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Updated: Aug 13, 2026
14:57
Spectrophotometric Screening for Potential Inhibitors of Cytosolic Glutathione S-Transferases
Published on: October 10, 2020
Glutathione S-transferase from malarial parasites: structural and functional aspects
1Interdisciplinary Research Center, Giessen University, Germany.
Methods in Enzymology
|January 10, 2006
Summary
Malaria drug resistance is rising, prompting research into Plasmodium falciparum
Area of Science:
- Malariology
- Parasitology
- Biochemistry
Background:
- Malaria is an emerging disease due to drug resistance and expanding geographic distribution of Plasmodium falciparum.
- The Plasmodium genome sequencing revealed a single glutathione S-transferase (PfGST), a potential drug resistance factor.
- PfGST is implicated in the metabolism of antimalarial drugs like chloroquine and methylene blue.
Purpose of the Study:
- To investigate the structure, function, and potential as a drug target of Plasmodium falciparum glutathione S-transferase (PfGST).
- To understand PfGST's role in antimalarial drug resistance.
- To explore PfGST as a target for novel antimalarial drug development.
Main Methods:
- Studied PfGST in parasite extracts and as a recombinant protein.
- Determined the x-ray structure of PfGST.
- Compared PfGST structure and function to known glutathione S-transferase classes and human GSTs.
Main Results:
- PfGST is a homodimeric enzyme not belonging to known GST classes.
- PfGST exhibits significant structural differences from human GSTs, particularly at the H-site.
- Inhibition of PfGST is predicted to disrupt multiple parasite metabolic pathways.
Conclusions:
- PfGST is a unique enzyme with potential as a novel antimalarial drug target.
- Targeting PfGST may overcome existing drug resistance mechanisms.
- Further research into PfGST inhibition could lead to new therapeutic strategies against malaria.
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