ArticleChemMedChem2011
Identification of inhibitors of the Leishmania cdc2-related protein kinase CRK3.
Article in ChemMedChem, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Repurposing the Antibacterial Agents Peptide 19-4LF and Peptide 19-2.5 for Treatment of Cutaneous Leishmaniasis.Pharmaceutics · 2022Article
- Identification of Potential Kinase Inhibitors within the PI3K/AKT Pathway ofBiomolecules · 2021Article
- Review
- Review
- In vitro effectivity of three approved drugs and their synergistic interaction against Leishmania infantum.Biomedica : revista del Instituto Nacional de Salud · 2020Article
- Screening Marine Natural Products for New Drug Leads against Trypanosomatids and Malaria.Marine drugs · 2020Review
- Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase.PloS one · 2019Article
- Evaluation of Different Concentrations of Imatinib on the Viability ofAdvanced biomedical research · 2019Article
- Unveiling the Kinomes ofComputational and structural biotechnology journal · 2019Article
- Conditional gene deletion with DiCre demonstrates an essential role for CRK3 in Leishmania mexicana cell cycle regulation.Molecular microbiology · 2016Article
- Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library.ChemMedChem · 2015Article
- Using a non-image-based medium-throughput assay for screening compounds targeting N-myristoylation in intracellular Leishmania amastigotes.PLoS neglected tropical diseases · 2014Article
- Kinases as druggable targets in trypanosomatid protozoan parasites.Chemical reviews · 2014Review
- Recent developments in drug discovery for leishmaniasis and human African trypanosomiasis.Chemical reviews · 2014Review
- An inhibitor-driven study for enhancing the selectivity of indirubin derivatives towards leishmanial Glycogen Synthase Kinase-3 over leishmanial cdc2-related protein kinase 3.Parasites & vectors · 2014Article
- Target-based drug discovery for human African trypanosomiasis: selection of molecular target and chemical matter.Parasitology · 2014Review
- Article
- Locating sweet spots for screening hits and evaluating pan-assay interference filters from the performance analysis of two lead-like libraries.Journal of chemical information and modeling · 2013Article
- Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei.ACS chemical biology · 2012Article
Corrections and comments
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Authors and funding
13 authors.
Funding
Abstract
New drugs are urgently needed for the treatment of tropical parasitic diseases such as leishmaniasis and human African trypanosomiasis (HAT). This work involved a high-throughput screen of a focussed kinase set of ~3400 compounds to identify potent and parasite-selective inhibitors of an enzymatic Leishmania CRK3-cyclin 6 complex. The aim of this study is to provide chemical validation that Leishmania CRK3-CYC6 is a drug target. Eight hit series were identified, of which four were followed up. The optimisation of these series using classical SAR studies afforded low-nanomolar CRK3 inhibitors with significant selectivity over the closely related human cyclin dependent kinase CDK2.
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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.