ArticleAntimicrobial agents and chemotherapy2013
A class of tricyclic compounds blocking malaria parasite oocyst development and transmission.
Article in Antimicrobial agents and chemotherapy, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed, 35 citations in OpenAlex.
- Article
- A Plasmodium falciparum RING Finger E3 Ubiquitin Ligase Modifies the Roles of PfMDR1 and PfCRT in Parasite Drug Responses.Antimicrobial agents and chemotherapy · 2023Article
- ASGDB: a specialised genomic resource for interpreting Anopheles sinensis insecticide resistance.Parasites & vectors · 2018Article
- Efficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities.ACS combinatorial science · 2017Article
- Novel lead structures with both Plasmodium falciparum gametocytocidal and asexual blood stage activity identified from high throughput compound screening.Malaria journal · 2017Article
- Survey on synergism effect of ketotifen in combination with pyrimethamine in treatment of acute murine toxoplasmosis.Tropical medicine and health · 2017Article
- Human dihydrofolate reductase influences the sensitivity of the malaria parasite Plasmodium falciparum to ketotifen - A cautionary tale in screening transgenic parasites.International journal for parasitology. Drugs and drug resistance · 2016Article
- Monitoring the Prevalence of Leucocytozoon sabrazesi in Southern China and Testing Tricyclic Compounds against Gametocytes.PloS one · 2016Article
- Review
- Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning.PloS one · 2015Article
- Genomic Analysis of Detoxification Supergene Families in the Mosquito Anopheles sinensis.PloS one · 2015Article
- Development of potent and selective Plasmodium falciparum calcium-dependent protein kinase 4 (PfCDPK4) inhibitors that block the transmission of malaria to mosquitoes.European journal of medicinal chemistry · 2014Article
- Genome sequence of Anopheles sinensis provides insight into genetics basis of mosquito competence for malaria parasites.BMC genomics · 2014Article
- Article
- Article
- Gametocytocidal screen identifies novel chemical classes with Plasmodium falciparum transmission blocking activity.PloS one · 2014Article
- Antimalarial drug discovery - approaches and progress towards new medicines.Nature reviews. Microbiology · 2013Review
- A systems framework for vaccine design.Current opinion in immunology · 2013Review
- Recent advances in malaria drug discovery.Bioorganic & medicinal chemistry letters · 2013Review
- Malaria biology and disease pathogenesis: insights for new treatments.Nature medicine · 2013Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
17 authors at 2 institutions in 2 countries.
Funding
Abstract
Malaria is a deadly infectious disease in many tropical and subtropical countries. Previous efforts to eradicate malaria have failed, largely due to the emergence of drug-resistant parasites, insecticide-resistant mosquitoes and, in particular, the lack of drugs or vaccines to block parasite transmission. ATP-binding cassette (ABC) transporters are known to play a role in drug transport, metabolism, and resistance in many organisms, including malaria parasites. To investigate whether a Plasmodium falciparum ABC transporter (Pf14_0244 or PfABCG2) modulates parasite susceptibility to chemical compounds or plays a role in drug resistance, we disrupted the gene encoding PfABCG2, screened the recombinant and the wild-type 3D7 parasites against a library containing 2,816 drugs approved for human or animal use, and identified an antihistamine (ketotifen) that became less active against the PfABCG2-disrupted parasite in culture. In addition to some activity against asexual stages and gametocytes, ketotifen was highly potent in blocking oocyst development of P. falciparum and the rodent parasite Plasmodium yoelii in mosquitoes. Tests of structurally related tricyclic compounds identified additional compounds with similar activities in inhibiting transmission. Additionally, ketotifen appeared to have some activity against relapse of Plasmodium cynomolgi infection in rhesus monkeys. Further clinical evaluation of ketotifen and related compounds, including synthetic new derivatives, in blocking malaria transmission may provide new weapons for the current effort of malaria eradication.
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Registered trials
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.