Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria.

doi:10.1073/pnas.87.8.3018

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Back to search

Article

Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria.

Proceedings of the National Academy of Sciences of the United States of America - 1 Apr 1990

Peterson D S, Milhous W K, Wellems T E

Abstract excerpt

Proguanil and pyrimethamine are antifolate drugs with distinct chemical structures that are used commonly in the prophylaxis and treatment of Plasmodium falciparum malaria. Clinical reports and field studies have suggested that some parasites refractory to proguanil can be treated with pyrimethamine, and vice versa. Analysis of the P. falciparum dihydrofolate reductase (DHFR) from different parasites reveals the...

Topics

Amino Acid Sequence
Animals
Binding Sites
DNA
Drug Resistance
Humans
Malaria
Models, Structural
Molecular Structure
Mutation
Plasmodium falciparum

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Proguanil

Protein Conformation

Pyrimethamine

Structure-Activity Relationship

Tetrahydrofolate Dehydrogenase

Triazines

Source

Open in PubMed Open full text

Identifiers

PMID: 2183222
DOI: 10.1073/pnas.87.8.3018
PMCID: PMC53825

Genes

DHFR

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 29 Aug 2026. Prepared record publication-2183222-2026-08-29.1. Manifest publication-graph-cohort-2026-08-29.1.

Source receipt: PubMed via Helena Literature Corpus, retrieved 29 Aug 2026.

Community interpretation

Discuss the evidence

Ask a question, add context or challenge an interpretation. Community activity is separate from scientific evidence strength.

discussions

replies

Citations encouraged

Claims remain attributable.

No discussion yet

Be the first to add a careful, cited interpretation.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Molecular basis of differential resistance to cycloguanil and pyrimethamine in Plasmodium falciparum malaria.PMID 2183222Read ↗

Cycloguanil and its parent compound proguanil demonstrate distinct activities against Plasmodium falciparum malaria parasites transformed with human dihydrofolate reductase.Semantic proximity Read ↗

Point Mutations in the Dihydrofolate Reductase and Dihydropteroate Synthetase Genes and in Vitro Susceptibility to Pyrimethamine and Cycloguanil of Plasmodium falciparum Isolates from Papua New GuineaSemantic proximity Read ↗

Antifolate-resistant mutants of <i>Plasmodium falciparum</i> dihydrofolate reductaseSemantic proximity Read ↗

Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.Semantic proximity Read ↗

Novel alleles of Plasmodium falciparum dhfr that confer resistance to chlorcycloguanil.Semantic proximity Read ↗

Resistance to antifolates in Plasmodium falciparum, the causative agent of tropical malaria.Semantic proximity Read ↗

Malaria antifolate resistance with contrasting Plasmodium falciparum dihydrofolate reductase (DHFR) polymorphisms in humans and Anopheles mosquitoes.Semantic proximity Read ↗

Molecular epidemiology of malaria in Yaounde, Cameroon. VI. Sequence variations in the Plasmodium falciparum dihydrofolate reductase-thymidylate synthase gene and in vitro resistance to pyrimethamine and cycloguanil.Semantic proximity Read ↗

Prevalence of the dihydrofolate reductase Asn-108 mutation as the basis for pyrimethamine-resistant falciparum malaria in the Brazilian Amazon.Semantic proximity Read ↗

Combined spatial limitation around residues 16 and 108 of Plasmodium falciparum dihydrofolate reductase explains resistance to cycloguanil.Semantic proximity Read ↗

Stereospecific Resistance to N2-Acyl Tetrahydro-β-carboline Antimalarials Is Mediated by a PfMDR1 Mutation That Confers Collateral Drug SensitivitySemantic proximity Read ↗

Malarial dihydrofolate reductase as a paradigm for drug development against a resistance-compromised targetSemantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.