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Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum

Proceedings of the National Academy of Sciences - PNAS, 2012-10, Vol.109 (41), p.16708-16713

2012

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Persistence and activation of malaria hypnozoites in long-term primary hepatocyte cultures

Nature Medicine, 2014-03, Vol.20 (3), p.307-312

2014

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Exonuclease-mediated degradation of nascent RNA silences genes linked to severe malaria

Nature (London), 2014-09, Vol.513 (7518), p.431-435

2014

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Structural Plasticity of Malaria Dihydroorotate Dehydrogenase Allows Selective Binding of Diverse Chemical Scaffolds

The Journal of biological chemistry, 2009-09, Vol.284 (39), p.26999-27009

2009

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Host cell entry by apicomplexa parasites requires actin polymerization in the host cell

Cell host & microbe, 2009-03, Vol.5 (3), p.259-272

2009

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Comprehensive histone phosphorylation analysis and identification of Pf14-3-3 protein as a histone H3 phosphorylation reader in malaria parasites

PloS one, 2013-01, Vol.8 (1), p.e53179-e53179

2013

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High-throughput Screening for Potent and Selective Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase

The Journal of biological chemistry, 2005-06, Vol.280 (23), p.21847-21853

2005

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Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-Stage Antimalarial Compounds

ChemMedChem, 2014-10, Vol.9 (10), p.2360-2373

2014

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Analysis of Flavin Oxidation and Electron-Transfer Inhibition in Plasmodium falciparum Dihydroorotate Dehydrogenase

Biochemistry (Easton), 2008-02, Vol.47 (8), p.2466-2475

2008

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Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies

Molecular microbiology, 2008-04, Vol.68 (1), p.37-50

2008

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Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitors with Potent and Selective Activity against the Malaria Parasite Plasmodium falciparum

Journal of medicinal chemistry, 2008-06, Vol.51 (12), p.3649-3653

2008

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Plasmodium falciparum PfSET7: enzymatic characterization and cellular localization of a novel protein methyltransferase in sporozoite, liver and erythrocytic stage parasites

Scientific reports, 2016-02, Vol.6 (1), p.21802, Article 21802

2016

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Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans

Antimicrobial agents and chemotherapy, 2015-02, Vol.59 (2), p.950-959

2015

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Original 2‑(3-Alkoxy‑1H‑pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

Journal of medicinal chemistry, 2015-07, Vol.58 (14), p.5579-5598

2015

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Detergent-dependent Kinetics of Truncated Plasmodium falciparumDihydroorotate Dehydrogenase

The Journal of biological chemistry, 2007-04, Vol.282 (17), p.12678-12686

2007

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Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti- Plasmodium activity

MedChemComm, 2017-05, Vol.8 (5), p.1069-1092

2017

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Detergent-dependent kinetics of truncated Plasmodium falciparum dihydroorotate dehydrogenase

The Journal of biological chemistry, 2007-04, Vol.282 (17), p.12678-12686

2007

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Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity

The Journal of biological chemistry, 2002-11, Vol.277 (44), p.41827-41834

2002

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Malarial Dihydroorotate Dehydrogenase

The Journal of biological chemistry, 2002-11, Vol.277 (44), p.41827-41834

2002

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Regulation of surface coat exchange by differentiating African trypanosomes

Molecular and biochemical parasitology, 2006-06, Vol.147 (2), p.211-223

2006

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NO‐induced relaxation of labouring and non‐labouring human myometrium is not mediated by cyclic GMP

British journal of pharmacology, 2001-09, Vol.134 (1), p.206-214

2001

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Dissociation of cGMP accumulation and relaxation in myometrial smooth muscle: effects of S-nitroso- N-acetylpenicillamine and 3-morpholinosyndonimine

Cellular signalling, 2003-08, Vol.15 (8), p.763-772

2003

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Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activityThe authors declare no competing interests.Electronic supplementary information (ESI) available: Supplementary Tables ST1-ST5, experimental data for the representative diaminoquinazoline analogues, 2D NMRs of 85 and 111a and X-ray structure of 111a (Fig. SF1). The coordinates for 111a have been deposited with CCDC 1503377. For ESI and crystallographic data in

2017-05

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Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti-Plasmodium activity† †The authors declare no competing interests. ‡ ‡Electronic supplementary information (ESI) available: Supplementary Tables ST1–ST5, experimental data for the representative diaminoquinazoline analogues, 2D NMRs of 85 and 111a and X-ray structure of 111a (Fig. SF1). The coordinates for 111a have been deposited with CCDC 1503377. For ESI and crystallographic

MedChemComm, 2017-03, Vol.8 (5), p.1069-1092

2017

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Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-stage Anti-Malarial Compounds

ChemMedChem, 2014-07, Vol.9 (10), p.2360-2373

2014

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Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum

Persistence and activation of malaria hypnozoites in long-term primary hepatocyte cultures

Exonuclease-mediated degradation of nascent RNA silences genes linked to severe malaria

Structural Plasticity of Malaria Dihydroorotate Dehydrogenase Allows Selective Binding of Diverse Chemical Scaffolds

Host cell entry by apicomplexa parasites requires actin polymerization in the host cell

Comprehensive histone phosphorylation analysis and identification of Pf14-3-3 protein as a histone H3 phosphorylation reader in malaria parasites

High-throughput Screening for Potent and Selective Inhibitors of Plasmodium falciparum Dihydroorotate Dehydrogenase

Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-Stage Antimalarial Compounds

Analysis of Flavin Oxidation and Electron-Transfer Inhibition in Plasmodium falciparum Dihydroorotate Dehydrogenase

Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies

Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitors with Potent and Selective Activity against the Malaria Parasite Plasmodium falciparum

Plasmodium falciparum PfSET7: enzymatic characterization and cellular localization of a novel protein methyltransferase in sporozoite, liver and erythrocytic stage parasites

Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans

Original 2‑(3-Alkoxy‑1H‑pyrazol-1-yl)azines Inhibitors of Human Dihydroorotate Dehydrogenase (DHODH)

Detergent-dependent Kinetics of Truncated Plasmodium falciparumDihydroorotate Dehydrogenase

Histone lysine methyltransferase structure activity relationships that allow for segregation of G9a inhibition and anti- Plasmodium activity

Detergent-dependent kinetics of truncated Plasmodium falciparum dihydroorotate dehydrogenase

Malarial dihydroorotate dehydrogenase. Substrate and inhibitor specificity

Malarial Dihydroorotate Dehydrogenase

Regulation of surface coat exchange by differentiating African trypanosomes

NO‐induced relaxation of labouring and non‐labouring human myometrium is not mediated by cyclic GMP

Dissociation of cGMP accumulation and relaxation in myometrial smooth muscle: effects of S-nitroso- N-acetylpenicillamine and 3-morpholinosyndonimine

Development of Diaminoquinazoline Histone Lysine Methyltransferase Inhibitors as Potent Blood-stage Anti-Malarial Compounds

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