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Biological Chemistry and Drug Discovery

  1. Sterol 14α-demethylase mutation leads to amphotericin B resistance in Leishmania mexicana

    Mwenechanya, R., Kovářová, J., Dickens, N. J., Manikhandan, M., Herzyk, P., Vincent, I. M., Weidt, S. K., Burgess, K. E., Burchmore, R. J. S., Pountain, A. W., Smith, T. K., Creek, D. J., Kim, D. H., Lepesheva, G. I. & Barrett, M. P. 16 Jun 2017 In : PLoS Neglected Tropical Diseases. 11, 6, p. 1-21 21 p., e0005649

    Research output: Contribution to journalArticle

  2. Erythematous nodes, urticarial rash and arthralgias in a large pedigree with NLRC4-related autoinflammatory disease, expansion of the phenotype

    Volker-Touw, C. M. L., de Koning, H. D., Giltay, J., de Kovel, C., van Kempen, T. S., Oberndorff, K., Boes, M., van Steensel, M. A. M., van Well, G. T. J., Blokx, W. A. M., Schalkwijk, J., Simon, A., Frenkel, J. & van Gijn, M. E. 8 Dec 2016 In : British Journal of Dermatology. 176, 1, p. 244-248 5 p.

    Research output: Contribution to journalLetter

  3. Isolated recessive nail dysplasia caused by FZD6 mutations: report of three families and review of the literature

    Kasparis, C., Reid, D., Wilson, N. J., Okur, V., Cole, C., Hansen, C. D., Bosse, K., Betz, R. C., Khan, M. & Smith, F. J. D. Dec 2016 In : Clinical and Experimental Dermatology. 41, 8, p. 884-889 6 p.

    Research output: Contribution to journalArticle

  4. MSAViewer: interactive JavaScript visualization of multiple sequence alignments

    Yachdav, G., Wilzbach, S., Rauscher, B., Sheridan, R., Sillitoe, I., Procter, J., Lewis, S. E., Rost, B. & Goldberg, T. 15 Nov 2016 In : Bioinformatics. 32, 22, p. 3501-3503 3 p.

    Research output: Contribution to journalArticle

  5. Mutations in POGLUT1 in Galli-Galli/Dowling Degos-disease

    Wilson, N. J., Cole, C., Kroboth, K., Hunter, W. N., Mann, J. A., Irwin McLean, W. H., Kernland Lang, K., Beltraminelli, H., Sabroe, R. A., Tiffin, N., Sobey, G. J., Borradori, L., Simpson, E. & Smith, F. J. D. 24 Sep 2016 In : British Journal of Dermatology. 176, p. 270-274 5 p.

    Research output: Contribution to journalLetter

  6. Heat Shock Factor 1 is a Substrate for p38 Mitogen-Activated Protein Kinases

    Dayalan Naidu, S., Sutherland, C., Zhang, Y., Risco, A., de la Vega, L., Caunt, C. J., Hastie, C. J., Lamont, D. J., Torrente, L., Chowdhry, S., Benjamin, I. J., Keyse, S. M., Cuenda, A. & Dinkova-Kostova, A. T. 15 Sep 2016 In : Molecular and Cellular Biology. 36, 18, p. 2403-2417 15 p.

    Research output: Contribution to journalArticle

  7. Corrigendum: A novel multiple-stage antimalarial agent that inhibits protein synthesis

    Baragaña, 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. , Luksch, T. & 44 others 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., Jiménez-Díaz, M. B., Sanz, L. M., 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., Fairlamb, A. H., Willis, P. A., Rayner, J. C., Fidock, D. A., Read, K. D. & Gilbert, I. H. 25 May 2016 In : Nature. 537, 7618, p. 122 1 p.

    Research output: Contribution to journalArticle

  8. Phosphoinositides, kinases and adaptors coordinating endocytosis in Trypanosoma brucei

    Manna, P. T. & Field, M. C. 12 Apr 2016 In : Communicative & Integrative Biology. 8, 6, p. e1082691-1-e1082691-4 4 p., e1082691

    Research output: Contribution to journalArticle

  9. Keratin 12 missense mutation induces the unfolded protein response and apoptosis in meesmann epithelial corneal dystrophy

    Allen, E. H. A., Courtney, D. G., Atkinson, S. D., Moore, J. E., Mairs, L., Poulsen, E. T., Schiroli, D., Maurizi, E., Cole, C., Hickerson, R. P., James, J., Murgatroyd, H., Smith, F. J. D., MacEwen, C., Enghild, J. J., Nesbit, M. A., Leslie Pedrioli, D. M., McLean, W. H. I. & Moore, C. B. T. 15 Mar 2016 In : Human Molecular Genetics. 25, 6, p. 1176-1191 16 p., ddw001

    Research output: Contribution to journalArticle

  10. 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

  11. 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. 25 Feb 2016 In : Journal of Medicinal Chemistry. 59, 4, p. 1492-1500 9 p.

    Research output: Contribution to journalArticle

  12. 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

  13. Clinical features and HLA association of 5-aminosalicylate (5-ASA)-induced nephrotoxicity in inflammatory bowel disease

    Heap, G. A. , So, K. , Weedon, M. , Edney, N. , Bewshea, C. , Singh, A. , Annese, V. , Beckly, J. , Buurman, D. , Chaudhary, R. , Cole, A. T. , Cooper, S. C. , Creed, T. , Cummings, F. , de Boer, N. K. , D'Inca, R. , Daneshmend, T. K. , Delaney, M. , Dhar, A. , Direkze, N. & 43 others Dunckley, P., Gaya, D. R., Gearry, R., Gore, S., Halfvarson, J., Hart, A. L., Hawkey, C. J., Hoentjen, F., Iqbal, T., Irving, P., Lal, S., Lawrence, I., Lees, C. W., Lewis, S., Lockett, M., Mann, S., Mansfield, J. C., Mowat, C., Muller, F., Murray, C., Orchard, T., Parkes, M., Phillips, R., Pollok, R., Radford-Smith, G. L., Sebastian, S., Sen, S., Shirazi, T., Silverberg, M. S., Solomon, L., Sturniolo, G. C., Thomas, M., Tremelling, M., Tsianos, E. V., Watts, D., Weaver, S., Wesley, E., Holden, A., D'Souza, R., Mulgrew, C. J., Oram, R. A., Weersma, R. K. & Ahmad, T. 1 Feb 2016 In : Journal of Crohn's and Colitis. 10, 2, p. 149-158 10 p.

    Research output: Contribution to journalArticle

  14. 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 5 p.

    Research output: Contribution to journalArticle

  15. 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

  16. 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

  17. 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

  18. 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

  19. 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

  20. 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

  21. 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

  22. 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

  23. 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

  24. 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

  25. 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

  26. 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

  27. 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

  28. 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

  29. 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

  30. 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

  31. 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

  32. 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

  33. 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

  34. 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

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

    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. , Luksch, T. & 44 others 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., Fairlamb, A. H., Willis, P. A., Rayner, J. C., Fidock, D. A., Read, K. D. & Gilbert, I. H. 18 Jun 2015 In : Nature. 522, 7556, p. 315-320 6 p.

    Research output: Contribution to journalArticle

  36. 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

  37. 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

  38. 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

  39. 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

  40. 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

  41. 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

  42. 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

  43. 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

  44. 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

  45. 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

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

    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. , Fairlamb, A. H. , Ferguson, M. A. J. & 21 others 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

  47. 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

  48. 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

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