Research output per year
Research output per year
Search results
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2021
Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis
Thomas, M., Brand, S., De Rycker, M., Zuccotto, F., Lukac, I., Dodd, P., Ko, E.-J., Manthri, S., McGonagle, K., Osuna-Cabello, M., Riley, J., Pont, C., Simeons, F., Stojanovski, L., Thomas, J., Thompson, S., Viayna, E., Fiandor, J. M., Martín, J. & Wyatt, P. G. & 4 others, , 13 May 2021, In: Journal of Medicinal Chemistry. 64, 9, p. 5905-5930 26 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile33 Citations (Scopus)235 Downloads (Pure) -
2020
Discovery of an Allosteric Binding Site in Kinetoplastid Methionyl-tRNA Synthetase
Torrie, L. S., Robinson, D. A., Thomas, M. G., Hobrath, J. V., Shepherd, S. M., Post, J. M., Ko, E. J., Ferreira, R. A., Mackenzie, C. J., Wrobel, K., Edwards, D. P., Gilbert, I. H., Gray, D. W. (Lead / Corresponding author), Fairlamb, A. H. & De Rycker, M. (Lead / Corresponding author), 8 May 2020, In: ACS Infectious Diseases. 6, 5, p. 1044-1057 14 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile11 Citations (Scopus)143 Downloads (Pure) -
Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity
Thomas, M. (Lead / Corresponding author), De Rycker, M., Wall, R. J., Spinks, D., Epemolu, O., Manthri, S., Norval, S., Osuna-Cabello, M., Patterson, S., Riley, J., Simeons, F. R. C., Stojanovski, L., Thomas, J., Thompson, S., Naylor, C., Fiandor, J. M., Wyatt, P. G., Marco, M., Wyllie, S. & Read, K. D. & 2 others, , 10 Sept 2020, In: Journal of Medicinal Chemistry. 63, 17, p. 9523-9539 17 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile8 Citations (Scopus)273 Downloads (Pure) -
Identification of 6-amino-1H-pyrazolo[3,4-d]pyrimidines with in vivo efficacy against visceral leishmaniasis
Thomas, M. G., De Rycker, M., Ajakane, M., Crouch, S. D., Campbell, L., Daugan, A., Fra, G., Guerrero, C., Mackenzie, C. J., MacLean, L., Manthri, S., Martin, F., Norval, S., Osuna-Cabello, M., Riley, J., Shishikura, Y., Miguel-Siles, J., Simeons, F. R. C., Stojanovski, L. & Thomas, J. & 7 others, , 21 Oct 2020, In: RSC Medicinal Chemistry. 11, 10, p. 1168-1177 10 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile3 Citations (Scopus)100 Downloads (Pure) -
The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani: ACS Infectious Diseases
Wall, R. J., Carvalho, S., Milne, R., Bueren-Calabuig, J. A., Moniz, S., Cantizani-Perez, J., MacLean, L., Kessler, A., Cotillo, I., Sastry, L., Manthri, S., Patterson, S., Zuccotto, F., Thompson, S., Martin, J., Marco, M., Miles, T. J., De Rycker, M., Thomas, M. G. & Fairlamb, A. H. & 2 others, , 13 Mar 2020, In: ACS Infectious Diseases. 6, 3, p. 515-528 14 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile25 Citations (Scopus)206 Downloads (Pure) -
2019
Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase
Torrie, L., Zuccotto, F., Robinson, D., Gray, D., Gilbert, I. (Lead / Corresponding author) & De Rycker, M. (Lead / Corresponding author), 31 May 2019, In: PLoS ONE. 14, 5, p. 1-16 16 p., e0217828.Research output: Contribution to journal › Article › peer-review
Open AccessFile4 Citations (Scopus)169 Downloads (Pure) -
Pharmacological validation of N-myristoyltransferase as a drug target in Leishmania donovani
Corpas Lopez, V., Moniz, S., Thomas, M., Wall, R., Torrie, L., Zander-Dinse, D., Tinti, M., Brand, S., Stojanovski, L., Manthri, S., Hallyburton, I., Zuccotto, F., Wyatt, P., De Rycker, M., Horn, D., Ferguson, M., Clos, J., Read, K., Fairlamb, A. & Gilbert, I. (Lead / Corresponding author) & 1 others, , 11 Jan 2019, In: ACS Infectious Diseases. 5, 1, p. 111-122 12 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile58 Citations (Scopus)353 Downloads (Pure) -
Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition
Wyllie, S., Brand, S., Thomas, M., De Rycker, M., Chung, C.-W., Peña, I., Bingham, R., Bueren-Calabuig, J., Cantizani, J., Cebrian, D., Craggs, P. D., Ferguson, L., Goswami, P., Hobrath, J., Howe, J., Jeacock, L., Ko, E. J., Korczynska, J., MacLean, L. & Manthri, S. & 29 others, , 7 May 2019, In: Proceedings of the National Academy of Sciences. 116, 19, p. 9318-9323 6 p., 201820175.Research output: Contribution to journal › Article › peer-review
Open AccessFile130 Citations (Scopus)276 Downloads (Pure) -
2018
2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas’ disease
Thomas, M. G., De Rycker, M., Cotillo Torrejon, I., Thomas, J., Riley, J., Spinks, D., Read, K. D., Miles, T. J., Gilbert, I. H. & Wyatt, P. G. (Lead / Corresponding author), 1 Oct 2018, In: Bioorganic & Medicinal Chemistry Letters. 28, 18, p. 3025-3030 6 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile5 Citations (Scopus)140 Downloads (Pure) -
Anti-trypanosomal 8-hydroxyl naphthyridines are chelators of divalent transition metals
Wall, R. J., Moniz, S., Thomas, M., Norval, S., Ko, E. J., Marco, M., Miles, T. J., Gilbert, I., Horn, D., Fairlamb, A. & Wyllie, S. (Lead / Corresponding author), Aug 2018, In: Antimicrobial Agents and Chemotherapy. 62, 8, p. 1-15 15 p., e00235-18.Research output: Contribution to journal › Article › peer-review
Open AccessFile15 Citations (Scopus)240 Downloads (Pure) -
Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis
Wyllie, S., Thomas, M., Patterson, S., Crouch, S., De Rycker, M., Lowe, R., Gresham, S., Urbaniak, M. D., Otto, T. D., Stojanovski, L., Simeons, F. R. C., Manthri, S., MacLean, L. M., Zuccotto, F., Homeyer, N., Pflaumer, H., Boesche, M., Sastry, L., Connolly, P. & Albrecht, S. & 12 others, , 9 Aug 2018, In: Nature. 560, 7717, p. 192-197 6 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile119 Citations (Scopus)890 Downloads (Pure) -
2017
Chemical Validation of Methionyl tRNA Synthetase (MetRS) as a Druggable Target in Leishmania donovani
Torrie, L., Brand, S., Robinson, D., Ko, E. J., Stojanovski, L., Simeons, F. R. C., Wyllie, S., Thomas, J., Ellis, L., Osuna-Cabello, M., Epemolu, R., Nuehs, A., Riley, J., MacLean, L., Manthri, S., Read, K., Gilbert, I. (Lead / Corresponding author), Fairlamb, A. & De Rycker, M. (Lead / Corresponding author), Oct 2017, In: ACS Infectious Diseases. 3, 10, p. 718-727 10 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile21 Citations (Scopus)246 Downloads (Pure) -
Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi
Brand, S., Ko, E. J., Viayna, E., Thompson, S., Spinks, D., Thomas, M., Sandberg, L., Francisco, A. F., Jayawardhana, S., Smith, V. C., Jansen, C., De Rycker, M., Thomas, J., MacLean, L., Osuna-Cabello, M., Riley, J., Scullion, P., Stojanovski, L., Simeons, F. R. C. & Epemolu, O. & 16 others, , 14 Sept 2017, In: Journal of Medicinal Chemistry. 60, 17, p. 7284-7299 16 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile43 Citations (Scopus)305 Downloads (Pure) -
2016
The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis
Patterson, S., Wyllie, S., Norval, S., Stojanovski, L., Simeons, F. R. C., Auer, J. L., Osuna-Cabello, M., Read, K. D. & Fairlamb, A. H. (Lead / Corresponding author), 24 May 2016, In: eLife. 5, p. 1-21 21 p., e09744.Research output: Contribution to journal › Article › peer-review
Open AccessFile67 Citations (Scopus)280 Downloads (Pure) -
The N-myristoylome of Trypanosoma cruzi
Roberts, A. J. & Fairlamb, A. (Lead / Corresponding author), 5 Aug 2016, In: Scientific Reports. 6, p. 1-11 11 p., 31078.Research output: Contribution to journal › Article › peer-review
Open AccessFile19 Citations (Scopus)220 Downloads (Pure) -
2015
Development of a fluorescence-based Trypanosoma cruzi CYP51 inhibition assay for effective compound triaging in drug discovery programmes for Chagas disease
Riley, J., Brand, S., Voice, M., Caballero, I., Calvo, D. & Read, K. D. (Lead / Corresponding author), 22 Sept 2015, In: PLoS Neglected Tropical Diseases. 9, 9, 12 p., e0004014.Research output: Contribution to journal › Article › peer-review
42 Citations (Scopus) -
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., Nov 2015, In: ChemMedChem. 10, 11, p. 1821-1836 16 p.Research output: Contribution to journal › Article › peer-review
20 Citations (Scopus) -
Discovery of indoline-2-carboxamide derivatives as a new class of brain-penetrant inhibitors of Trypanosoma brucei
Cleghorn, L. A. T., Albrecht, S., Stojanovski, L., Simeons, F. R. J., 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. (Lead / Corresponding author), 8 Oct 2015, In: Journal of Medicinal Chemistry. 58, 19, p. 7695-7706 12 p.Research output: Contribution to journal › Article › peer-review
29 Citations (Scopus) -
Discovery of inhibitors of Trypanosoma brucei by phenotypic screening of a focused protein kinase library
Woodland, A., Thompson, S., Cleghorn, L. A. T., 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. (Lead / Corresponding author), Nov 2015, In: ChemMedChem. 10, 11, p. 1809-1820 12 p.Research output: Contribution to journal › Article › peer-review
14 Citations (Scopus) -
Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase
Robinson, D. A. & Wyatt, P. G. (Lead / Corresponding author), May 2015, In: Acta Crystallographica Section F: Structural Biology Communications. 71, 5, p. 586-593 8 p.Research output: Contribution to journal › Article › peer-review
3 Citations (Scopus) -
New compound sets identified from high throughput phenotypic screening against three kinetoplastid parasites: an open resource
Peña, I., Pilar Manzano, M., Cantizani, J., Kessler, A., Alonso-Padilla, J., Bardera, A. I., Alvarez, E., Colmenarejo, G., Cotillo, I., Roquero, I., de Dios-Anton, F., Barroso, V., Rodriguez, A., Gray, D. W., Navarro, M., Kumar, V., Sherstnev, A., Drewry, D. H., Brown, J. R. & Fiandor, J. M. & 1 others, , 2015, In: Scientific Reports. 5, 12 p., 8771.Research output: Contribution to journal › Article › peer-review
Open AccessFile216 Citations (Scopus)379 Downloads (Pure) -
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. A., Torrie, L. S., Ruda, G. F., Wyatt, P. G., Gilbert, I. H. & van Aalten, D. M. F. (Lead / Corresponding author), 19 Jun 2015, In: ACS Chemical Biology. 10, 6, p. 1425-1434 10 p.Research output: Contribution to journal › Article › peer-review
Open Access40 Citations (Scopus) -
2014
Biochemical and genetic characterization of Trypanosoma cruzi N-myristoyltransferase
Roberts, A. J., Torrie, L. S., Wyllie, S. & Fairlamb, A. H. (Lead / Corresponding author), 15 Apr 2014, In: Biochemical Journal. 459, 2, p. 323-332 10 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile27 Citations (Scopus)189 Downloads (Pure) -
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
Brand, S., Norcross, N. R., Thompson, S., Harrison, J. R., Smith, V. C., Robinson, D. A., Torrie, L. S., McElroy, S. P., Hallyburton, I., Norval, S., Scullion, P., Stojanovski, L., Simeons, F. R. C., Van Aalten, D., Frearson, J. A., Brenk, R., Fairlamb, A. H., Ferguson, M. A. J., Wyatt, P. G. & Gilbert, I. H. & 1 others, , 11 Dec 2014, In: Journal of Medicinal Chemistry. 57, 23, p. 9855-9869 15 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile62 Citations (Scopus)179 Downloads (Pure) -
Nitro drugs for the treatment of trypanosomatid diseases: past, present, and future prospects
Patterson, S. (Lead / Corresponding author) & Wyllie, S. (Lead / Corresponding author), 2014, In: Trends in Parasitology. 30, 6, p. 289-298 10 p.Research output: Contribution to journal › Article › peer-review
Open AccessFile268 Citations (Scopus)245 Downloads (Pure) -
2013
The R Enantiomer of the Antitubercular Drug PA-824 as a Potential Oral Treatment for Visceral Leishmaniasis
Patterson, S., Wyllie, S., Stojanovski, L., Perry, M. R., Simeons, F. R. C., Norval, S., Osuna-Cabello, M., De Rycker, M., Read, K. D. (Lead / Corresponding author) & Fairlamb, A. H. (Lead / Corresponding author), Oct 2013, In: Antimicrobial Agents and Chemotherapy. 57, 10, p. 4699-4706 8 p.Research output: Contribution to journal › Article › peer-review
57 Citations (Scopus)