ReviewCellular and molecular life sciences : CMLS2012
Know your enemy: understanding the role of PfCRT in drug resistance could lead to new antimalarial tactics.
Review in Cellular and molecular life sciences : CMLS, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Who cites it
49 citing papers in PubMed.
- Gain-of-function PfAAT1 mutations compensate for impaired PfCRT function inResearch square · 2026Article
- Changing genetic profiles ofAntimicrobial agents and chemotherapy · 2026Article
- Molecular basis of the functional conflict between chloroquine and peptide transport in the Malaria parasite chloroquine resistance transporter PfCRT.Nature communications · 2025Article
- Computational elucidation ofIn silico pharmacology · 2025Article
- Design, synthesis and mechanistic exploration of anti-plasmodial Indolo[2,3-Future medicinal chemistry · 2024Article
- PfCRT mutations conferring piperaquine resistance in falciparum malaria shape the kinetics of quinoline drug binding and transport.PLoS pathogens · 2023Article
- The Knock-Down of the Chloroquine Resistance Transporter PfCRT Is Linked to Oligopeptide Handling in Plasmodium falciparum.Microbiology spectrum · 2022Article
- Mechanistic basis for multidrug resistance and collateral drug sensitivity conferred to the malaria parasite by polymorphisms in PfMDR1 and PfCRT.PLoS biology · 2022Article
- Heme Detoxification in the Malaria Parasite: A Target for Antimalarial Drug Development.Accounts of chemical research · 2021Review
- Amide Tethered 4-Aminoquinoline-naphthalimide Hybrids: A New Class of Possible Dual Function Antiplasmodials.ACS medicinal chemistry letters · 2020Article
- Synthesis and biological evaluation of novel quinoline-piperidine scaffolds as antiplasmodium agents.European journal of medicinal chemistry · 2020Article
- From Metabolite to Metabolome: Metabolomics Applications inFrontiers in microbiology · 2020Review
- Emergence of Plasmodium vivax Resistance to Chloroquine in French Guiana.Antimicrobial agents and chemotherapy · 2019Article
- The genomic architecture of antimalarial drug resistance.Briefings in functional genomics · 2019Review
- Plasmodium vivax chloroquine resistance links to pvcrt transcription in a genetic cross.Nature communications · 2019Article
- Phosphomimetic substitution at Ser-33 of the chloroquine resistance transporter PfCRT reconstitutes drug responses inThe Journal of biological chemistry · 2019Article
- Elucidating Mechanisms of Drug-Resistant Plasmodium falciparum.Cell host & microbe · 2019Review
- Iron is a substrate of theThe Journal of biological chemistry · 2017Article
- Article
- Unexpected selections of Plasmodium falciparum polymorphisms in previously treatment-naïve areas after monthly presumptive administration of three different anti-malarial drugs in Liberia 1976-78.Malaria journal · 2017Article
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The prevention and treatment of malaria is heavily dependent on antimalarial drugs. However, beginning with the emergence of chloroquine (CQ)-resistant Plasmodium falciparum parasites 50 years ago, efforts to control the disease have been thwarted by failed or failing drugs. Mutations in the parasite's 'chloroquine resistance transporter' (PfCRT) are the primary cause of CQ resistance. Furthermore, changes in PfCRT (and in several other transport proteins) are associated with decreases or increases in the parasite's susceptibility to a number of other antimalarial drugs. Here, we review recent advances in our understanding of CQ resistance and discuss these in the broader context of the parasite's susceptibilities to other quinolines and related drugs. We suggest that PfCRT can be viewed both as a 'multidrug-resistance carrier' and as a drug target, and that the quinoline-resistance mechanism is a potential 'Achilles' heel' of the parasite. We examine a number of the antimalarial strategies currently undergoing development that are designed to exploit the resistance mechanism, including relatively simple measures, such as alternative CQ dosages, as well as new drugs that either circumvent the resistance mechanism or target it directly.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.