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Biological Chemistry and Drug Discovery

  1. Goserelin, as an ovarian protector during (neo)adjuvant breast cancer chemotherapy, prevents long term altered bone turnover

    Wilson, C., Gossiel, F., Leonard, R., Anderson, R. A., Adamson, D. J. A., Thomas, G. & Coleman, R. E. Mar 2016 In : Journal of Bone Oncology. 5, 1, p. 43-49 7 p.

    Research output: Contribution to journalArticle

  2. Biophysical characterization of laforin-carbohydrate interaction

    Dias, D. M., Furtado, J., Wasielewski, E., Cruz, R., Costello, B., Cole, L., Faria, T. Q., Baaske, P., Brito, R. M. M., Ciulli, A., Simões, I., Macedo-Ribeiro, S., Faro, C., Geraldes, C. F. G. C. & Castanheira, P. 1 Feb 2016 In : Biochemical Journal. 473, 3, p. 335-345 11 p.

    Research output: Contribution to journalArticle

  3. Optimization of inhibitors of Mycobacterium tuberculosis pantothenate synthetase based on group efficiency analysis

    Hung, A. W., Silvestre, H. L., Wen, S., George, G. P. C., Boland, J., Blundell, T. L., Ciulli, A. & Abell, C. 5 Jan 2016 In : ChemMedChem. 11, 1, p. 38-42

    Research output: Contribution to journalArticle

  4. Subunit connectivity, assembly determinants and architecture of the yeast exocyst complex

    Heider, M. R., Gu, M., Duffy, C. M., Mirza, A. M., Marcotte, L. L., Walls, A. C., Farrall, N., Hakhverdyan, Z., Field, M. C., Rout, M. P., Frost, A. & Munson, M. Jan 2016 In : Nature Structural & Molecular Biology. 23, 1, p. 59-66 8 p.

    Research output: Contribution to journalArticle

  5. The use of the Rx spin label in orientation measurement on proteins, by EPR

    Stevens, M. A., McKay, J. E., Robinson, J. L. S., El Mkami, H., Smith, G. M. & Norman, D. G. 2016 In : Physical Chemistry Chemical Physics. 18, 8, p. 5799-5806 8 p.

    Research output: Contribution to journalArticle

  6. Correction: Modulation of the surface proteome through multiple ubiquitylation pathways in African Trypanosomes

    Zoltner, M., Leung, K. F., Alsford, S., Horn, D. & Field, M. C. 23 Nov 2015 In : PLoS Pathogens. 11, 11, 3 p., e1005291

    Research output: Contribution to journalArticle

  7. 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 journalArticle

  8. 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. Nov 2015 In : ChemMedChem. 10, 11, p. 1809-1820 12 p.

    Research output: Contribution to journalArticle

  9. Modulation of the surface proteome through multiple ubiquitylation pathways in African Trypanosomes

    Zoltner, M., Leung, K. F., Alsford, S., Horn, D. & Field, M. C. 22 Oct 2015 In : PLoS Pathogens. 11, 10, 26 p., e1005236

    Research output: Contribution to journalArticle

  10. Discovery and optimisation studies of antimalarial phenotypic hits

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

    Research output: Contribution to journalArticle

  11. 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. 8 Oct 2015 In : Journal of Medicinal Chemistry. 58, 19, p. 7695-7706 12 p.

    Research output: Contribution to journalArticle

  12. Leishmania major UDP-sugar pyrophosphorylase salvages galactose for glycoconjugate biosynthesis

    Damerow, S., Hoppe, C., Bandini, G., Zarnovican, P., Buettner, F. F. R., Ferguson, M. A. J. & Routier, F. H. Oct 2015 In : International Journal for Parasitology. 45, 12, p. 783-790 8 p.

    Research output: Contribution to journalArticle

  13. Cohort comparison study of cardiac disease and atherosclerotic burden in type 2 diabetic adults using whole body cardiovascular magnetic resonance imaging

    Duce, S. L., Weir-McCall, J. R., Gandy, S. J., Matthew, S. Z., Cassidy, D. B., McCormick, L., Rauchhaus, P., Looker, H., Colhoun, H. M. & Houston, J. G. 18 Sep 2015 In : Cardiovascular Diabetology. 14, 11 p., 122

    Research output: Contribution to journalArticle

  14. A mutant O-GlcNAcase as a probe to reveal global dynamics of protein O-GlcNAcylation during Drosophila embryonic development

    Mariappa, D., Selvan, N., Borodkin, V. S., Alonso , J., Ferenbach, A. T., Shepherd, C., Navratilova, I. H. & Van Aalten, D. M. F. Sep 2015 In : Biochemical Journal. 470, 2, p. 255-262 8 p.

    Research output: Contribution to journalArticle

  15. Selective small molecule induced degradation of the BET bromodomain protein BRD4

    Zengerle, M., Chan, K-H. & Ciulli, A. 21 Aug 2015 In : ACS Chemical Biology. 10, 8, p. 1770-1777 8 p.

    Research output: Contribution to journalArticle

  16. Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity

    Sola, I., Castellà, S., Viayna, E., Galdeano, C., Taylor, M. C., Gbedema, S. Y., Pérez, B., Clos, M. V., Jones, D. C., Fairlamb, A. H., Wright, C. W., Kelly, J. M. & Muñoz-Torrero, D. 15 Aug 2015 In : Bioorganic & Medicinal Chemistry. 23, 16, p. 5156-5167 12 p.

    Research output: Contribution to journalArticle

  17. Bacillus anthracis meningitis during an outbreak of injectional anthrax, Scotland, UK

    Dewar, S., Weir-McCall, J. R., Batchelor, L., Cole, S. & Parcell, B. J. 1 Aug 2015 In : Clinical Microbiology and Infection. 21, 8, p. e49-e50 2 p.

    Research output: Contribution to journalArticle

  18. Binding to serine 65-phosphorylated ubiquitin primes Parkin for optimal PINK1-dependent phosphorylation and activation

    Kazlauskaite, A., Martínez-Torres, R. J., Wilkie, S., Kumar, A., Peltier, J., Gonzalez, A., Johnson, C., Zhang, J., Hope, A. G., Peggie, M., Trost, M., van Aalten, D. M., Alessi, D. R., Prescott, A. R., Knebel, A., Walden, H. & Muqit, M. M. K. 1 Aug 2015 In : EMBO Reports. 16, 8, p. 939-954 16 p.

    Research output: Contribution to journalArticle

  19. Chimerization at the AQP2-AQP3 locus is the genetic basis of melarsoprol-pentamidine cross-resistance in clinical Trypanosoma brucei gambiense isolates

    Graf, F. E., Baker, N., Munday, J. C., de Koning, H. P., Horn, D. & Mäser, P. Aug 2015 In : International Journal for Parasitology: Drugs and Drug Resistance. 5, 2, p. 65-68 4 p.

    Research output: Contribution to journalArticle

  20. Quantitative sequencing confirms VSG diversity as central to immune evasion by Trypanosoma brucei

    McCulloch, R. & Field, M. C. Aug 2015 In : Trends in Parasitology. 31, 8, p. 346-349 4 p.

    Research output: Contribution to journalArticle

  21. Vacuolar ATPase depletion affects mitochondrial ATPase function, kinetoplast dependency, and drug sensitivity in trypanosomes

    Baker, N., Hamilton, G., Wilkes, J. M., Hutchinson, S., Barrett, M. P. & Horn, D. 21 Jul 2015 In : Proceedings of the National Academy of Sciences of the United States of America. 112, 29, p. 9112-9117 6 p.

    Research output: Contribution to journalArticle

  22. Crystal structures reveal that the reaction mechanism of imidazoleglycerol-phosphate dehydratase is controlled by switching Mn(II) coordination

    Bisson, C., Britton, K. L., Sedelnikova, S. E., Rodgers, H. F., Eadsforth, T. C., Viner, R. C., Hawkes, T. R., Baker, P. J. & Rice, D. W. 7 Jul 2015 In : Structure. 23, 7, p. 1236-1245 10 p.

    Research output: Contribution to journalArticle

  23. Architecture of a host-parasite interface: complex targeting mechanisms revealed through proteomics

    Gadelha, C., Zhang, W., Chamberlain, J. W., Chait, B. T., Wickstead, B. & Field, M. C. Jul 2015 In : Molecular & Cellular Proteomics. 14, 7, p. 1911-1926 16 p.

    Research output: Contribution to journalArticle

  24. 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. 19 Jun 2015 In : ACS Chemical Biology. 10, 6, p. 1425-1434 10 p.

    Research output: Contribution to journalArticle

  25. A novel multiple-stage antimalarial agent that inhibits protein synthesis

    Fairlamb, A. H. , Gilbert, I. H. & 61 others Baragana, B., Hallyburton, I., Lee, M. C. S., 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., Santos Martinez, M., 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., Belén Jiménez-Díaz, M., Maria Sanz, L., 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., Javier Gamo, F., 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., Willis, P. A., Rayner, J. C., Fidock, D. A. & Read, K. D. 18 Jun 2015 In : Nature. 522, 7556, p. 315-320 6 p.

    Research output: Contribution to journalArticle

  26. Application of RNAi to genomic drug target validation in schistosomes

    Guidi, A., Mansour, N. R., Paveley, R. A., Carruthers, I. M., Besnard, J., Hopkins, A. L., Gilbert, I. H. & Bickle, Q. D. 20 May 2015 In : PLoS Neglected Tropical Diseases. 9, 5, 22 p., e0003801

    Research output: Contribution to journalArticle

  27. Targeting Cullin-RING E3 ubiquitin ligases for drug discovery: structure, assembly and small-molecule modulation

    Bulatov, E. & Ciulli, A. 1 May 2015 In : Biochemical Journal. 467, 3, p. 365-386 22 p.

    Research output: Contribution to journalArticle

  28. Crystal structure of the C-terminal domain of tubulin-binding cofactor C from Leishmania major

    Barrack, K. L., Fyfe, P. K., Finney, A. J. & Hunter, W. N. May 2015 In : Molecular and Biochemical Parasitology. 201, 1, p. 26-30 5 p.

    Research output: Contribution to journalArticle

  29. Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase

    Robinson, D. A. & Wyatt, P. G. May 2015 In : Acta Crystallographica Section F: Structural Biology Communications. 71, 5, p. 586-593 8 p.

    Research output: Contribution to journalArticle

  30. Macromolecular crystallography and what it can contribute to antiparasite drug discovery

    Hunter, W. N. & Weiss, M. S. May 2015 In : Acta Crystallographica Section F: Structural Biology Communications. 71, 5, p. 483-484 2 p.

    Research output: Contribution to journalEditorial

  31. Identification of caveolar resident proteins in ventricular myocytes using a quantitative proteomic approach: dynamic changes in caveolar composition following adrenoceptor activation

    Wypijewski, K. J., Tinti, M., Chen, W., Lamont, D., Ashford, M. L. J., Calaghan, S. C. & Fuller, W. Mar 2015 In : Molecular & Cellular Proteomics. 14, 3, p. 596-608 13 p.

    Research output: Contribution to journalArticle

  32. Arsenic, antimony, and Leishmania: has arsenic contamination of drinking water in India led to treatment-resistant kala-azar?

    Perry, M., Wyllie, S., Prajapati, V., Menten, J., Raab, A., Feldmann, J., Chakraborti, D., Sundar, S., Boelaert, M., Picado, A. & Fairlamb, A. 26 Feb 2015 In : Lancet. 385, Supplement 1, p. S80 1 p.

    Research output: Contribution to journalArticle

  33. Decreased adipogenesis and adipose tissue in mice with inactivated protein phosphatase 5

    Jacob, W., Rosenzweig, D., Vázquez-Martin, C., Duce, S. L. & Cohen, P. T. W. 15 Feb 2015 In : Biochemical Journal. 466, 1, p. 163-176 14 p.

    Research output: Contribution to journalArticle

  34. 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-Cabello, M., Taylor, M., Gilbert, I., McLaren, A. W. & Wolf, C. R. 1 Feb 2015 In : Biochemical Journal. 465, 3, p. 479-488 10 p.

    Research output: Contribution to journalArticle

  35. The Joint European Compound Library: boosting precompetitive research

    Besnard, J., Jones, P. S., Hopkins, A. L. & Pannifer, A. D. Feb 2015 In : Drug Discovery Today. 20, 2, p. 181-186 6 p.

    Research output: Contribution to journalArticle

  36. TrypanoCyc: a community-led biochemical pathways database for Trypanosoma brucei

    Fairlamb, A. H. , Ferguson, M. A. J. & 39 others Shameer, S., Logan-Klumpler, F. J., Vinson, F., Cottret, L., Merlet, B., Achcar, F., Boshart, M., Berriman, M., Breitling, R., Bringaud, F., Bütikofer, P., Cattanach, A. M., Bannerman-Chukualim, B., Creek, D. J., Crouch, K., de Koning, H. P., Denise, H., Ebikeme, C., Ginger, M. L., Hertz-Fowler, C., Kerkhoven, E. J., Mäser, P., Michels, P. A. M., Nayak, A., Nes, D. W., Nolan, D. P., Olsen, C., Silva-Franco, F., Smith, T. K., Taylor, M. C., Tielens, A. G. M., Urbaniak, M. D., van Hellemond, J. J., Vincent, I. M., Wilkinson, S. R., Wyllie, S., Opperdoes, F. R., Barrett, M. P. & Jourdan, F. 28 Jan 2015 In : Nucleic Acids Research. 43, D1, p. D637-D644 8 p.

    Research output: Contribution to journalArticle

  37. Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC

    Tallant, C., Valentini, E., Fedorov, O., Overvoorde, L., Ferguson, F. M., Filippakopoulos, P., Svergun, D. I., Knapp, S. & Ciulli, A. 6 Jan 2015 In : Structure. 23, 1, p. 80-92 13 p.

    Research output: Contribution to journalArticle

  38. Crystals on the cover 2015

    Einspahr, H., Weiss, M. S. & Hunter, W. N. Jan 2015 In : Acta Crystallographica Section F: Structural Biology Communications. F71, 1, p. 1-2 2 p.

    Research output: Contribution to journalArticle

  39. Fragment-Based Screening in Tandem with Phenotypic Screening Provides Novel Antiparasitic Hits

    Blaazer, A. R., Orrling, K. M., Shanmugham, A., Jansen, C., Maes, L., Edink, E., Sterk, G. J., Siderius, M., England, P., Bailey, D., de Esch, I. J. P. & Leurs, R. Jan 2015 In : Journal of Biomolecular Screening. 20, 1, p. 131-140 10 p.

    Research output: Contribution to journalArticle

  40. Genome-scale RNAi screens for high-throughput phenotyping in bloodstream-form African trypanosomes

    Glover, L., Alsford, S., Baker, N., Turner, D. J., Sanchez-Flores, A., Hutchinson, S., Hertz-Fowler, C., Berriman, M. & Horn, D. Jan 2015 In : Nature Protocols. 10, 1, p. 106-33 28 p.

    Research output: Contribution to journalArticle

  41. 14-3-3-Pred: Improved methods to predict 14-3-3-binding phosphopeptides

    Madeira, F., Tinti, M., Murugesan, G., Berrett, E., Stafford, M., Toth, R., Cole, C., MacKintosh, C. & Barton, G. J. 2015 In : Bioinformatics.

    Research output: Contribution to journalArticle

  42. Arsenic exposure and outcomes of antimonial treatment in visceral leishmaniasis patients in bihar, India: a retrospective cohort study

    Perry, M. R., Prajapati, V. K., Menten, J., Raab, A., Feldmann, J., Chakraborti, D., Sundar, S., Fairlamb, A. H., Boelaert, M. & Picado, A. 2015 In : PLoS Neglected Tropical Diseases. 9, 3, 17 p., e0003518

    Research output: Contribution to journalArticle

  43. Development and applications of biosensor assays for fragment screening of wild-type GPCRs

    Hopkins Navratilova, I. & Fagge, T. 2015 In : European Pharmaceutical Review. 20, 6, p. 29-31 3 p.

    Research output: Contribution to journalArticle

  44. ENTH and ANTH domain proteins participate in AP2-independent clathrin-mediated endocytosis

    Manna, P. T., Gadelha, C., Puttick, A. E. & Field, M. C. 2015 In : Journal of Cell Science. 128, 11, p. 2130-2142 13 p.

    Research output: Contribution to journalArticle

  45. Identification of a glycosylphosphatidylinositol anchor-modifying β1-3 galactosyltransferase in Trypanosoma brucei

    Izquierdo, L., Acosta-Serrano, A., Mehlert, A. & Ferguson, M. A. J. 2015 In : Glycobiology. 25, 4, p. 438-447 50 p.

    Research output: Contribution to journalArticle

  46. 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. & 2 others Fiandor, J. M. & Julio Martin, J. 2015 In : Scientific Reports. 5, 12 p., 8771

    Research output: Contribution to journalArticle

  47. New synthetic routes to Triazolo-benzodiazepine analogues: expanding the scope of the bump-and-hole approach for selective Bromo and Extra-Terminal (BET) bromodomain inhibition

    Baud, M. G. J., Lin-Shiao, E., Zengerle, M., Tallant, C. & Ciulli, A. 2015 In : Journal of Medicinal Chemistry. 59, 4, p. 1492-1500 9 p.

    Research output: Contribution to journalArticle

  48. Surface plasmon resonance analysis of seven-transmembrane receptors

    Aristotelous, T., Hopkins, A. L. & Navratilova, I. 2015 Membrane proteins—production and functional characterization. Shukla, A. K. (ed.). Academic Press, p. 499-525 27 p. (Methods in Enzymology; vol. 556)

    Research output: Chapter in Book/Report/Conference proceedingChapter (peer-reviewed)

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