Development of a continuous assay for high throughput screening to identify inhibitors of the purine salvage pathway in Plasmodium falciparum

Grube, Christopher D.; Gill, Cameron P.; Roy, Hervé

doi:10.1016/j.slasd.2021.12.002

Cited by 3 publications

(1 citation statement)

References 63 publications

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“…Results revealed identification of five compounds with inhibitory efficacy against all investigated enzymes. The investigators validated this approach to be effectively utilized for development of novel drugs with inhibitory activity against multiple targets [32] .…”

Section: Drug Targets In Plasmodium Sppmentioning

confidence: 99%

Recent advances in identification of potential drug targets and development of novel drugs in parasitic diseases. Part IV. Plasmodium spp.

Abaza

2022

Parasitologists United Journal

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In the last two decades, transporters attracted much attention in identification of potential drug targets against intracellular protozoa. Several membrane molecules exhibit essential roles in trafficking pathways for nutrients, essential enzymes and virulence factors. In this context, P. falciparum possesses a complex of genomic plasticity-encoding transporters with high potentiality for aneuploidy, and gene expression modulation in response to drug exposure. Therefore, it is able to undergo gene mutations in enzymes controlling drug uptake, and evade host immune response by antigenic variations as well. The genetic mechanism of antimalarial drug resistance arises early with monotherapy using fast-acting drugs or a single targeting drug. Accordingly, combined therapy acting on multiple targets would decrease the emergence of drug resistance. Evolutionary technology on genetic approach enabled researchers to identify and propose novel Plasmodium drug targets. The main objective of this part is to review potential drug targets for apicomplexans and discuss recent approaches in identifying Plasmodium targets, as well as advances in the design and development of novel antimalarial drugs.

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Section: Drug Targets In Plasmodium Sppmentioning

confidence: 99%