Papers 2015

Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei. Cleghorn, L. A.; Albrecht, S.; Stojanovski, L.; Simeons, F. R.; Norval, S.; Kime, R.; Collie, I. T.; De Rycker, M.; Campbell, L.; Hallyburton, I.; Frearson, J. A.; Wyatt, P. G.; Read, K. D.; Gilbert, I. H. J Med Chem. 2015, 58, 7695-7706. PMCID: PMC4601051

Discovery and optimisation studies of antimalarial phenotypic hits. Mital, A.; Murugesan, D.; Kaiser, M.; Yeates, C.; Gilbert, I. H. Eur J. Med. Chem. 2015, 103, 530-538.

Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode. Spinks, D.; Smith, V.; Thompson, S.; Robinson, D. A.; Luksch, T.; Smith, A.; Torrie, L. S.; McElroy, S.; Stojanovski, L.; Norval, S.; Collie, I. T.; Hallyburton, I.; Rao, B.; Brand, S.; Brenk, R.; Frearson, J. A.; Read, K. D.; Wyatt, P. G.; Gilbert, I. H. ChemMedChem. 2015, 10, 1821-1836. PMCID: PMC4648043

Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library. Woodland, A.; Thompson, S.; Cleghorn, L. A.; Norcross, N.; De Rycker, M.; Grimaldi, R.; Hallyburton, I.; Rao, B.; Norval, S.; Stojanovski, L.; Brun, R.; Kaiser, M.; Frearson, J. A.; Gray, D. W.; Wyatt, P. G.; Read, K. D.; Gilbert, I. H. ChemMedChem. 2015, 10, 1809-1820. PMCID: PMC4648050

A novel multiple-stage antimalarial agent that inhibits protein synthesis. Baragaña, B.; Hallyburton, I.; Lee, M. C.; Norcross, N. R.; Grimaldi, R.; Otto, T. D.; Proto, W. R.; Blagborough, A. M.; Meister, S.; Wirjanata, G.; Ruecker, A.; Upton, L. M.; Abraham, T. S.; Almeida, M. J.; Pradhan, A.; Porzelle, A.; Martínez, M. S.; Bolscher, J. M.; Woodland, A.; Norval, S.; Zuccotto, F.; Thomas, J.; Simeons, F.; Stojanovski, L.; Osuna-Cabello, M.; Brock, P. M.; Churcher, T. S.; Sala, K. A.; Zakutansky, S. E.; Jiménez-Díaz, M. B.; Sanz, L. M.; Riley, J.; Basak, R.; Campbell, M.; Avery, V. M.; Sauerwein, R. W.; Dechering, K. J.; Noviyanti, R.; Campo, B.; Frearson, J. A.; Angulo-Barturen, I.; Ferrer-Bazaga, S.; Gamo, F. J.; Wyatt, P. G.; Leroy, D.; Siegl, P.; Delves, M. J.; Kyle, D. E.; Wittlin, S.; Marfurt, J.; Price, R. N.; Sinden, R. E.; Winzeler, E. A.; Charman, S. A.; Bebrevska, L.; Gray, D. W.; Campbell, S.; Fairlamb, A. H.; Willis, P. A.; Rayner, J. C.; Fidock, D. A.; Read, K. D.; Gilbert, I.H. Nature, 2015, 522, 315-320. PMCID: PMC4700930

Application of a novel regulatable Cre recombinase system to define the role of liver and gut metabolism in drug oral bioavailability. Henderson, C. J.; McLaughlin, L. A.; Osuna-Caello, M.; Taylor, M.; Gilbert, I. H.; McLaren, A. W.; Wolf, C. R. Biochem. J., 2015, 465, 479-488.

Application of RNAi to genomic drug target validation in schistosomes. Guidi, A.; Mansour, N. R.; Paveley, R.; Carruthers, I. M.; Besnard, J.; Hopkins, A. L.; Gilbert, I. H.; Quentin D. Bickle, Q. D. PLoS Negl. Trop. Dis., 2015, 9, e0003801.

N-Myristoyltransferase is a cell wall target in Aspergillus fumigatus. Fang, W.; Robinson, D. A.; Raimi, O. G.; Blair, D. E.; Harrison, J. R.; Lockhart, D. E.; Torrie, L. S.; Ruda, G. F.; Wyatt, P. G.; Gilbert, I. H.; van Aalten, D. ACS Chem. Biol., 2015, 10, 1425-1434.