Complexes of Trypanosoma cruzi Sterol 14 -Demethylase (CYP51) with Two Pyridine-based Drug Candidates for Chagas Disease: STRUCTURAL BASIS FOR PATHOGEN SELECTIVITY (Q27679983)

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English	Complexes of Trypanosoma cruzi Sterol 14 -Demethylase (CYP51) with Two Pyridine-based Drug Candidates for Chagas Disease: STRUCTURAL BASIS FOR PATHOGEN SELECTIVITY	scientific article

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scholarly article

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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 (English)

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Trypanosoma cruzi

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Zdzislaw Wawrzak

2

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author name string

Tatiana Y Hargrove

1

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Paul W Alexander

3

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Jason H Chaplin

4

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Martine Keenan

5

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Susan A Charman

6

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Catherine J Perez

7

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Michael R Waterman

8

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Eric Chatelain

9

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Galina I Lepesheva

10

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language of work or name

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publication date

1 November 2013

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Journal of Biological Chemistry

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288

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44

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31602-15

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Antifungal Azoles: Structural Insights into Undesired Tight Binding to Cholesterol-Metabolizing CYP46A1

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CYP51 structures and structure-based development of novel, pathogen-specific inhibitory scaffolds

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20 March 2017

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

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20 March 2017

VNI cures acute and chronic experimental Chagas disease

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20 March 2017

Organocatalytic, enantioselective synthesis of VNI: a robust therapeutic development platform for Chagas, a neglected tropical disease

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20 March 2017

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

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20 March 2017

Unusual Spectroscopic and Ligand Binding Properties of the Cytochrome P450-Flavodoxin Fusion Enzyme XplA

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20 March 2017

Structural complex of sterol 14 -demethylase (CYP51) with 14 -methylenecyclopropyl- 7-24, 25-dihydrolanosterol

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20 March 2017

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

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20 March 2017

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

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20 March 2017

Structural basis of human CYP51 inhibition by antifungal azoles

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20 March 2017

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

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20 March 2017

Features and development of Coot

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20 March 2017

The integration of macromolecular diffraction data

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20 March 2017

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20 March 2017

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20 March 2017

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

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20 March 2017

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7 April 2017

In vitro and in vivo studies of the antiparasitic activity of sterol 14α-demethylase (CYP51) inhibitor VNI against drug-resistant strains of Trypanosoma cruzi.

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29 September 2017

Analogues of fenarimol are potent inhibitors of Trypanosoma cruzi and are efficacious in a murine model of Chagas disease

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29 September 2017

Triazole antifungal agents drug-drug interactions involving hepatic cytochrome P450.

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29 September 2017

Targeting Trypanosoma cruzi sterol 14α-demethylase (CYP51)

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29 September 2017

Structural basis for conservation in the CYP51 family

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29 September 2017

Indomethacin amides as a novel molecular scaffold for targeting Trypanosoma cruzi sterol 14alpha-demethylase

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29 September 2017

CYP51: A major drug target in the cytochrome P450 superfamily

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29 September 2017

Mechanisms of resistance to antifungal agents: yeasts and filamentous fungi

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29 September 2017

Antimicrobial resistance: resistance to antifungal agents: mechanisms and clinical impact

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29 September 2017

Sterol 14alpha-demethylase as a potential target for antitrypanosomal therapy: enzyme inhibition and parasite cell growth

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29 September 2017

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29 September 2017

Sterol 14alpha-demethylase cytochrome P450 (CYP51), a P450 in all biological kingdoms

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29 September 2017

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29 September 2017

The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions

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29 September 2017

The protein farnesyltransferase inhibitor Tipifarnib as a new lead for the development of drugs against Chagas disease

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29 September 2017

CYP51--the omnipotent P450.

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29 September 2017

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29 September 2017

A class of sterol 14-demethylase inhibitors as anti-Trypanosoma cruzi agents.

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Antiproliferative synergism of the allylamine SF 86-327 and ketoconazole on epimastigotes and amastigotes of Trypanosoma (Schizotrypanum) cruzi

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29 September 2017

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Ergosterol biosynthesis and drug development for Chagas disease

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Chagas disease: pushing through the pipeline

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21 January 2018

CYP51 from Trypanosoma cruzi: a phyla-specific residue in the B' helix defines substrate preferences of sterol 14alpha-demethylase

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21 January 2018

CYP51 from Trypanosoma brucei is obtusifoliol-specific

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21 January 2018

Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.

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Conservation in the CYP51 family. Role of the B' helix/BC loop and helices F and G in enzymatic function

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Folding requirements are different between sterol 14alpha-demethylase (CYP51) from Mycobacterium tuberculosis and human or fungal orthologs

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Inhibition of cytochromes P450 by antifungal imidazole derivatives

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Effects of ketoconazole on sterol biosynthesis by Trypanosoma cruzi epimastigotes

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Biochemical and ultrastructural alterations produced by miconazole and econazole in Trypanosoma cruzi

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Mechanistic studies of lanosterol 14 alpha-methyl demethylase: substrate requirements for the component reactions catalyzed by a single cytochrome P-450 isozyme

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10.1074/JBC.M113.497990

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