Cargando…

Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library

A screen of a focused kinase inhibitor library against Trypanosoma brucei rhodesiense led to the identification of seven series, totaling 121 compounds, which showed >50 % inhibition at 5 μm. Screening of these hits in a T. b. brucei proliferation assay highlighted three compounds with a 1H-imida...

Descripción completa

Detalles Bibliográficos
Autores principales:	Woodland, Andrew, Thompson, Stephen, Cleghorn, Laura A T, Norcross, Neil, De Rycker, Manu, Grimaldi, Raffaella, Hallyburton, Irene, Rao, Bhavya, Norval, Suzanne, Stojanovski, Laste, Brun, Reto, Kaiser, Marcel, Frearson, Julie A, Gray, David W, Wyatt, Paul G, Read, Kevin D, Gilbert, Ian H
Formato:	Online Artículo Texto
Lenguaje:	English
Publicado:	Blackwell Publishing Ltd 2015
Materias:	Full Papers
Acceso en línea:	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4648050/ https://www.ncbi.nlm.nih.gov/pubmed/26381210 http://dx.doi.org/10.1002/cmdc.201500300

Ejemplares similares

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei
por: Cleghorn, Laura A. T., et al.
Publicado: (2015)

Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488
por: Smith, Victoria C, et al.
Publicado: (2011)

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode
por: Spinks, Daniel, et al.
Publicado: (2015)

From On-Target to Off-Target Activity: Identification and Optimisation of Trypanosoma brucei GSK3 Inhibitors and Their Characterisation as Anti-Trypanosoma brucei Drug Discovery Lead Molecules
por: Woodland, Andrew, et al.
Publicado: (2013)

Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma bruceiN-Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis
por: Brand, Stephen, et al.
Publicado: (2014)

Nuclear DBF-2-related Kinases Are Essential Regulators of Cytokinesis in Bloodstream Stage Trypanosoma brucei
por: Ma, Jiangtao, et al.
Publicado: (2010)

Chemical Proteomic Analysis Reveals the Drugability of the Kinome of Trypanosoma brucei
por: Urbaniak, Michael D., et al.
Publicado: (2012)

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase
por: Torrie, Leah S., et al.
Publicado: (2019)

Development of a 2,4-Diaminothiazole Series for the Treatment of Human African Trypanosomiasis Highlights the Importance of Static–Cidal Screening of Analogues
por: Cleghorn, Laura A. T., et al.
Publicado: (2023)

The Design and Synthesis of Potent and Selective Inhibitors of Trypanosoma brucei Glycogen Synthase Kinase 3 for the Treatment of Human African Trypanosomiasis
por: Urich, Robert, et al.
Publicado: (2014)

Investigation of Trypanothione Reductase as a Drug Target in Trypanosoma brucei
por: Spinks, Daniel, et al.
Publicado: (2009)

Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis
por: Jones, Deuan C., et al.
Publicado: (2010)

Screening a protein kinase inhibitor library against Plasmodium falciparum
por: Hallyburton, Irene, et al.
Publicado: (2017)

Design, Synthesis and Biological Evaluation of Trypanosoma brucei Trypanothione Synthetase Inhibitors
por: Spinks, Daniel, et al.
Publicado: (2012)

A Static-Cidal Assay for Trypanosoma brucei to Aid Hit Prioritisation for Progression into Drug Discovery Programmes
por: De Rycker, Manu, et al.
Publicado: (2012)

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors
por: Brand, Stephen, et al.
Publicado: (2011)

Steroid Alkaloids from Holarrhena africana with Strong Activity against Trypanosoma brucei rhodesiense
por: Nnadi, Charles Okeke, et al.
Publicado: (2017)

The R Enantiomer of the Antitubercular Drug PA-824 as a Potential Oral Treatment for Visceral Leishmaniasis
por: Patterson, Stephen, et al.
Publicado: (2013)

Bottlenecks and the Maintenance of Minor Genotypes during the Life Cycle of Trypanosoma brucei
por: Oberle, Michael, et al.
Publicado: (2010)

In Silico Identification and in Vitro Activity of Novel Natural Inhibitors of Trypanosoma brucei Glyceraldehyde-3-phosphate-dehydrogenase †
por: Herrmann, Fabian C., et al.
Publicado: (2015)

Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1
por: Spinks, Daniel, et al.
Publicado: (2011)

Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
por: Baragaña, Beatriz, et al.
Publicado: (2016)

Survival of Trypanosoma brucei in the Tsetse Fly Is Enhanced by the Expression of Specific Forms of Procyclin
por: Ruepp, Stefan, et al.
Publicado: (1997)

Exploring the Trypanosoma brucei Hsp83 Potential as a Target for Structure Guided Drug Design
por: Pizarro, Juan Carlos, et al.
Publicado: (2013)

Aquaporin 2 Mutations in Trypanosoma brucei gambiense Field Isolates Correlate with Decreased Susceptibility to Pentamidine and Melarsoprol
por: Graf, Fabrice E., et al.
Publicado: (2013)

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors
por: Harrison, Justin R., et al.
Publicado: (2018)

Isothermal Microcalorimetry, a New Tool to Monitor Drug Action against Trypanosoma brucei and Plasmodium falciparum
por: Wenzler, Tanja, et al.
Publicado: (2012)

SUMOylation in Trypanosoma brucei
por: Klein, Cornelia Andrea, et al.
Publicado: (2013)

Trypanosoma evansi is alike to Trypanosoma brucei brucei in the subcellular localisation of glycolytic enzymes
por: Moreno, S Andrea, et al.
Publicado: (2015)

Major Surface Glycoproteins of Insect Forms of Trypanosoma brucei Are Not Essential for Cyclical Transmission by Tsetse
por: Vassella, Erik, et al.
Publicado: (2009)

Evaluation of In Vitro Activity of Essential Oils against Trypanosoma brucei brucei and Trypanosoma evansi
por: Habila, Nathan, et al.
Publicado: (2010)

C-Terminal Mutants of Apolipoprotein L-I Efficiently Kill Both Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense
por: Lecordier, Laurence, et al.
Publicado: (2009)

De Novo Genome Assembly Shows Genome Wide Similarity between Trypanosoma brucei brucei and Trypanosoma brucei rhodesiense
por: Sistrom, Mark, et al.
Publicado: (2016)

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography
por: Patterson, Stephen, et al.
Publicado: (2011)

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors
por: Bayliss, Tracy, et al.
Publicado: (2017)

Golgi duplication in Trypanosoma brucei
por: He, Cynthia Y., et al.
Publicado: (2004)

Phylogeography and Taxonomy of Trypanosoma brucei
por: Balmer, Oliver, et al.
Publicado: (2011)

The nuclear proteome of Trypanosoma brucei
por: Goos, Carina, et al.
Publicado: (2017)

Signatures of hybridization in Trypanosoma brucei
por: Kay, Christopher, et al.
Publicado: (2022)

Route of inoculation influences Trypanosoma congolense and Trypanosoma brucei brucei virulence in Swiss white mice
por: Ndungu, Kariuki, et al.
Publicado: (2019)

Cannot write session to /tmp/vufind_sessions/sess_4d9jv2096nhuqo7iiiiv8dbht5