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CYP51 as drug targets for fungi and protozoan parasites: past, present and future

Parasitology, 2018-12, Vol.145 (14), p.1820-1836

2018

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

Current topics in medicinal chemistry, 2011-08, Vol.11 (16), p.2060

2011

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A requirement for an active proton delivery network supports a compound I-mediated C–C bond cleavage in CYP51 catalysis

The Journal of biological chemistry, 2020-07, Vol.295 (29), p.9998-10007

2020

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Unravelling the role of transient redox partner complexes in P450 electron transfer mechanics

Scientific reports, 2022-09, Vol.12 (1), p.16232-16232, Article 16232

2022

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Rational Modification of a Candidate Cancer Drug for Use Against Chagas Disease

Journal of medicinal chemistry, 2009-03, Vol.52 (6), p.1639-1647

2009

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In Vitro and In Vivo Studies of the Antiparasitic Activity of Sterol 14α-Demethylase (CYP51) Inhibitor VNI against Drug-Resistant Strains of Trypanosoma cruzi

Antimicrobial Agents and Chemotherapy, 2013-09, Vol.57 (9), p.4151-4163

2013

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Sterol 14α-demethylase mutation leads to amphotericin B resistance in Leishmania mexicana

PLoS neglected tropical diseases, 2017-06, Vol.11 (6), p.e0005649-e0005649

2017

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The First Virally Encoded Cytochrome P450

Journal of Virology, 2009-08, Vol.83 (16), p.8266-8269

2009

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Novel sterol metabolic network of Trypanosoma brucei procyclic and bloodstream forms

Biochemical journal, 2012-04, Vol.443 (1), p.267-277

2012

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

Antimicrobial Agents and Chemotherapy, 2012-09, Vol.56 (9), p.4914-4921

2012

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CYP51: A Major Drug Target in the Cytochrome P450 Superfamily

Lipids, 2008-12, Vol.43 (12), p.1117-1125

2008

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Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis

The Journal of biological chemistry, 2017-04, Vol.292 (16), p.6728-6743

2017

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Structure-Functional Characterization of Cytochrome P450 Sterol 14α-Demethylase (CYP51B) from Aspergillus fumigatus and Molecular Basis for the Development of Antifungal Drugs

The Journal of biological chemistry, 2015-09, Vol.290 (39), p.23916-23934

2015

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Human sterol 14α-demethylase as a target for anticancer chemotherapy: towards structure-aided drug design1

Journal of lipid research, 2016-08, Vol.57 (8), p.1552-1563

2016

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The Clinically Approved Antifungal Drug Posaconazole Inhibits Human Cytomegalovirus Replication

Antimicrobial agents and chemotherapy, 2020-09, Vol.64 (10)

2020

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Oxygen‐18 Labeling Reveals a Mixed Fe−O Mechanism in the Last Step of Cytochrome P450 51 Sterol 14α‐Demethylation

Angewandte Chemie International Edition, 2024-02, Vol.63 (9), p.e202317711-n/a

International ed. in English, 2024

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The antifungal drug isavuconazole inhibits the replication of human cytomegalovirus (HCMV) and acts synergistically with anti-HCMV drugs

Antiviral research, 2021-05, Vol.189, p.105062-105062, Article 105062

2021

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Structural basis for conservation in the CYP51 family

Biochimica et biophysica acta, 2011-01, Vol.1814 (1), p.88-93

2011

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Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors

Journal of medicinal chemistry, 2019-11, Vol.62 (22), p.10391-10401

2019

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Processive kinetics in the three-step lanosterol 14α-demethylation reaction catalyzed by human cytochrome P450 51A1

The Journal of biological chemistry, 2023-07, Vol.299 (7), p.104841-104841, Article 104841

2023

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Identification of Potent and Selective Inhibitors of Acanthamoeba: Structural Insights into Sterol 14α-Demethylase as a Key Drug Target

Journal of medicinal chemistry, 2024-05, Vol.67 (9), p.7443-7457

2024

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Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity

Antimicrobial agents and chemotherapy, 2017-07, Vol.61 (7)

2017

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Conservation in the CYP51 Family. Role of the B‘ Helix/BC Loop and Helices F and G in Enzymatic Function

Biochemistry (Easton), 2003-08, Vol.42 (30), p.9091-9101

2003

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Concerning P450 Evolution: Structural Analyses Support Bacterial Origin of Sterol 14α-Demethylases

Molecular biology and evolution, 2021-03, Vol.38 (3), p.952-967

2021

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Relaxed Substrate Requirements of Sterol 14α-Demethylase from Naegleria fowleri Are Accompanied by Resistance to Inhibition

Journal of medicinal chemistry, 2021-12, Vol.64 (23), p.17511-17522

2021

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CYP51 as drug targets for fungi and protozoan parasites: past, present and future

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

A requirement for an active proton delivery network supports a compound I-mediated C–C bond cleavage in CYP51 catalysis

Unravelling the role of transient redox partner complexes in P450 electron transfer mechanics

Rational Modification of a Candidate Cancer Drug for Use Against Chagas Disease

In Vitro and In Vivo Studies of the Antiparasitic Activity of Sterol 14α-Demethylase (CYP51) Inhibitor VNI against Drug-Resistant Strains of Trypanosoma cruzi

Sterol 14α-demethylase mutation leads to amphotericin B resistance in Leishmania mexicana

The First Virally Encoded Cytochrome P450

Novel sterol metabolic network of Trypanosoma brucei procyclic and bloodstream forms

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

CYP51: A Major Drug Target in the Cytochrome P450 Superfamily

Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol biosynthesis

Structure-Functional Characterization of Cytochrome P450 Sterol 14α-Demethylase (CYP51B) from Aspergillus fumigatus and Molecular Basis for the Development of Antifungal Drugs

Human sterol 14α-demethylase as a target for anticancer chemotherapy: towards structure-aided drug design1

The Clinically Approved Antifungal Drug Posaconazole Inhibits Human Cytomegalovirus Replication

Oxygen‐18 Labeling Reveals a Mixed Fe−O Mechanism in the Last Step of Cytochrome P450 51 Sterol 14α‐Demethylation

The antifungal drug isavuconazole inhibits the replication of human cytomegalovirus (HCMV) and acts synergistically with anti-HCMV drugs

Structural basis for conservation in the CYP51 family

Validation of Human Sterol 14α-Demethylase (CYP51) Druggability: Structure-Guided Design, Synthesis, and Evaluation of Stoichiometric, Functionally Irreversible Inhibitors

Processive kinetics in the three-step lanosterol 14α-demethylation reaction catalyzed by human cytochrome P450 51A1

Identification of Potent and Selective Inhibitors of Acanthamoeba: Structural Insights into Sterol 14α-Demethylase as a Key Drug Target

Crystal Structure of the New Investigational Drug Candidate VT-1598 in Complex with Aspergillus fumigatus Sterol 14α-Demethylase Provides Insights into Its Broad-Spectrum Antifungal Activity

Conservation in the CYP51 Family. Role of the B‘ Helix/BC Loop and Helices F and G in Enzymatic Function

Concerning P450 Evolution: Structural Analyses Support Bacterial Origin of Sterol 14α-Demethylases

Relaxed Substrate Requirements of Sterol 14α-Demethylase from Naegleria fowleri Are Accompanied by Resistance to Inhibition

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