ArticleACS chemical biology2012
Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.
Article in ACS chemical biology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 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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Who cites it
28 citing papers in PubMed, 56 citations in OpenAlex.
- Cyclin-dependent kinase-inhibitor screening and structural analysis identify a CDK-like kinase candidate in Naegleria fowleri.Parasites & vectors · 2026Article
- Potent kinase inhibitors from the Merck KGaA OGHL: Novel hits against Trypanosoma brucei with potential for repurposing.PLoS neglected tropical diseases · 2025Article
- Discovery of effectors for casein kinase signaling in the African trypanosome.Scientific reports · 2025Article
- Genome-scale RNA interference profiling of Trypanosoma brucei cell cycle progression defects.Nature communications · 2022Article
- Structure, function and druggability of the African trypanosome flagellum.Journal of cellular physiology · 2022Review
- Partially Purified Leaf Fractions of Azadirachta indica Inhibit Trypanosome Alternative Oxidase and Exert Antitrypanosomal Effects on Trypanosoma congolense.Acta parasitologica · 2022Article
- Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead forJournal of medicinal chemistry · 2020Article
- Organising the cell cycle in the absence of transcriptional control: Dynamic phosphorylation co-ordinates the Trypanosoma brucei cell cycle post-transcriptionally.PLoS pathogens · 2019Article
- Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells.Scientific reports · 2019Article
- Review
- Who Needs a Contractile Actomyosin Ring? The Plethora of Alternative Ways to Divide a Protozoan Parasite.Frontiers in cellular and infection microbiology · 2019Review
- Kinome chemoproteomics characterization of pyrrolo[3,4-c]pyrazoles as potent and selective inhibitors of glycogen synthase kinase 3.Molecular omics · 2018Article
- A paradigm shift: The mitoproteomes of procyclic and bloodstream Trypanosoma brucei are comparably complex.PLoS pathogens · 2017Review
- RNAi screening identifies Trypanosoma brucei stress response protein kinases required for survival in the mouse.Scientific reports · 2017Article
- Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need.Nature reviews. Microbiology · 2017Review
- Characterisation of Casein Kinase 1.1 inBioMed research international · 2017Article
- Identification of "Preferred" Human Kinase Inhibitors for Sleeping Sickness Lead Discovery. Are Some Kinases Better than Others for Inhibitor Repurposing?ACS infectious diseases · 2016Article
- Conversion of a Single Polypharmacological Agent into Selective Bivalent Inhibitors of Intracellular Kinase Activity.ACS chemical biology · 2016Article
- New compound sets identified from high throughput phenotypic screening against three kinetoplastid parasites: an open resource.Scientific reports · 2015Article
- Kinases as druggable targets in trypanosomatid protozoan parasites.Chemical reviews · 2014Review
Corrections and comments
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Authors and funding
10 authors at 1 institution in 1 country.
Funding
Abstract
The protozoan parasite Trypanosoma brucei is the causative agent of African sleeping sickness, and there is an urgent unmet need for improved treatments. Parasite protein kinases are attractive drug targets, provided that the host and parasite kinomes are sufficiently divergent to allow specific inhibition to be achieved. Current drug discovery efforts are hampered by the fact that comprehensive assay panels for parasite targets have not yet been developed. Here, we employ a kinase-focused chemoproteomics strategy that enables the simultaneous profiling of kinase inhibitor potencies against more than 50 endogenously expressed T. brucei kinases in parasite cell extracts. The data reveal that T. brucei kinases are sensitive to typical kinase inhibitors with nanomolar potency and demonstrate the potential for the development of species-specific inhibitors.
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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.