principally in oncology. In malaria, several protein kinases are under …

Epistasis studies reveal redundancy among calcium-dependent protein kinases in motility and invasion of malaria parasites

H Fang, AR Gomes, N Klages, P Pino, B Maco… - Nature …, 2018 - nature.com
In malaria parasites, evolution of parasitism has been linked to functional optimisation.
Despite this optimisation, most members of a calcium-dependent protein kinase (CDPK) …

High-throughput screening of the Plasmodium falciparum cGMP-dependent protein kinase identified a thiazole scaffold which kills erythrocytic and sexual stage …

M Penzo, L de Las Heras-Dueña, L Mata-Cantero… - Scientific reports, 2019 - nature.com
Antimalarial drug resistance compels the quest for new compounds that target alternative
pathways to current drugs. The Plasmodium cyclic GMP-dependent protein kinase (PKG) …

Chemo‐proteomics in antimalarial target identification and engagement

BL Bailey, W Nguyen, AF Cowman… - Medicinal Research …, 2023 - Wiley Online Library
Humans have lived in tenuous battle with malaria over millennia. Today, while much of the
world is free of the disease, areas of South America, Asia, and Africa still wage this war with …

Chemical probes for understudied kinases: challenges and opportunities

RAM Serafim, JM Elkins, WJ Zuercher… - Journal of Medicinal …, 2021 - ACS Publications
Over 20 years after the approval of the first-in-class protein kinase inhibitor imatinib, the
biological function of a significant fraction of the human kinome remains poorly understood …

Imidazo [1, 2-b] pyridazine as privileged scaffold in medicinal chemistry: an extensive review

A Garrido, G Vera, PO Delaye… - European Journal of …, 2021 - Elsevier
Abstract Imidazo [1, 2-b] pyridazine scaffold represents an important class of heterocyclic
nucleus which provides various bioactives molecules. Among them, the successful kinase …

Plasmodial kinase inhibitors: license to cure?

DG Cabrera, A Horatscheck, CR Wilson… - Journal of Medicinal …, 2018 - ACS Publications
Advances in the genetics, function, and stage-specificity of Plasmodium kinases has driven
robust efforts to identify targets for the design of antimalarial therapies. Reverse genomics …