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Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R)‑1-((S)‑2-(1-Cyanocyclopropanecarboxamido)-3,3-dimethylbutanoyl)-4-hydroxy‑N‑(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide (VH298)

Journal of medicinal chemistry, 2018-01, Vol.61 (2), p.599-618

2018

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Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

Nature communications, 2016-11, Vol.7 (1), p.13312-13312, Article 13312

2016

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Activation of Bicyclic Nitro-drugs by a Novel Nitroreductase (NTR2) in Leishmania

PLoS pathogens, 2016-11, Vol.12 (11), p.e1005971-e1005971

2016

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Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

Scientific reports, 2016-10, Vol.6 (1), p.35351, Article 35351

2016

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Development of a Fluorescence-based Trypanosoma cruzi CYP51 Inhibition Assay for Effective Compound Triaging in Drug Discovery Programmes for Chagas Disease

PLoS neglected tropical diseases, 2015-09, Vol.9 (9), p.e0004014-e0004014

2015

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Sperm Toolbox-A selection of small molecules to study human spermatozoa

PloS one, 2024-02, Vol.19 (2), p.e0297666-e0297666

2024

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Targeting N-myristoylation for therapy of B-cell lymphomas

Nature communications, 2020-10, Vol.11 (1), p.5348-5348, Article 5348

2020

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A Systematic Study of the In Vitro Pharmacokinetics and Estimated Human In Vivo Clearance of Indole and Indazole-3-Carboxamide Synthetic Cannabinoid Receptor Agonists Detected on the Illicit Drug Market

Molecules (Basel, Switzerland), 2021-03, Vol.26 (5), p.1396

2021

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Target validation: linking target and chemical properties to desired product profile

Current topics in medicinal chemistry, 2011-05, Vol.11 (10), p.1275

2011

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Veterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs

PLoS pathogens, 2020-11, Vol.16 (11), p.e1008932-e1008932

2020

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The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis

eLife, 2016-05, Vol.5

2016

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Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

Antimicrobial Agents and Chemotherapy, 2010-07, Vol.54 (7), p.2893-2900

2010

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Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

Journal of medicinal chemistry, 2016-11, Vol.59 (21), p.9686-9720

2016

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The R Enantiomer of the Antitubercular Drug PA-824 as a Potential Oral Treatment for Visceral Leishmaniasis

Antimicrobial Agents and Chemotherapy, 2013-10, Vol.57 (10), p.4699-4706

2013

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Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles

PLoS pathogens, 2018-02, Vol.14 (2), p.e1006850

2018

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Anti-trypanosomatid drug discovery: progress and challenges

Nature reviews. Microbiology, 2023-01, Vol.21 (1), p.35-50

2023

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Receptor occupancy and brain free fraction

Drug metabolism and disposition, 2009-04, Vol.37 (4), p.753

2009

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Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo

PloS one, 2012-05, Vol.7 (5), p.e37097

2012

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Combining PET Biodistribution and Equilibrium Dialysis Assays to Assess the Free Brain Concentration and BBB Transport of CNS Drugs

Journal of cerebral blood flow and metabolism, 2012-05, Vol.32 (5), p.874-883

2012

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Temporal and Wash-Out Studies Identify Medicines for Malaria Venture Pathogen Box Compounds with Fast-Acting Activity against Both Trypanosoma cruzi and Trypanosoma brucei

Microorganisms (Basel), 2022-06, Vol.10 (7), p.1287

2022

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Loss of CRMP2 O-GlcNAcylation leads to reduced novel object recognition performance in mice

Open biology, 2019-11, Vol.9 (11), p.190192-190192

2019

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Chemical synthesis, characterisation and in vitro and in vivo metabolism of the synthetic opioid MT-45 and its newly identified fluorinated analogue 2F-MT-45 with metabolite confirmation in urine samples from known drug users

Forensic toxicology, 2018, Vol.36 (2), p.359-374

2018

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Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

Nature reviews. Microbiology, 2017-04, Vol.15 (4), p.217-231

2017

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Potent and selective chemical probe of hypoxic signalling downstream of HIF-α hydroxylation via VHL inhibition

Activation of Bicyclic Nitro-drugs by a Novel Nitroreductase (NTR2) in Leishmania

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

Development of a Fluorescence-based Trypanosoma cruzi CYP51 Inhibition Assay for Effective Compound Triaging in Drug Discovery Programmes for Chagas Disease

Sperm Toolbox-A selection of small molecules to study human spermatozoa

Targeting N-myristoylation for therapy of B-cell lymphomas

A Systematic Study of the In Vitro Pharmacokinetics and Estimated Human In Vivo Clearance of Indole and Indazole-3-Carboxamide Synthetic Cannabinoid Receptor Agonists Detected on the Illicit Drug Market

Target validation: linking target and chemical properties to desired product profile

N -myristoyltransferase inhibitors as new leads to treat sleeping sickness

Veterinary trypanocidal benzoxaboroles are peptidase-activated prodrugs

The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis

Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

The R Enantiomer of the Antitubercular Drug PA-824 as a Potential Oral Treatment for Visceral Leishmaniasis

Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles

Anti-trypanosomatid drug discovery: progress and challenges

Receptor occupancy and brain free fraction

Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo

Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N‑Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis

Combining PET Biodistribution and Equilibrium Dialysis Assays to Assess the Free Brain Concentration and BBB Transport of CNS Drugs

Temporal and Wash-Out Studies Identify Medicines for Malaria Venture Pathogen Box Compounds with Fast-Acting Activity against Both Trypanosoma cruzi and Trypanosoma brucei

Loss of CRMP2 O-GlcNAcylation leads to reduced novel object recognition performance in mice

Chemical synthesis, characterisation and in vitro and in vivo metabolism of the synthetic opioid MT-45 and its newly identified fluorinated analogue 2F-MT-45 with metabolite confirmation in urine samples from known drug users

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

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