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Biological Chemistry and Drug Discovery

  1. 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

  2. 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

  3. 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

  4. 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

  5. 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

  6. 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

  7. 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

  8. 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

  9. 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

  10. 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 Julio Martin, J. 2015 In : Scientific Reports. 5, 12 p.8771

    Research output: Contribution to journalArticle

  11. PITX1, a specificity determinant in the HIF-1α-mediated transcriptional response to hypoxia

    Mudie, S., Bandarra, D., Batie, M., Biddlestone, J., Moniz, S., Ortmann, B., Shmakova, A. & Rocha, S. 15 Dec 2014 In : Cell Cycle. 13, 24, p. 3878-3891 14 p.

    Research output: Contribution to journalArticle

  12. O-GlcNAcase: promiscuous hexosaminidase or key regulator of O-GlcNAc signalling?

    Alonso , J., Schimpl, M. & van Aalten, D. M. F. 12 Dec 2014 In : Journal of Biological Chemistry. 289, 50, p. 34433-34439 7 p.

    Research output: Contribution to journalArticle

  13. Evolutionary cell biology: Two origins, one objective

    Lynch, M., Field, M. C., Goodson, H. V., Malik, H. S., Pereira-Leal, J. B., Roos, D. S., Turkewitz, A. P. & Sazer, S. 2 Dec 2014 In : Proceedings of the National Academy of Sciences of the United States of America. 111, 48, p. 16990-16994 5 p.

    Research output: Contribution to journalArticle

  14. Disposition and Metabolic Profiling of [14C]Cerlapirdine Using Accelerator Mass Spectrometry

    Tse, S., Leung, L., Raje, S., Seymour, M., Shishikura, Y. & Obach, R. S. Dec 2014 In : Drug Metabolism and Disposition. 42, 12, p. 2023-2032 10 p.

    Research output: Contribution to journalArticle

  15. Erratum for De Rycker et al., Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

    De Rycker, M., 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. Dec 2014 In : Antimicrobial Agents and Chemotherapy. 58, 12, p. 7622 1 p.

    Research output: Contribution to journalArticle

  16. GEN1 from a thermophilic fungus is functionally closely similar to non-eukaryotic junction-resolving enzymes

    Freeman, A. D. J., Liu, Y., Déclais, A-C., Gartner, A. & Lilley, D. M. J. Dec 2014 In : Journal of Molecular Biology. 426, 24, p. 3946-3959 14 p.

    Research output: Contribution to journalArticle

  17. The times they are a-changin' - news from Acta Crystallographica Section F

    Hunter, W. N. & Weiss, M. S. Dec 2014 In : Acta Crystallographica Section F: Structural Biology Communications. 70, 12, p. 1575 1 p.

    Research output: Contribution to journalEditorial

  18. Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III phosphoinositide 3-kinase

    Bago, R., Malik, N., Munson, M. J., Prescott, A. R., Davies, P., Sommer, E., Shpiro, N., Ward, R., Cross, D., Ganley, I. G. & Alessi, D. R. Nov 2014 In : Biochemical Journal. 463, 3, p. 413-427 15 p.

    Research output: Contribution to journalArticle

  19. Fragment screening by SPR and advanced application to GPCRs

    Shepherd, C. A., Hopkins, A. L. & Navratilova, I. Nov 2014 In : Progress in Biophysics and Molecular Biology. 116, 2-3, p. 113-123 11 p.

    Research output: Contribution to journalArticle

  20. NMR approaches in structure-based lead discovery: recent developments and new frontiers for targeting multi-protein complexes

    Dias, D. M. & Ciulli, A. Nov 2014 In : Progress in Biophysics and Molecular Biology. 116, 2-3, p. 101-112 12 p.

    Research output: Contribution to journalArticle

  21. Respiratory flexibility in response to inhibition of cytochrome C oxidase in Mycobacterium tuberculosis

    Arora, K., Ochoa-Montaño, B., Tsang, P. S., Blundell, T. L., Dawes, S. S., Mizrahi, V., Bayliss, T., Mackenzie, C. J., Cleghorn, L. A. T., Ray, P. C., Wyatt, P. G., Uh, E., Lee, J., Barry, C. E. & Boshoff, H. I. Nov 2014 In : Antimicrobial Agents and Chemotherapy. 58, 11, p. 6962-6965 4 p.

    Research output: Contribution to journalArticle

  22. The mitochondrial respiratory chain of the secondary green alga Euglena gracilis shares many additional subunits with parasitic Trypanosomatidae

    Perez, E., Lapaille, M., Degand, H., Cilibrasi, L., Villavicencio-Queijeiro, A., Morsomme, P., González-Halphen, D., Field, M. C., Remacle, C., Baurain, D. & Cardol, P. Nov 2014 In : Mitochondrion. 19 Pt B, p. 338-49 12 p.

    Research output: Contribution to journalArticle

  23. The spatial effect of protein deuteration on nitroxide spin-label relaxation: implications for EPR distance measurement

    El Mkami, H., Ward, R., Bowman, A., Owen-Hughes, T. & Norman, D. G. Nov 2014 In : Journal of Magnetic Resonance . 248, p. 36-41 6 p.

    Research output: Contribution to journalArticle

  24. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes

    Baud, M. G. J., Lin-Shiao, E., Cardote, T., Tallant, C., Pschibul, A., Chan, K-H., Zengerle, M., Garcia, J. R., Kwan, T. T-L., Ferguson, F. M. & Ciulli, A. 31 Oct 2014 In : Science. 346, 6209, p. 638-641 4 p.

    Research output: Contribution to journalArticle

  25. Binding hotspots of BAZ2B bromodomain: histone interaction revealed by solution NMR driven docking

    Ferguson, F. M., Dias, D. M., Rodrigues, J. P. G. L. M., Wienk, H., Boelens, R., Bonvin, A. M. J. J., Abell, C. & Ciulli, A. 28 Oct 2014 In : Biochemistry. 53, 42, p. 6706-6716 11 p.

    Research output: Contribution to journalArticle

  26. Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities

    Galdeano , C., Gadd, M. S., Soares, P., Scaffidi, S., Van Molle, I., Birced, I., Hewitt, S., Dias, D. M. & Ciulli, A. 23 Oct 2014 In : Journal of Medicinal Chemistry. 57, 20, p. 8657-8663 7 p.

    Research output: Contribution to journalArticle

  27. Characterization of a melamino nitroheterocycle as a potential lead for the treatment of human African trypanosomiasis

    Giordani, F., Buschini, A., Baliani, A., Kaiser, M., Brun, R., Barrett, M. P., Pellacani, C., Poli, P. & Gilbert, I. H. Oct 2014 In : Antimicrobial Agents and Chemotherapy. 58, 10, p. 5747-5757 11 p.

    Research output: Contribution to journalArticle

  28. Elevated O-GlcNAc levels activate epigenetically repressed genes and delay mouse ES cell differentiation without affecting naive to primed cell transition

    Speakman, C. M., Domke, T. C. E., Wongpaiboonwattana, W., Sanders, K., Mudaliar, M., van Aalten, D. M. F., Barton, G. J. & Stavridis, M. P. Oct 2014 In : Stem Cells. 32, 10, p. 2605-2615

    Research output: Contribution to journalArticle

  29. Missing pieces of an ancient puzzle: evolution of the Eukaryotic Membrane-Trafficking System

    Schlacht, A., Herman, E. K., Klute, M. J., Field, M. C. & Dacks, J. B. Oct 2014 In : Cold Spring Harbor Perspectives in Biology. 6, 10, a016048

    Research output: Contribution to journalArticle

  30. The design and synthesis of potent and selective inhibitors of trypanosoma brucei glycogen synthase kinase 3 for the treatment of human African trypanosomiasis

    Urich, R., Grimaldi, R., Luksch, T., Frearson, J. A., Brenk, R. & Wyatt, P. G. 25 Sep 2014 In : Journal of Medicinal Chemistry. 57, 18, p. 7536-7549 14 p.

    Research output: Contribution to journalArticle

  31. Reproducible Automated Phosphopeptide Enrichment using Magnetic TiO2 and Ti-IMAC

    Tape, C. J., Worboys, J. D., Sinclair, J., Gourlay, R., Vogt, J., McMahon (Broster), K. M., Trost, M., Lauffenburger, D. A., Lamont, D. J. & Jørgensen, C. 18 Sep 2014 In : Analytical Chemistry. ASAP

    Research output: Contribution to journalArticle

  32. 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. 17 Sep 2014 In : Journal of Biomolecular Screening.

    Research output: Contribution to journalArticle

  33. Loss of glial neurofascin155 delays developmental synapse elimination at the neuromuscular junction

    Roche, S. L., Sherman, D. L., Dissanayake, K., Soucy, G., Desmazieres, A., Lamont, D. J., Peles, E., Julien, J-P., Wishart, T. M., Ribchester, R. R., Brophy, P. J. & Gillingwater, T. H. 17 Sep 2014 In : Journal of Neuroscience. 34, 38, p. 12904-12918 15 p.

    Research output: Contribution to journalArticle

  34. Structures of bacterial kynurenine formamidase reveal a crowded binuclear zinc catalytic site primed to generate a potent nucleophile

    Díaz-Sáez, L., Srikannathasan, V., Zoltner, M. & Hunter, W. N. 15 Sep 2014 In : Biochemical Journal. 462, 3, p. 581-589 9 p.

    Research output: Contribution to journalArticle

  35. A target repurposing approach identifies N-myristoyltransferase as a new candidate drug target in filarial nematodes

    Galvin, B. D., Li, Z., Villemaine, E., Poole, C. B., Chapman, M. S., Pollastri, M. P., Wyatt, P. G. & Carlow, C. K. S. Sep 2014 In : PLoS Neglected Tropical Diseases. 8, 9, 13 p.e3145

    Research output: Contribution to journalArticle

  36. ATP7B activity is stimulated by PKCɛ in porcine liver

    Cardoso, L. H. D., Britto Borges, T., Vieyra, A. & Lowe, J. Sep 2014 In : International Journal of Biochemistry & Cell Biology. 54, p. 60-67 8 p.

    Research output: Contribution to journalArticle

  37. Crystal structure and mechanistic investigation of the twister ribozyme

    Liu, Y., Wilson, T. J., McPhee, S. A. & Lilley, D. M. J. Sep 2014 In : Nature Chemical Biology. 10, 9, p. 739-744 6 p.

    Research output: Contribution to journalArticle

  38. Heterogeneity in ess transcriptional organization and variable contribution of the Ess/Type VII protein secretion system to virulence across closely related Staphylocccus aureus strains

    Kneuper, H., Cao, Z. P., Twomey, K. B., Zoltner, M., Jäger, F., Cargill, J. S., Chalmers, J., van der Kooi-Pol, M. M., van Dijl, J. M., Ryan, R. P., Hunter, W. N. & Palmer, T. Sep 2014 In : Molecular Microbiology. 93, 5, p. 928-943 15 p.

    Research output: Contribution to journalArticle

  39. Quantification of biliary excretion and sinusoidal excretion of 5(6)-carboxy-2',7'-dichlorofluorescein (CDF) in cultured hepatocytes isolated from Sprague Dawley, Wistar and Mrp2-deficient Wistar (TR-) rats

    Ellis, L. C. J., Grant, M. H., Hawksworth, G. M. & Weaver, R. J. Sep 2014 In : Toxicology in Vitro. 28, 6, p. 1165-1175 11 p.

    Research output: Contribution to journalArticle

  40. Screening-based discovery of Aspergillus fumigatus plant-type chitinase inhibitors

    Lockhart, D. E. A., Schuettelkopf, A., Blair, D. E. & van Aalten, D. M. F. 25 Aug 2014 In : FEBS Letters. 588, 17, p. 3282-3290 9 p.

    Research output: Contribution to journalArticle

  41. A structural and biochemical model of processive chitin synthesis

    Dorfmueller, H. C., Ferenbach, A. T., Borodkin, V. S. & van Aalten, D. M. F. 15 Aug 2014 In : Journal of Biological Chemistry. 289, p. 23020-23028 9 p.

    Research output: Contribution to journalArticle

  42. Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1

    Khalaf, A. I., Huggan, J. K., Suckling, C. J., Gibson, C. L., Stewart, K., Giordani, F., Barrett, M. P., Wong, P. E., Barrack, K. L. & Hunter, W. N. 14 Aug 2014 In : Journal of Medicinal Chemistry. 57, 15, p. 6479-6494 16 p.

    Research output: Contribution to journalArticle

  43. Major transcriptome re-organisation and abrupt changes in signalling, cell cycle and chromatin regulation at neural differentiation in vivo

    Olivera-Martinez, I., Schurch, N., Li, R., Song, J., Halley, P. A., Das, R. M., Burt, D. W., Barton, G. J. & Storey, K. G. Aug 2014 In : Development. 141, 16, p. 3266-3276 11 p.

    Research output: Contribution to journalArticle

  44. Identification of sVSG117 as an immunodiagnostic antigen and evaluation of a dual-antigen lateral flow test for the diagnosis of human african trypanosomiasis

    Sullivan, L., Fleming, J., Sastry, L., Mehlert, A., Wall, S. J. & Ferguson, M. A. J. 17 Jul 2014 In : PLoS Neglected Tropical Diseases. 8, 7, p. e2976

    Research output: Contribution to journalArticle

  45. Molecular cloning and functional characterization of components of the capsule biosynthesis complex of Neisseria meningitidis serogroup A: toward in vitro vaccine production

    Fiebig, T., Freiberger, F., Pinto, V., Romano, M. R., Black, A., Litschko, C., Bethe, A., Yashunsky, D., Adamo, R., Nikolaev, A., Berti, F. & Gerardy-Schahn, R. 11 Jul 2014 In : Journal of Biological Chemistry. 289, 28, p. 19395-19407 13 p.

    Research output: Contribution to journalArticle

  46. Antigenic variation in African trypanosomes

    Horn, D. Jul 2014 In : Molecular and Biochemical Parasitology. 195, 2, p. 123-129 7 p.

    Research output: Contribution to journalArticle

  47. C-reactive protein is essential for innate resistance to pneumococcal infection

    Simons, J. P., Loeffler, J. M., Al-Shawi, R., Ellmerich, S., Hutchinson, W. L., Tennent, G. A., Petrie, A., Raynes, J. G., de Souza, J. B., Lawrence, R. A., Read, K. D. & Pepys, M. B. Jul 2014 In : Immunology. 142, 3, p. 414-420 7 p.

    Research output: Contribution to journalArticle

  48. Filaggrin-stratified transcriptomic analysis of pediatric skin identifies mechanistic pathways in patients with atopic dermatitis

    Cole, C., Kroboth, K., Schurch, N. J., Sandilands, A., Sherstnev, A., O'Regan, G. M., Watson, R. M., McLean, W. H. I., Barton, G. J., Irvine, A. D. & Brown, S. J. Jul 2014 In : Journal of Allergy and Clinical Immunology. 134, 1, p. 82-91 10 p.

    Research output: Contribution to journalArticle

  49. Validity of ligand efficiency metrics

    Murray, C. W., Erlanson, D. A., Hopkins, A. L., Keserü, G. M., Leeson, P. D., Rees, D. C., Reynolds, C. H. & Richmond, N. J. 12 Jun 2014 In : ACS Medicinal Chemistry Letters. 5, 6, p. 616-618 3 p.

    Research output: Contribution to journalArticle

  50. Glycogen Synthase Kinase (GSK) 3β phosphorylates and protects nuclear myosin 1c from proteasome-mediated degradation to activate rDNA transcription in early G1 cells

    Sarshad, A. A., Corcoran, M., Al-Muzzaini, B., Borgonovo-Brandter, L., Von Euler, A., Lamont, D., Visa, N. & Percipalle, P. 5 Jun 2014 In : PLoS Genetics. 10, 6, 17 p.e1004390

    Research output: Contribution to journalArticle

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