ArticlePloS one2015
A New Set of Chemical Starting Points with Plasmodium falciparum Transmission-Blocking Potential for Antimalarial Drug Discovery.
Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.
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Who cites it
40 citing papers in PubMed.
- Identification of novel compounds with prophylactic activity against hypnozoites using aAntimicrobial agents and chemotherapy · 2025Article
- An all-in-one pipeline for the in vitro discovery and in vivo testing of Plasmodium falciparum malaria transmission blocking drugs.Nature communications · 2025Article
- Quinazolinedione Derivatives as Potential Anticancer Agents Through Apoptosis Induction in MCF-7.International journal of molecular sciences · 2025Article
- Natural products as transmission-blocking agents against malaria: a comprehensive review of bioactive compounds and their therapeutic potential.Malaria journal · 2025Review
- Unravelling the mode of action of the Tres Cantos Antimalarial Set (TCAMS): investigating the mechanism of potent antimalarial compounds potentially targeting the human serotonin receptor.Malaria journal · 2025Article
- Simple supplementation of serum-free medium produces gametocytes of Plasmodium falciparum that transmit to mosquitoes.Malaria journal · 2024Article
- Transmission-Blocking Strategies for Malaria Eradication: Recent Advances in Small-Molecule Drug Development.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Machine Learning Approaches Identify Chemical Features for Stage-Specific Antimalarial Compounds.ACS omega · 2023Article
- Machine learning-based phenotypic imaging to characterise the targetable biology of Plasmodium falciparum male gametocytes for the development of transmission-blocking antimalarials.PLoS pathogens · 2023Article
- Isoliensinine from Cissampelos pariera rhizomes exhibits potential gametocytocidal and anti-malarial activities against Plasmodium falciparum clinical isolates.Malaria journal · 2023Article
- Safe drugs with high potential to block malaria transmission revealed by a spleen-mimetic screening.Nature communications · 2023Article
- Rational Design and Lead Optimisation of Potent Antimalarial Quinazolinediones and Their Cytotoxicity against MCF-7.Molecules (Basel, Switzerland) · 2023Article
- Random Forest Model Predictions Afford Dual-Stage Antimalarial Agents.ACS infectious diseases · 2022Article
- Gametocyte-specific and all-blood-stage transmission-blocking chemotypes discovered from high throughput screening on Plasmodium falciparum gametocytes.Communications biology · 2022Article
- Indole-Containing Pyrazino[2,1-ACS medicinal chemistry letters · 2022Article
- Streamlined and Robust Stage-Specific Profiling of Gametocytocidal Compounds AgainstFrontiers in cellular and infection microbiology · 2022Article
- Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway inJournal of medicinal chemistry · 2021Article
- Natural Products: A Potential Source of Malaria Transmission Blocking Drugs?Pharmaceuticals (Basel, Switzerland) · 2020Review
- Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials.ACS infectious diseases · 2020Article
- The antimalarial screening landscape-looking beyond the asexual blood stage.Current opinion in chemical biology · 2019Review
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The discovery of new antimalarials with transmission blocking activity remains a key issue in efforts to control malaria and eventually eradicate the disease. Recently, high-throughput screening (HTS) assays have been successfully applied to Plasmodium falciparum asexual stages to screen millions of compounds, with the identification of thousands of new active molecules, some of which are already in clinical phases. The same approach has now been applied to identify compounds that are active against P. falciparum gametocytes, the parasite stage responsible for transmission. This study reports screening results for the Tres Cantos Antimalarial Set (TCAMS), of approximately 13,533 molecules, against P. falciparum stage V gametocytes. Secondary confirmation and cytotoxicity assays led to the identification of 98 selective molecules with dual activity against gametocytes and asexual stages. Hit compounds were chemically clustered and analyzed for appropriate physicochemical properties. The TCAMS chemical space around the prioritized hits was also studied. A selection of hit compounds was assessed ex vivo in the standard membrane feeding assay and demonstrated complete block in transmission. As a result of this effort, new chemical structures not connected to previously described antimalarials have been identified. This new set of compounds may serve as starting points for future drug discovery programs as well as tool compounds for identifying new modes of action involved in malaria transmission.
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