Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth - sprookjes - yvandenbroek - TriplyDB

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

http://www.wikidata.org/entity/Q27676649

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Complexes of Trypanosoma cruzi Sterol 14 -Demethylase (CYP51) with Two Pyridine-based Drug Candidates for Chagas Disease: STRUCTURAL BASIS FOR PATHOGEN SELECTIVITY Rational Development of 4-Aminopyridyl-Based Inhibitors Targeting Trypanosoma cruzi CYP51 as Anti-Chagas Agents Expanding the Binding Envelope of CYP51 Inhibitors TargetingTrypanosoma cruziwith 4-Aminopyridyl-Based Sulfonamide Derivatives R -Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi Structural Basis for Rational Design of Inhibitors Targeting Trypanosoma cruzi Sterol 14α-Demethylase: Two Regions of the Enzyme Molecule Potentiate Its Inhibition The Potential of Secondary Metabolites from Plants as Drugs or Leads against Protozoan Neglected Diseases-Part III: In-Silico Molecular Docking Investigations High throughput screening for anti-Trypanosoma cruzi drug discovery Machine Learning Models and Pathway Genome Data Base for Trypanosoma cruzi Drug Discovery Utilizing Chemical Genomics to Identify Cytochrome b as a Novel Drug Target for Chagas Disease Development of a Fluorescence-based Trypanosoma cruzi CYP51 Inhibition Assay for Effective Compound Triaging in Drug Discovery Programmes for Chagas Disease New compound sets identified from high throughput phenotypic screening against three kinetoplastid parasites: an open resource.Drug strategies targeting CYP51 in neglected tropical diseases Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.Dynamics of CYP51: implications for function and inhibitor design.Interactions of antiparasitic sterols with sterol 14α-demethylase (CYP51) of human pathogens Structure-Functional Characterization of Cytochrome P450 Sterol 14α-Demethylase (CYP51B) from Aspergillus fumigatus and Molecular Basis for the Development of Antifungal Drugs.Ligand tunnels in T. brucei and human CYP51: Insights for parasite-specific drug design.Nitrotriazole-based acetamides and propanamides with broad spectrum antitrypanosomal activity.Design or screening of drugs for the treatment of Chagas disease: what shows the most promise?Two analogues of fenarimol show curative activity in an experimental model of Chagas disease.Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis.Antitrypanosomal activity of 5-nitro-2-aminothiazole-based compounds.Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents Nitrotriazole-Based Compounds as Antichagasic Agents in a Long-Treatment In Vivo Assay.Repurposing of Human Kinase Inhibitors in Neglected Protozoan Diseases.Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi.Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease.Binding of anti-Trypanosoma natural products from African flora against selected drug targets: a docking study

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P2860

Antitrypanosomal Lead Discovery: Identification of a Ligand-Efficient Inhibitor of Trypanosoma cruzi CYP51 and Parasite Growth

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2013 nî lūn-bûn

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2013 թուականի Մարտին հրատարակուած գիտական յօդուած

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2013 թվականի մարտին հրատարակված գիտական հոդված

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2013年の論文

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Cristin E Juda

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Galina I Lepesheva

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Gilles Courtemanche

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Grasiella Andriani

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Jodianne T Wood

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William Devine

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Zeke Clements

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P2860

Crystal structures of Trypanosoma brucei sterol 14alpha-demethylase and implications for selective treatment of human infections

Structural Insights into Inhibition of Sterol 14 -Demethylase in the Human Pathogen Trypanosoma cruzi

Substrate Preferences and Catalytic Parameters Determined by Structural Characteristics of Sterol 14α-Demethylase (CYP51) from Leishmania infantum

Pharmacological Characterization, Structural Studies, and In Vivo Activities of Anti-Chagas Disease Lead Compounds Derived from Tipifarnib

Identification of three classes of heteroaromatic compounds with activity against intracellular Trypanosoma cruzi by chemical library screening

Activity in vivo of anti-Trypanosoma cruzi compounds selected from a high throughput screening

Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51

Sterol 14alpha-demethylase (CYP51) as a therapeutic target for human trypanosomiasis and leishmaniasis

Ligand efficiency: a useful metric for lead selection

Successful treatment with posaconazole of a patient with chronic Chagas disease and systemic lupus erythematosus.

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Zdzislaw Wawrzak

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