Martin J. McPhillie
University of Leeds
DruggabilityBinding sitePhenotypeReductaseTransporterNucleoside-diphosphate kinaseMolecular biologyVirologySmall moleculeNanotechnologyEnzymeChemistryGenomicsIn vivoIn silicoToxoplasmosisToxoplasma gondiiPlasmodium falciparumDrugOrnithine aminotransferaseTriclosanStructure basedProtein structureAntibioticsThe RenaissanceGeneticsBiochemistryBioinformaticsComputational biologyMedicineDrug discoveryNAD+ kinasePolymeraseBiologyPhosphoglycerate mutaseAntibiotic resistanceCRISPRPharmacology
Publications 25
#1Kyle Orritt (University of Leeds)
#2Anthony Maxwell (Norwich Research Park)H-Index: 68
Last. Martin J. McPhillie (University of Leeds)H-Index: 7
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#1Kyle Orritt (University of Leeds)
#2Juliette Newell (University of Leeds)
Last. Colin W. G. Fishwick (University of Leeds)H-Index: 33
view all 9 authors...
By 2050 it is predicted that antimicrobial resistance will be responsible for 10 million global deaths annually, costing the world economy $100 trillion. Clearly, strategies to address this problem are required as bacterial evolution is rendering our current antibiotics ineffective. The discovery of an allosteric binding site on the established antibacterial target DNA gyrase offers a new medicinal chemistry strategy, as this site is distinct from the fluoroquinolone-DNA site binding site. Using...
#1Ana Pavić (LBU: Leeds Beckett University)H-Index: 1
#2Yurui JiH-Index: 5
Last. Vincent L. G. PostisH-Index: 12
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ABSTRACT Characterizing the mycobacterial transporters involved in the uptake and/or catabolism of host-derived nutrients required by mycobacteria may identify novel drug targets against tuberculosis. Here, we identify and characterize a member of the amino acid-polyamine-organocation superfamily, a potential γ-aminobutyric acid (GABA) transport protein, GabP, from Mycobacterium smegmatis. The protein was expressed to a level allowing its purification to homogeneity, and size exclusion chromatog...
#1Andrew N. BoaH-Index: 18
#1Jacqueline Farinha Shimizu (UNESP: Sao Paulo State University)H-Index: 6
#2Daniel Oliveira Silva Martins (UNESP: Sao Paulo State University)H-Index: 2
Last. Ana Carolina Gomes Jardim (UNESP: Sao Paulo State University)H-Index: 12
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Chikungunya virus (CHIKV) is a mosquito-transmitted virus of special concern as it causes Chikungunya fever, characterized by an acute febrile illness, rash, and arthralgia that can progress to chronic and debilitating arthritic symptoms. The effects of climate change on the geographic distribution of the mosquito vector has the potential to expose more of the globe to this virus. No antiviral agents or vaccines are currently available against CHIKV infection and the development of novel therapi...
8 CitationsSource
#1Martin J. McPhillie (University of Leeds)H-Index: 7
#2Ying Zhou (U of C: University of Chicago)H-Index: 13
Last. Rima McLeod (U of C: University of Chicago)H-Index: 66
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Apicomplexan infections cause substantial morbidity and mortality, worldwide. New, improved therapies are needed. Herein, we create a next generation anti-apicomplexan lead compound, JAG21, a tetrahydroquinolone, with increased sp3-character to improve parasite selectivity. Relative to other cytochrome b inhibitors, JAG21 has improved solubility and ADMET properties, without need for pro-drug. JAG21 significantly reduces Toxoplasma gondii tachyzoites and encysted bradyzoites in vitro, and in pri...
2 CitationsSource
#1Martin J. McPhillie (University of Leeds)H-Index: 7
#2Ying Zhou (U of C: University of Chicago)H-Index: 13
Last. Rima McLeod (U of C: University of Chicago)H-Index: 66
view all 39 authors...
#1Arundhasa Chandrabalan (Hull York Medical School)H-Index: 1
#2Martin J. McPhillie (University of Leeds)H-Index: 7
Last. Laura R. Sadofsky (Hull York Medical School)H-Index: 12
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The transient receptor potential ankyrin 1 (TRPA1) channel is a non-selective cation channel, which detects noxious stimuli leading to pain, itch and cough. However, the mechanism(s) of channel modulation by many of the known, non-reactive modulators has not been fully elucidated. N-cinnamoylanthranilic acid derivatives (CADs) contain structural elements from the TRPA1 modulators cinnamaldehyde and flufenamic acid, so it was hypothesized that specific modulators could be found amongst them and m...
7 CitationsSource
#1Kamal El Bissati (U of C: University of Chicago)H-Index: 20
#2Henry Redel (Albert Einstein College of Medicine)H-Index: 1
Last. Louis M. Weiss (Albert Einstein College of Medicine)H-Index: 84
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Twenty-two compounds belonging to several classes of polyamine analogs have been examined for their ability to inhibit the growth of the human malaria parasite Plasmodium falciparum in vitro and in vivo. Four lead compounds from the thiourea sub-series and one compound from the urea-based analogs were found to be potent inhibitors of both chloroquine-resistant (Dd2) and chloroquine-sensitive (3D7) strains of Plasmodium with IC₅₀ values ranging from 150 to 460 nM. In addition, the compound RHW, N...
7 CitationsSource
#1Rachel M. Johnson (University of Leeds)H-Index: 7
#2Shaun Rawson (University of Leeds)H-Index: 14
Last. Stephen P. Muench (University of Leeds)H-Index: 27
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Parasitic diseases are a huge burden on human health causing significant morbidity and mortality. However, parasitic structure based drug discovery programmes have been hindered by a lack of high resolution structural information from parasitic derived proteins and have largely relied upon homology models from mammalian systems. The recent renaissance in electron microscopy (EM) has caused a dramatic rise in the number of structures being determined at high resolution and subsequently enabled it...