Aref#d: 19815. Wellcome Trust Centre for Drug Discovery (Strategic Award)

2020

PDBE-KB: A community-driven resource for structural and functional annotations

PDBe-KB consortium, 8 Jan 2020, In: Nucleic Acids Research. 48, D1, p. D344-D353 10 p.

Research output: Contribution to journal › Article › peer-review

Open Access

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87 Citations (Scopus)

113 Downloads (Pure)

2017

Screening a protein kinase inhibitor library against Plasmodium falciparum

Hallyburton, I., Grimaldi, R., Woodland, A., Baragana, B., Luksch, T., Spinks, D., James, D., Leroy, D., Waterson, D., Fairlamb, A. H., Wyatt, P. G., Gilbert, I. H. (Lead / Corresponding author) & Frearson, J. A., 7 Nov 2017, In: Malaria Journal. 16, p. 1-11 11 p., 446.

Research output: Contribution to journal › Article › peer-review

Open Access

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15 Citations (Scopus)

384 Downloads (Pure)

2015

Discovery and optimisation studies of antimalarial phenotypic hits

Mital, A., Murugesan, D., Kaiser, M., Yeates, C. & Gilbert, I. H. (Lead / Corresponding author), 20 Oct 2015, In: European Journal of Medicinal Chemistry. 103, p. 530-538 9 p.

Research output: Contribution to journal › Article › peer-review

17 Citations (Scopus)

Homoserine and quorum-sensing acyl homoserine lactones as alternative sources of threonine: A potential role for homoserine kinase in insect-stage Trypanosoma brucei

Ong, H. B., Lee, W. S., Patterson, S., Wyllie, S. & Fairlamb, A. H., 1 Jan 2015, In: Molecular Microbiology. 95, 1, p. 143-156 14 p.

Research output: Contribution to journal › Article › peer-review

Open Access

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15 Citations (Scopus)

166 Downloads (Pure)

2013

Allosteric activation of trypanosomatid deoxyhypusine synthase by a catalytically dead paralog

Nguyen, S., Jones, D. C., Wyllie, S., Fairlamb, A. H. & Phillips, M. A., 24 May 2013, In: Journal of Biological Chemistry. 288, 21, p. 15256-15267 12 p.

Research output: Contribution to journal › Article › peer-review

Open Access

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43 Citations (Scopus)

136 Downloads (Pure)

A novel allosteric inhibitor of the uridine diphosphate N-acetylglucosamine pyrophosphorylase from Trypanosoma brucei

Urbaniak, M. D., Collie, I. T., Fang, W., Aristotelous, T., Eskilsson, S., Raimi, O. G., Harrison, J., Navratilova, I. H., Frearson, J. A., van Aalten, D. M. F. & Ferguson, M. A. J., 20 Sept 2013, In: ACS Chemical Biology. 8, 9, p. 1981-1987 7 p.

Research output: Contribution to journal › Article › peer-review

23 Citations (Scopus)

Assessing the Essentiality of Leishmania donovani Nitroreductase and Its Role in Nitro Drug Activation

Wyllie, S., Patterson, S. & Fairlamb, A. H., Feb 2013, In: Antimicrobial Agents and Chemotherapy. 57, 2, p. 901-906 6 p.

Research output: Contribution to journal › Article › peer-review

53 Citations (Scopus)

Characterization of Staphylococcus aureus EssB, an integral membrane component of the Type VII secretion system: atomic resolution crystal structure of the cytoplasmic segment

Zoltner, M., Fyfe, P. K., Palmer, T. & Hunter, W. N., 15 Jan 2013, In: Biochemical Journal. 449, 2, p. 469-477 9 p.

Research output: Contribution to journal › Article › peer-review

20 Citations (Scopus)

Chronic exposure to arsenic in drinking water can lead to resistance to antimonial drugs in a mouse model of visceral leishmaniasis

Perry, M. R., Wyllie, S., Raab, A., Feldmann, J. & Fairlamb, A. H. (Lead / Corresponding author), 2013, In: Proceedings of the National Academy of Sciences. n/a, n/a.

Research output: Contribution to journal › Article › peer-review

58 Citations (Scopus)

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay.

De Rycker, M. (Lead / Corresponding author), Hallyburton, I., Thomas, J., Campbell, L., Wyllie, S., Joshi, D., Cameron, S., Gilbert, I. H., Wyatt, P. G., Frearson, J. A., Fairlamb, A. H. & Gray, D. W., Jul 2013, In: Antimicrobial Agents and Chemotherapy. 57, 7, p. 2913-2922 10 p.

Research output: Contribution to journal › Article › peer-review

130 Citations (Scopus)

Discovery and structure-activity relationships of pyrrolone antimalarials

Murugesan, D., Mital, A., Kaiser, M., Shackleford, D. M., Morizzi, J., Katneni, K., Campbell, M., Hudson, A., Charman, S. A., Yeates, C. & Gilbert, I. H. (Lead / Corresponding author), 2013, In: Journal of Medicinal Chemistry. 56, 7, p. 2975-2990 16 p.

Research output: Contribution to journal › Article › peer-review

67 Citations (Scopus)

Exploring the Trypanosoma brucei Hsp83 Potential as a Target for Structure Guided Drug Design

Pizarro, J. C. (Lead / Corresponding author), Hills, T., Senisterra, G., Wernimont, A. K., Mackenzie, C., Norcross, N. R., Ferguson, M. A. J., Wyatt, P. G., Gilbert, I. H. & Hui, R., 17 Oct 2013, In: PLoS Neglected Tropical Diseases. 7, 10, e2492.

Research output: Contribution to journal › Article › peer-review

Open Access

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34 Citations (Scopus)

177 Downloads (Pure)

Global quantitative SILAC phosphoproteomics reveals differential phosphorylation is widespread between the procyclic and bloodstream form lifecycle stages of Trypanosoma brucei

Urbaniak, M. D., Martin, D. M. A. & Ferguson, M. A. J., 3 May 2013, In: Journal of Proteome Research. 12, 5, p. 2233-2244 12 p.

Research output: Contribution to journal › Article › peer-review

147 Citations (Scopus)

Proteomic selection of immunodiagnostic antigens for human African trypanosomiasis and generation of a prototype lateral flow immunodiagnostic device

Sullivan, L., Wall, S. J., Carrington, M. & Ferguson, M. A. J., 28 Feb 2013, In: PLoS Neglected Tropical Diseases. 7, 2, 14 p., e2087.

Research output: Contribution to journal › Article › peer-review

44 Citations (Scopus)

Structure-Activity Relationship Studies of Pyrrolone Antimalarial Agents

Murugesan, D., Kaiser, M., White, K. L., Norval, S., Riley, J., Wyatt, P. G., Charman, S. A., Read, K. D., Yeates, C. & Gilbert, I. H. (Lead / Corresponding author), 2013, In: ChemMedChem.

Research output: Contribution to journal › Article › peer-review

37 Citations (Scopus)

Structure of a complex phosphoglycan epitope from gp72 of Trypanosoma cruzi

Allen, S., Richardson, J. M., Mehlert, A. & Ferguson, M. A. J., 19 Apr 2013, In: Journal of Biological Chemistry. 288, 16, p. 11093-11105 13 p.

Research output: Contribution to journal › Article › peer-review

22 Citations (Scopus)

Structure of diaminohydroxyphosphoribosylaminopyrimidine deaminase/5-amino-6-(5-phosphoribosylamino)uracil reductase from Acinetobacter baumannii

Dawson, A., Trumper, P., Chrysostomou, G. & Hunter, W. N., 2013, In: Acta Crystallographica F-Structural Biology and Crystallization Communications. 69, 6, p. 611-617 7 p.

Research output: Contribution to journal › Article › peer-review

3 Citations (Scopus)

Structure of Pseudomonas aeruginosa inosine 5-monophosphate dehydrogenase

Rao, V. A., Shepherd, S. M., Owen, R. & Hunter, W. N., 2013, In: Acta Crystallographica F-Structural Biology and Crystallization Communications. 69, 3, p. 243-247 5 p.

Research output: Contribution to journal › Article › peer-review

15 Citations (Scopus)

The architecture of EssB, an integral membrane component of the type VII secretion system

Zoltner, M., Norman, D. G., Fyfe, P. K., El Mkami, H., Palmer, T. & Hunter, W. N. (Lead / Corresponding author), 2 Apr 2013, In: Structure. 21, 4, p. 595-603 9 p.

Research output: Contribution to journal › Article › peer-review

14 Citations (Scopus)

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

59 Citations (Scopus)

Trypanosoma brucei (UMP synthase null mutants) are avirulent in mice, but recover virulence upon prolonged culture in vitro while retaining pyrimidine auxotrophy

Ong, H. B., Sienkiewicz, N., Wyllie, S., Patterson, S. & Fairlamb, A. H., Oct 2013, In: Molecular Microbiology. 90, 2, p. 443-455 13 p.

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

2012

Assessment of pseudomonas aeruginosa N-5,N-10-methylenetetrahydrofolate dehydrogenase - cyclohydrolase as a potential antibacterial drug target

Eadsforth, T. C., Gardiner, M., Maluf, F. V., McElroy, S., James, D., Frearson, J., Gray, D. & Hunter, W. N., 2012, In: PLoS ONE. 7, 4, p. - 11 p., e35973.

Research output: Contribution to journal › Article › peer-review

19 Citations (Scopus)

A static-cidal assay for Trypanosoma brucei to aid hit prioritisation for progression into drug discovery programmes

De Rycker, M. (Lead / Corresponding author), O'Neill, S., Joshi, D., Campbell, L., Gray, D. W. & Fairlamb, A. H., 29 Nov 2012, In: PLoS Neglected Tropical Diseases. 6, 11, p. e1932

Research output: Contribution to journal › Article › peer-review

31 Citations (Scopus)

Automated design of ligands to polypharmacological profiles

Besnard, J., Ruda, G. F., Setola, V., Abecassis, K., Rodriguiz, R. M., Huang, X.-P., Norval, S., Sassano, M. F., Shin, A. I., Webster, L. A., Simeons, F. R. C., Stojanovski, L., Prat, A., Seidah, N. G., Constam, D. B., Bickerton, G. R., Read, K. D., Wetsel, W. C., Gilbert, I. H. & Roth, B. L. (Lead / Corresponding author) & 1 others, Hopkins, A. L. (Lead / Corresponding author), 13 Dec 2012, In: Nature. 492, 7428, p. 215-220 8 p.

Research output: Contribution to journal › Article › peer-review

682 Citations (Scopus)

Chemical, genetic and structural assessment of pyridoxal kinase as a drug target in the African trypanosome

Jones, D. C., Alphey, M. S., Wyllie, S. & Fairlamb, A. H. (Lead / Corresponding author), Oct 2012, In: Molecular Microbiology. 86, 1, p. 51-64 14 p.

Research output: Contribution to journal › Article › peer-review

28 Citations (Scopus)

Chemical Proteomic Analysis Reveals the Drugability of the Kinome of Trypanosoma brucei

Urbaniak, M. D., Mathieson, T., Bantscheff, M., Eberhard, D., Grimaldi, R., Miranda-Saavedra, D., Wyatt, P., Ferguson, M. A. J., Frearson, J. & Drewes, G., 2012, In: ACS Chemical Biology. 7, 11, p. 1858-1865 8 p.

Research output: Contribution to journal › Article › peer-review

49 Citations (Scopus)

Comparative SILAC proteomic analysis of Trypanosoma brucei bloodstream and procyclic lifecycle stages

Urbaniak, M. D., Guther, M. L. S. & Ferguson, M. A. J., 2012, In: PLoS ONE. 7, 5, p. - 8 p., e36619.

Research output: Contribution to journal › Article › peer-review

131 Citations (Scopus)

Conserved signal peptide recognition systems across the prokaryotic domains

Coulthurst, S. J., Dawson, A., Hunter, W. N. & Sargent, F. (Lead / Corresponding author), 28 Feb 2012, In: Biochemistry. 51, 8, p. 1678-1686 9 p.

Research output: Contribution to journal › Article › peer-review

24 Citations (Scopus)

Design, Synthesis and Biological Evaluation of Trypanosoma brucei Trypanothione Synthetase Inhibitors

Spinks, D., Torrie, L. S., Thompson, S., Harrison, J. R., Frearson, J. A., Read, K. D., Fairlamb, A. H., Wyatt, P. G. & Gilbert, I. H., 2 Jan 2012, In: ChemMedChem. 7, 1, p. 95-106 12 p.

Research output: Contribution to journal › Article › peer-review

43 Citations (Scopus)

6 Downloads (Pure)

IQGAP Proteins Reveal an Atypical Phosphoinositide (aPI) Binding Domain with a Pseudo C2 Domain Fold

Dixon, M. J., Gray, A., Schenning, M., Agacan, M., Tempel, W., Tong, Y., Nedyalkova, L., Park, H.-W., Leslie, N. R., van Aalten, D. M. F., Downes, C. P. & Batty, I. H., 29 Jun 2012, In: Journal of Biological Chemistry. 287, 27, p. 22483-22496 14 p.

Research output: Contribution to journal › Article › peer-review

23 Citations (Scopus)

Leishmania TDR1 structure, a unique trimeric glutathione transferase capable of deglutathionylation and antimonial prodrug activation

Fyfe, P. K., Westrop, G. D., Silva, A. M., Coombs, G. H. & Hunter, W. N. (Lead / Corresponding author), 2012, In: Proceedings of the National Academy of Sciences of the United States of America. 109, 29, p. 11693-11698 6 p.

Research output: Contribution to journal › Article › peer-review

39 Citations (Scopus)

Modeling of the N-Glycosylated Transferrin Receptor Suggests How Transferrin Binding Can Occur within the Surface Coat of Trypanosoma brucei

Mehlert, A., Wormald, M. R. & Ferguson, M. A. J. (Lead / Corresponding author), Apr 2012, In: PLoS Pathogens. 8, 4, p. - 11 p., e1002618.

Research output: Contribution to journal › Article › peer-review

36 Citations (Scopus)

New secreted toxins and immunity proteins encoded within the type VI secretion system gene cluster of Serratia marcescens

English, G., Trunk, K., Rao, V. A., Srikannathasan, V., Hunter, W. N. & Coulthurst, S. J. (Lead / Corresponding author), Nov 2012, In: Molecular Microbiology. 86, 4, p. 921-936 16 p.

Research output: Contribution to journal › Article › peer-review

106 Citations (Scopus)

Quantifying the chemical beauty of drugs

Bickerton, G. R., Paolini, G. V., Besnard, J., Muresan, S. & Hopkins, A. L. (Lead / Corresponding author), Feb 2012, In: Nature Chemistry. 4, 2, p. 90-98 9 p.

Research output: Contribution to journal › Article › peer-review

1470 Citations (Scopus)

Synthesis and Evaluation of α-Thymidine Analogues as Novel Antimalarials

Cui, H., Carrero-Lérida, J., Silva, A. P. G., Whittingham, J. L., Brannigan, J. A., Ruiz-Pérez, L. M., Read, K. D., Wilson, K. S. (Lead / Corresponding author), González-Pacanowska, D. (Lead / Corresponding author) & Gilbert, I. H. (Lead / Corresponding author), 2012, In: Journal of Medicinal Chemistry. 55, 24, p. 10948-57 10 p.

Research output: Contribution to journal › Article › peer-review

36 Citations (Scopus)

The Anti-Trypanosome Drug Fexinidazole Shows Potential for Treating Visceral Leishmaniasis

Wyllie, S., Patterson, S., Stojanovski, L., Simeons, F. R. C., Norval, S., Kime, R., Read, K. D. & Fairlamb, A. H. (Lead / Corresponding author), 1 Feb 2012, In: Science Translational Medicine. 4, 119, p. - 7 p., 119re1.

Research output: Contribution to journal › Article › peer-review

124 Citations (Scopus)

The crystal structure of Leishmania major N-5,N-10-methylenetetrahydrofolate dehydrogenase/cyclohydrolase and assessment of a potential drug target

Eadsforth, T. C., Cameron, S. & Hunter, W. N., Feb 2012, In: Molecular and Biochemical Parasitology. 181, 2, p. 178-185 8 p.

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

The de novo and salvage pathways of GDP-mannose biosynthesis are both sufficient for the growth of bloodstream-form Trypanosoma brucei

Kuettel, S., Wadum, M. C. T., Guther, M. L. S., Marino, K., Riemer, C. & Ferguson, M. A. J. (Lead / Corresponding author), Apr 2012, In: Molecular Microbiology. 84, 2, p. 340-351 12 p.

Research output: Contribution to journal › Article › peer-review

19 Citations (Scopus)

The lipid-linked oligosaccharide donor specificities of Trypanosoma brucei oligosaccharyltransferases

Izquierdo, L., Mehlert, A. & Ferguson, M. A. J., May 2012, In: Glycobiology. 22, 5, p. 696-703 8 p.

Research output: Contribution to journal › Article › peer-review

21 Citations (Scopus)

Whole organism high-content screening by label-free, image-based Bayesian classification for parasitic diseases

Paveley, R. A., Mansour, N. R., Hallyburton, I., Bleicher, L. S., Benn, A. E., Mikic, I., Guidi, A., Gilbert, I. H., Hopkins, A. L. & Bickle, Q. D. (Lead / Corresponding author), 31 Jul 2012, In: PLoS Neglected Tropical Diseases. 6, 7, 11 p., e1762.

Research output: Contribution to journal › Article › peer-review

86 Citations (Scopus)

2011

Antitumor Quinol PMX464 Is a Cytocidal Anti-trypanosomal Inhibitor Targeting Trypanothione Metabolism

Konig, J., Wyllie, S., Wells, G., Stevens, M. F., Wyatt, P. G. & Fairlamb, A. H., 11 Mar 2011, In: Journal of Biological Chemistry. 286, 10, p. 8523-8533 11 p.

Research output: Contribution to journal › Article › peer-review

36 Citations (Scopus)

A Screen for Novel Phosphoinositide 3-kinase Effector Proteins

Dixon, M. J., Gray, A., Boisvert, F.-M., Agacan, M., Morrice, N. A., Gourlay, R., Leslie, N. R., Downes, C. P. & Batty, I. H., Apr 2011, In: Molecular & Cellular Proteomics. 10, 4, p. - 13 p., 003178.

Research output: Contribution to journal › Article › peer-review

26 Citations (Scopus)

Chemical structure of Trichomonas vaginalis surface lipoglycan: a role for short galactose (beta 1-4/3) N-acetylglucosamine repeats in host cell interaction

Ryan, C. M., Mehlert, A., Richardson, J. M., Ferguson, M. A. J. & Johnson, P. J., 25 Nov 2011, In: Journal of Biological Chemistry. 286, 47, p. 40494-40508 15 p.

Research output: Contribution to journal › Article › peer-review

39 Citations (Scopus)

Computational approaches to selecting and optimising targets for structural biology

Overton, I. M. & Barton, G. J., Sept 2011, In: Journal of Neuroscience Methods. 55, 1, p. 311 9 p.

Research output: Contribution to journal › Article › peer-review

8 Citations (Scopus)

Crystal structures of Burkholderia cenocepacia dihydropteroate synthase in the apo-form and complexed with the product 7,8-dihydropteroate

Morgan, R. E., Batot, G. O., Dement, J. M., Rao, V. A., Eadsforth, T. C. & Hunter, W. N., 9 May 2011, In: BMC Structural Biology. 11, p. - 9 p., 21.

Research output: Contribution to journal › Article › peer-review

18 Citations (Scopus)

Crystal structures of penicillin-binding protein 3 from Pseudomonas aeruginosa: comparison of native and antibiotic-bound forms

Sainsbury, S., Bird, L., Rao, V., Shepherd, S. M., Stuart, D. I., Hunter, W. N., Owens, R. J. & Ren, J., 7 Jan 2011, In: Journal of Molecular Biology. 405, 1, p. 173-184 12 p.

Research output: Contribution to journal › Article › peer-review

75 Citations (Scopus)

Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein Crystallography

Patterson, S., Alphey, M. S., Jones, D. C., Shanks, E. J., Street, I. P., Frearson, J. A., Wyatt, P. G., Gilbert, I. H. & Fairlamb, A. H., 13 Oct 2011, In: Journal of Medicinal Chemistry. 54, 19, p. 6514-6530 17 p.

Research output: Contribution to journal › Article › peer-review

123 Citations (Scopus)

Investigation of copper(II) tetrafluoroborate catalysed epoxide opening

Capes, A. S., Crossman, A. T., Webster, L. A., Ferguson, M. A. J. & Gilbert, I. H., 28 Dec 2011, In: Tetrahedron Letters. 52, 52, p. 7091-7094 4 p.

Research output: Contribution to journal › Article › peer-review

12 Citations (Scopus)

13 Downloads (Pure)

Java bioinformatics analysis web services for multiple sequence alignment-JABAWS:MSA

Troshin, P. V., Procter, J. B. & Barton, G. J., 15 Jul 2011, In: BMC Bioinformatics. 27, 14, p. 2001-2002 2 p.

Research output: Contribution to journal › Article › peer-review

105 Citations (Scopus)

Probing Elongating and Branching beta-D-Galactosyltransferase Activities in Leishmania Parasites by Making Use of Synthetic Phosphoglycans

Sizova, O. V., Ross, A. J., Ivanova, I. A., Borodkin, V. S., Ferguson, M. A. J. & Nikolaev, A. V. (Lead / Corresponding author), Jun 2011, In: ACS Chemical Biology. 6, 6, p. 648-657 10 p.

Research output: Contribution to journal › Article › peer-review

6 Citations (Scopus)

Aref#d: 19815. Wellcome Trust Centre for Drug Discovery (Strategic Award)

Research output

Search results