ArticleChembiochem : a European journal of chemical biology2014
Chemical interrogation of the malaria kinome.
Article in Chembiochem : a European journal of chemical biology, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 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.
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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
19 citing papers in PubMed, 39 citations in OpenAlex.
- Screening the Global Health Priority Box against Plasmodium berghei liver stage parasites using an inexpensive luciferase detection protocol.Malaria journal · 2024Article
- Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.Journal of medicinal chemistry · 2024Article
- Human Polo-like Kinase Inhibitors as Antiplasmodials.ACS infectious diseases · 2023Article
- Random Forest Model Predictions Afford Dual-Stage Antimalarial Agents.ACS infectious diseases · 2022Article
- Functional analysis of theiScience · 2022Article
- Plasmodium vivax Liver and Blood Stages Recruit the Druggable Host Membrane Channel Aquaporin-3.Cell chemical biology · 2020Article
- Overcoming Fungal Echinocandin Resistance through Inhibition of the Non-essential Stress Kinase Yck2.Cell chemical biology · 2020Article
- Antimalarial Drug Resistance and Novel Targets for Antimalarial Drug Discovery.Infection and drug resistance · 2020Review
- Potent bicyclic inhibitors of malarial cGMP-dependent protein kinase: approaches to combining improvements in cell potency, selectivity and structural novelty.Bioorganic & medicinal chemistry letters · 2019Article
- Plasmodium pseudo-Tyrosine Kinase-like binds PP1 and SERA5 and is exported to host erythrocytes.Scientific reports · 2019Article
- Plasmodium PK9 Inhibitors Promote Growth of Liver-Stage Parasites.Cell chemical biology · 2019Article
- Potent inhibitors of malarial P. Falciparum protein kinase G: Improving the cell activity of a series of imidazopyridines.Bioorganic & medicinal chemistry letters · 2019Article
- In silico Screening and Evaluation of Plasmodium falciparum Protein Kinase 5 (PK5) Inhibitors.ChemMedChem · 2018Article
- Plasmodium parasite exploits host aquaporin-3 during liver stage malaria infection.PLoS pathogens · 2018Article
- Kinase inhibitors: the road ahead.Nature reviews. Drug discovery · 2018Review
- Identification of Hsp90 Inhibitors with Anti-Plasmodium Activity.Antimicrobial agents and chemotherapy · 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
- Progress towards a public chemogenomic set for protein kinases and a call for contributions.PloS one · 2017Article
- Current therapies and future possibilities for drug development against liver-stage malaria.The Journal of clinical investigation · 2016Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
13 authors at 4 institutions in 2 countries.
Funding
Abstract
Malaria, an infectious disease caused by eukaryotic parasites of the genus Plasmodium, afflicts hundreds of millions of people every year. Both the parasite and its host utilize protein kinases to regulate essential cellular processes. Bioinformatic analyses of parasite genomes predict at least 65 protein kinases, but their biological functions and therapeutic potential are largely unknown. We profiled 1358 small-molecule kinase inhibitors to evaluate the role of both the human and the malaria kinomes in Plasmodium infection of liver cells, the parasites' obligatory but transient developmental stage that precedes the symptomatic blood stage. The screen identified several small molecules that inhibit parasite load in liver cells, some with nanomolar efficacy, and each compound was subsequently assessed for activity against blood-stage malaria. Most of the screening hits inhibited both liver- and blood-stage malaria parasites, which have dissimilar gene expression profiles and infect different host cells. Evaluation of existing kinase activity profiling data for the library members suggests that several kinases are essential to malaria parasites, including cyclin-dependent kinases (CDKs), glycogen synthase kinases, and phosphoinositide-3-kinases. CDK inhibitors were found to bind to Plasmodium protein kinase 5, but it is likely that these compounds target multiple parasite kinases. The dual-stage inhibition of the identified kinase inhibitors makes them useful chemical probes and promising starting points for antimalarial development.
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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.