University of Dundee

Biological Chemistry and Drug Discovery 2012

Abdelwahab, N. Z., Crossman, A. T., Sullivan, L., Ferguson, M. A. and Urbaniak, M. D. (2012) Inhibitors incorporating zinc-binding groups target the GlcNAc-PI de-N-acetylase in Trypanosoma brucei, the causative agent of African sleeping sickness. Chemical biology & drug design. 79, 270-278
doi; 10.1111/j.1747-0285.2011.01300.x
PMC22222041

Alsford, S., duBois, K., Horn, D. and Field, M. C. (2012) Epigenetic mechanisms, nuclear architecture and the control of gene expression in trypanosomes. Expert Rev Mol Med. 14, e13
doi; 10.1017/erm.2012.7
PMC22640744

Bandini, G., Marino, K., Guther, M. L., Wernimont, A. K., Kuettel, S., Qiu, W., Afzal, S., Kelner, A., Hui, R. and Ferguson, M. A. (2012) Phosphoglucomutase is absent in Trypanosoma brucei and redundantly substituted by phosphomannomutase and phospho-N-acetylglucosamine mutase. Molecular microbiologydoi; 10.1111/j.1365-2958.2012.08124.x
PMC22676716

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., 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. and Hopkins, A. L. (2012) Automated design of ligands to polypharmacological profiles. Nature. 492, 215-220
doi; 10.1038/nature11691
PMID;3653568  PMC23235874

Bickerton, G. R., Paolini, G. V., Besnard, J., Muresan, S. and Hopkins, A. L. (2012) Quantifying the chemical beauty of drugs. Nature chemistry. 4, 90-98
doi; 10.1038/nchem.1243
PMC22270643

Boisvert, F. M., Ahmad, Y., Gierlinski, M., Charriere, F., Lamont, D., Scott, M., Barton, G. and Lamond, A. I. (2012) A quantitative spatial proteomics analysis of proteome turnover in human cells. Mol Cell Proteomics. 11, M111 011429
doi; 10.1074/mcp.M111.011429
PMID;3316722  PMC21937730

Brand, S., Cleghorn, L. A., McElroy, S. P., Robinson, D. A., Smith, V. C., Hallyburton, I., Harrison, J. R., Norcross, N. R., Spinks, D., Bayliss, T., Norval, S., Stojanovski, L., Torrie, L. S., Frearson, J. A., Brenk, R., Fairlamb, A. H., Ferguson, M. A., Read, K. D., Wyatt, P. G. and Gilbert, I. H. (2012) Discovery of a novel class of orally active trypanocidal N-myristoyltransferase inhibitors. J Med Chem. 55, 140-152
doi; 10.1021/jm201091t
PMID;3256935  PMC22148754

Brenk, R. and Rauh, D. (2012) Change or be changed: Reflections of the workshop 'Future in Medicinal Chemistry'. Bioorganic & medicinal chemistry. 20, 3695-3697
doi; 10.1016/j.bmc.2012.04.038
PMC22607881

Capes, A., Patterson, S., Wyllie, S., Hallyburton, I., Collie, I. T., McCarroll, A. J., Stevens, M. F., Frearson, J. A., Wyatt, P. G., Fairlamb, A. H. and Gilbert, I. H. (2012) Quinol derivatives as potential trypanocidal agents. Bioorg Med Chem. 20, 1607-1615
doi; 10.1016/j.bmc.2011.12.018
PMID;3281193  PMC22264753

Coulthurst, S. J., Dawson, A., Hunter, W. N. and Sargent, F. (2012) Conserved signal peptide recognition systems across the prokaryotic domains. Biochemistry. 51, 1678-1686
doi; 10.1021/bi201852d
PMID;3290102  PMC22289056

Cui, H., Carrero-Lerida, J., Silva, A. P., Whittingham, J. L., Brannigan, J. A., Ruiz-Perez, L. M., Read, K. D., Wilson, K. S., Gonzalez-Pacanowska, D. and Gilbert, I. H. (2012) Synthesis and evaluation of alpha-thymidine analogues as novel antimalarials. J Med Chem. 55, 10948-10957
doi; 10.1021/jm301328h
PMID;3530961  PMC23240776

Daneshvar, H., Wyllie, S., Phillips, S., Hagan, P. and Burchmore, R. (2012) Comparative proteomics profiling of a gentamicin-attenuated Leishmania infantum cell line identifies key changes in parasite thiol-redox metabolism. J Proteomics. 75, 1463-1471
doi; 10.1016/j.jprot.2011.11.018
PMC22154982

De Rycker, M., O'Neill, S., Joshi, D., Campbell, L., Gray, D. W. and Fairlamb, A. H. (2012) A static-cidal assay for Trypanosoma brucei to aid hit prioritisation for progression into drug discovery programmes. PLoS Negl Trop Dis. 6, e1932
doi; 10.1371/journal.pntd.0001932
PMID;3510075  PMC23209868

Eadsforth, T. C., Cameron, S. and Hunter, W. N. (2012) The crystal structure of Leishmania major N(5),N(10)-methylenetetrahydrofolate dehydrogenase/cyclohydrolase and assessment of a potential drug target. Mol Biochem Parasitol. 181, 178-185
doi; 10.1016/j.molbiopara.2011.11.004
PMID;3368264  PMC22108435

Eadsforth, T. C., Gardiner, M., Maluf, F. V., McElroy, S., James, D., Frearson, J., Gray, D. and Hunter, W. N. (2012) Assessment of Pseudomonas aeruginosa N5,N10-methylenetetrahydrofolate dehydrogenase-cyclohydrolase as a potential antibacterial drug target. PLoS One. 7, e35973
doi; 10.1371/journal.pone.0035973
PMID;3338484  PMC22558288

Eadsforth, T. C., Maluf, F. V. and Hunter, W. N. (2012) Acinetobacter baumannii FolD ligand complexes --potent inhibitors of folate metabolism and a re-evaluation of the structure of LY374571. FEBS J. 279, 4350-4360
doi; 10.1111/febs.12025
PMID;3655515  PMC23050773

Fairlamb, A. H. (2012) Infectious disease: Genomics decodes drug action. Nature. 482, 167-169
doi; 10.1038/482167a
PMC22318598

Ferguson, M. A. and Anderson, J. S. (2012) Dynamical stability of intrinsic connectivity networks. Neuroimage. 59, 4022-4031
doi; 10.1016/j.neuroimage.2011.10.062
PMID;3288774  PMC22056459

Fyfe, P. K., Westrop, G. D., Ramos, T., Muller, S., Coombs, G. H. and Hunter, W. N. (2012) Structure of Leishmania major cysteine synthase. Acta crystallographica. Section F, Structural biology and crystallization communications. 68, 738-743
doi; 10.1107/S1744309112019124
PMC22750854

Fyfe, P. K., Westrop, G. D., Silva, A. M., Coombs, G. H. and Hunter, W. N. (2012) Leishmania TDR1 structure, a unique trimeric glutathione transferase capable of deglutathionylation and antimonial prodrug activation. Proceedings of the National Academy of Sciences of the United States of Americadoi; 10.1073/pnas.1202593109
PMC22753509

Han, J., Miranda-Saavedra, D., Luebbering, N., Singh, A., Sibbet, G., Ferguson, M. A. and Cleghon, V. (2012) Deep evolutionary conservation of an intramolecular protein kinase activation mechanism. PLoS One. 7, e29702
doi; 10.1371/journal.pone.0029702
PMID;3250476  PMC22235329

Hudson, S. A., McLean, K. J., Surade, S., Yang, Y. Q., Leys, D., Ciulli, A., Munro, A. W. and Abell, C. (2012) Application of fragment screening and merging to the discovery of inhibitors of the Mycobacterium tuberculosis cytochrome P450 CYP121. Angew Chem Int Ed Engl. 51, 9311-9316
doi; 10.1002/anie.201202544
PMC22890978

Izquierdo, L., Mehlert, A. and Ferguson, M. A. (2012) The lipid-linked oligosaccharide donor specificities of Trypanosoma brucei oligosaccharyltransferases. Glycobiology. 22, 696-703
doi; 10.1093/glycob/cws003
PMID;3311286  PMC22241825

Jones, D. C., Alphey, M. S., Wyllie, S. and Fairlamb, A. H. (2012) Chemical, genetic and structural assessment of pyridoxal kinase as a drug target in the African trypanosome. Mol Microbiol. 86, 51-64
doi; 10.1111/j.1365-2958.2012.08189.x
PMID;3470933  PMC22857512

Kuettel, S., Wadum, M. C., Guther, M. L., Marino, K., Riemer, C. and Ferguson, M. A. (2012) The de novo and salvage pathways of GDP-mannose biosynthesis are both sufficient for the growth of bloodstream-form Trypanosoma brucei. Molecular microbiology. 84, 340-351
doi; 10.1111/j.1365-2958.2012.08026.x
PMC22375793

Mehlert, A., Wormald, M. R. and Ferguson, M. A. (2012) Modeling of the N-glycosylated transferrin receptor suggests how transferrin binding can occur within the surface coat of Trypanosoma brucei. PLoS pathogens. 8, e1002618
doi; 10.1371/journal.ppat.1002618
PMID;3320590  PMC22496646

Miranda-Saavedra, D., Gabaldon, T., Barton, G. J., Langsley, G. and Doerig, C. (2012) The kinomes of apicomplexan parasites. Microbes Infect. 14, 796-810
doi; 10.1016/j.micinf.2012.04.007
PMC22587893

Muramoto, T., Cannon, D., Gierlinski, M., Corrigan, A., Barton, G. J. and Chubb, J. R. (2012) Live imaging of nascent RNA dynamics reveals distinct types of transcriptional pulse regulation. Proceedings of the National Academy of Sciences of the United States of America. 109, 7350-7355
doi; 10.1073/pnas.1117603109
PMID;3358836  PMC22529358

Navratilova, I., Macdonald, G., Robinson, C., Hughes, S., Mathias, J., Phillips, C. and Cook, A. (2012) Biosensor-based approach to the identification of protein kinase ligands with dual-site modes of action. J Biomol Screen. 17, 183-193
doi; 10.1177/1087057111422746
PMC22068706

Paveley, R. A., Mansour, N. R., Hallyburton, I., Bleicher, L. S., Benn, A. E., Mikic, I., Guidi, A., Gilbert, I. H., Hopkins, A. L. and Bickle, Q. D. (2012) Whole organism high-content screening by label-free, image-based Bayesian classification for parasitic diseases. PLoS Negl Trop Dis. 6, e1762
doi; 10.1371/journal.pntd.0001762
PMID;3409125  PMC22860151

Pohler, E., Mamai, O., Hirst, J., Zamiri, M., Horn, H., Nomura, T., Irvine, A. D., Moran, B., Wilson, N. J., Smith, F. J., Goh, C. S., Sandilands, A., Cole, C., Barton, G. J., Evans, A. T., Shimizu, H., Akiyama, M., Suehiro, M., Konohana, I., Shboul, M., Teissier, S., Boussofara, L., Denguezli, M., Saad, A., Gribaa, M., Dopping-Hepenstal, P. J., McGrath, J. A., Brown, S. J., Goudie, D. R., Reversade, B., Munro, C. S. and McLean, W. H. (2012) Haploinsufficiency for AAGAB causes clinically heterogeneous forms of punctate palmoplantar keratoderma. Nat Genet. 44, 1272-1276
doi; 10.1038/ng.2444
PMID;3836166  PMC23064416

Ramasamy, R. and Field, M. C. (2012) Terminal galactosylation of glycoconjugates in Plasmodium falciparum asexual blood stages and Trypanosoma brucei bloodstream trypomastigotes. Exp Parasitol. 130, 314-320
doi; 10.1016/j.exppara.2012.02.017
PMC22406352

Scott, M. S., Ono, M., Yamada, K., Endo, A., Barton, G. J. and Lamond, A. I. (2012) Human box C/D snoRNA processing conservation across multiple cell types. Nucleic Acids Res. 40, 3676-3688
doi; 10.1093/nar/gkr1233
PMID;3333852  PMC22199253

Sherstnev, A., Duc, C., Cole, C., Zacharaki, V., Hornyik, C., Ozsolak, F., Milos, P. M., Barton, G. J. and Simpson, G. G. (2012) Direct sequencing of Arabidopsis thaliana RNA reveals patterns of cleavage and polyadenylation. Nat Struct Mol Biol. 19, 845-852
doi; 10.1038/nsmb.2345
PMID;3533403  PMC22820990

Spinks, D., Torrie, L. S., Thompson, S., Harrison, J. R., Frearson, J. A., Read, K. D., Fairlamb, A. H., Wyatt, P. G. and Gilbert, I. H. (2012) Design, synthesis and biological evaluation of Trypanosoma brucei trypanothione synthetase inhibitors. ChemMedChem. 7, 95-106
doi; 10.1002/cmdc.201100420
PMID;3320663  PMC22162199

Tibarewal, P., Zilidis, G., Spinelli, L., Schurch, N., Maccario, H., Gray, A., Perera, N. M., Davidson, L., Barton, G. J. and Leslie, N. R. (2012) PTEN protein phosphatase activity correlates with control of gene expression and invasion, a tumor-suppressing phenotype, but not with AKT activity. Sci Signal. 5, ra18
doi; 10.1126/scisignal.2002138
PMC22375056

Tidten-Luksch, N., Grimaldi, R., Torrie, L. S., Frearson, J. A., Hunter, W. N. and Brenk, R. (2012) IspE Inhibitors Identified by a Combination of In Silico and In Vitro High-Throughput Screening. PloS one. 7, e35792
doi; 10.1371/journal.pone.0035792
PMID;3340893  PMC22563402

Urbaniak, M. D., Guther, M. L. and Ferguson, M. A. (2012) Comparative SILAC Proteomic Analysis of Trypanosoma brucei Bloodstream and Procyclic Lifecycle Stages. PloS one. 7, e36619
doi; 10.1371/journal.pone.0036619
PMID;3344917  PMC22574199

Urbaniak, M. D., Mathieson, T., Bantscheff, M., Eberhard, D., Grimaldi, R., Miranda-Saavedra, D., Wyatt, P., Ferguson, M. A., Frearson, J. and Drewes, G. (2012) Chemical proteomic analysis reveals the drugability of the kinome of Trypanosoma brucei. ACS Chem Biol. 7, 1858-1865
doi; 10.1021/cb300326z
PMID;3621575  PMC22908928

Wullschleger, S., Garcia-Martinez, J. M. and Duce, S. L. (2012) Quantitative MRI establishes the efficacy of PI3K inhibitor (GDC-0941) multi-treatments in PTEN-deficient mice lymphoma. Anticancer Res. 32, 415-420
doi; PMID;3292793  PMC22287727

Wyllie, S., Patterson, S., Stojanovski, L., Simeons, F. R., Norval, S., Kime, R., Read, K. D. and Fairlamb, A. H. (2012) The anti-trypanosome drug fexinidazole shows potential for treating visceral leishmaniasis. Sci Transl Med. 4, 119re111
doi; 10.1126/scitranslmed.3003326
PMID;3457684  PMC22301556