Drug Discovery Unit

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2020

8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi

Fersing, C., Boudot, C., Castera-Ducros, C., Pinault, E., Hutter, S., Paoli-Lombardo, R., Primas, N., Pedron, J., Seguy, L., Bourgeade-Delmas, S., Sournia-Saquet, A., Stigliani, J. L., Brossas, J. Y., Paris, L., Valentin, A., Wyllie, S., Fairlamb, A. H., Boutet-Robinet, É., Corvaisier, S., Since, M. & 8 others, Malzert-Fréon, A., Destere, A., Mazier, D., Rathelot, P., Courtioux, B., Azas, N., Verhaeghe, P. & Vanelle, P., 8 Jul 2020, In : European Journal of Medicinal Chemistry. 202, 15 p., 112558.

Research output: Contribution to journalArticle

A platform for target prediction of phenotypic screening hit molecules

Homeyer, N., van Deursen, R., Ochoa-Montaño, B., Heikamp, K., Ray, P., Zuccotto, F., Blundell, T. L. & Gilbert, I. H., Mar 2020, In : Journal of Molecular Graphics & Modelling. 95, p. 1-9 9 p., 107485.

Research output: Contribution to journalArticle

Open Access
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Computer-driven development of an in silico tool for finding selective histone deacetylase 1 inhibitors

Sirous, H., Campiani, G., Brogi, S., Calderone, V. & Chemi, G., 22 Apr 2020, In : Molecules. 25, 8, p. 1-20 20 p., 1952.

Research output: Contribution to journalArticle

Open Access
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15 Downloads (Pure)
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3 Citations (Scopus)
364 Downloads (Pure)

Discovery and Optimization of a Compound Series Active against Trypanosoma cruzi, the Causative Agent of Chagas Disease

Harrison, J. R., Sarkar, S., Hampton, S., Riley, J., Stojanovski, L., Sahlberg, C., Appelqvist, P., Erath, J., Mathan, V., Rodriguez, A., Kaiser, M., Pacanowska, D. G., Read, K. D., Johansson, N. G. & Gilbert, I. H., 26 Mar 2020, In : Journal of Medicinal Chemistry. 63, 6, p. 3066-3089 24 p.

Research output: Contribution to journalArticle

Discovery of an Allosteric Binding Site in Kinetoplastid Methionyl-tRNA Synthetase

Torrie, L. S., Robinson, D. A., Thomas, M. G., Hobrath, J. V., Shepherd, S. M., Post, J. M., Ko, E. J., Ferreira, R. A., Mackenzie, C. J., Wrobel, K., Edwards, D. P., Gilbert, I. H., Gray, D. W., Fairlamb, A. H. & De Rycker, M., 8 May 2020, In : ACS Infectious Diseases. 6, 5, p. 1044-1057 14 p.

Research output: Contribution to journalArticle

Open Access
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Instability of aquaglyceroporin 2 leads to drug resistance in Trypanosoma brucei

Quintana, J. F., Bueren-Calabuig, J., Zuccotto, F., Zoltner, M., Canavate Del Pino, R., de Koning, H. P., Horn, D. & Field, M. C., 9 Jul 2020, In : PLoS Neglected Tropical Diseases. 14, 7, 26 p., e0008458.

Research output: Contribution to journalArticle

Open Access

Metabolism of bifenthrin, β-cyfluthrin, λ-cyhalothrin, cyphenothrin and esfenvalerate by rat and human cytochrome P450 and carboxylesterase enzymes

Hedges, L., Brown, S., MacLeod, A. K., Moreau, M., Yoon, M., Creek, M. R., Osimitz, T. G. & Lake, B. G., 16 Jul 2020, In : Xenobiotica. 9 p.

Research output: Contribution to journalArticle

PE/PPE proteins mediate nutrient transport across the outer membrane of Mycobacterium tuberculosis

Wang, Q., Boshoff, H. I. M., Harrison, J. R., Ray, P. C., Green, S. R., Wyatt, P. G. & Barry, C. E., 6 Mar 2020, In : Science. 367, 6482, p. 1147-1151 5 p.

Research output: Contribution to journalArticle

Setting our sights on infectious diseases

De Rycker, M., Horn, D., Aldridge, B., Amewu, R. K., Barry, C. E., Buckner, F. S., Cook, S., Ferguson, M. A. J., Gobeau, N., Herrmann, J., Herrling, P., Hope, W., Keiser, J., Lafuente-Monasterio, M. J., Leeson, P. D., Leroy, D., Manjunatha, U. H., McCarthy, J., Miles, T. J., Mizrahi, V. & 17 others, Moshynets, O., Niles, J., Overington, J. P., Pottage, J., Rao, S. P. S., Read, K. D., Ribeiro, I., Silver, L. L., Southern, J., Spangenberg, T., Sundar, S., Taylor, C., Van Voorhis, W. C., White, N. J., Wyllie, S., Wyatt, P. G. & Gilbert, I. H., 10 Jan 2020, In : ACS Infectious Diseases. 6, p. 3-13 11 p.

Research output: Contribution to journalArticle

Open Access
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Substrate and stereochemical control of peptidoglycan crosslinking by transpeptidation by Escherichia coli PBP1B

Catherwood, A. C., Lloyd, A. J., Tod, J. A., Chauhan, S., Slade, S. E., Walkowiak, G., Galley, N. F., Punekar, A., Smart, K., Rea, D., Evans, N. D., Chappell, M. J., Roper, D. I. & Dowson, C. G., 18 Mar 2020, In : Journal of the American Chemical Society. 142, 11, p. 5034-5048 15 p.

Research output: Contribution to journalArticle

1 Citation (Scopus)

Targeting a critical step in fungal hexosamine biosynthesis

Lockhart, D., Stanley, M., Raimi, O., Robinson, D., Boldovjakova, D., Squair, D., Ferenbach, A., Fang, W. & van Aalten, D., 26 Jun 2020, In : Journal of Biological Chemistry. 295, 26, p. 8678-8691 14 p.

Research output: Contribution to journalArticle

Open Access
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Targeting the rheumatoid arthritis synovial fibroblast via cyclin dependent kinase inhibition: An early phase trial

Siebert, S., Pratt, A. G., Stocken, D. D., Morton, M., Cranston, A., Cole, M., Frame, S., Buckley, C. D., Ng, W-F., Filer, A., McInnes, I. B. & Isaacs, J. D., 26 Jun 2020, In : Medicine. 99, 26, 9 p., e20458.

Research output: Contribution to journalArticle

Open Access
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The efficacy of a topical formulation of selamectin plus sarolaner in preventing the development of a macrocyclic lactone-resistant strain of Dirofilaria immitis in cats

Pullins, A., McTier, T. L., Mahabir, S., DeRose, G. & Hedges, L., Jun 2020, In : Veterinary Parasitology. 282, p. 1-7 7 p., 109122.

Research output: Contribution to journalArticle

The Qi Site of Cytochrome b is a Promiscuous Drug Target in Trypanosoma cruzi and Leishmania donovani: ACS Infectious Diseases

Wall, R. J., Carvalho, S., Milne, R., Bueren-Calabuig, J. A., Moniz, S., Cantizani-Perez, J., MacLean, L., Kessler, A., Cotillo, I., Sastry, L., Manthri, S., Patterson, S., Zuccotto, F., Thompson, S., Martin, J., Marco, M., Miles, T. J., De Rycker, M., Thomas, M. G., Fairlamb, A. H. & 2 others, Gilbert, I. H. & Wyllie, S., 13 Mar 2020, In : ACS Infectious Diseases. 6, 3, p. 515-528 14 p.

Research output: Contribution to journalArticle

Open Access
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1 Citation (Scopus)
40 Downloads (Pure)
2019

A brain-permeable inhibitor of the neurodegenerative disease target kynurenine 3-monooxygenase prevents accumulation of neurotoxic metabolites

Zhang, S., Sakuma, M., Deora, G. S., Levy, C. W., Klausing, A., Breda, C., Read, K. D., Edlin, C. D., Ross, B. P., Wright Muelas, M., Day, P. J., O'Hagan, S., Kell, D. B., Schwarcz, R., Leys, D., Heyes, D. J., Giorgini, F. & Scrutton, N. S., 24 Jul 2019, In : Communications Biology. 2, p. 1-10 10 p., 271.

Research output: Contribution to journalArticle

Open Access
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2 Citations (Scopus)
78 Downloads (Pure)

A Continuous Flow Strategy for the Facile Synthesis and Elaboration of Semi-Saturated Heterobicyclic Fragments

Luise, N., Wyatt, E. W., Tarver, G. & Wyatt, P., 14 Feb 2019, In : European Journal of Organic Chemistry. 2019, 6, p. 1341-1349 9 p.

Research output: Contribution to journalArticle

Open Access
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Burkholderia pseudomallei D-alanine-D-alanine ligase: detailed characterisation and assessment of a potential antibiotic drug target

Díaz‐Sáez, L., Torrie, L. S., McElroy, S. P., Gray, D. & Hunter, W. M., 18 Nov 2019, In : FEBS Journal. 286, 22, p. 4509-4524 16 p.

Research output: Contribution to journalArticle

Open Access
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1 Citation (Scopus)
82 Downloads (Pure)

Characterising Covalent Warhead Reactivity

Martin, J., Mackenzie, C., Fletcher, D. & Gilbert, I., 15 May 2019, In : Bioorganic & Medicinal Chemistry. 27, 10, p. 2066-2074 9 p.

Research output: Contribution to journalArticle

Open Access
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7 Citations (Scopus)
180 Downloads (Pure)

Chemical disarming of isoniazid resistance in Mycobacterium tuberculosis

Flentie, K., Harrison, G. A., Tükenmez, H., Livny, J., Good, J. A. . D., Sarkar, S., Zhu, D. X., Kinsella, R. L., Weiss, L. A., Solomon, S. D., Schene, M. E., Hansen, M. R., Cairns, A. G., Kulén, M., Wixe, T., Lindgren, A. E. G., Chorell, E., Bengtsson, C., Krishnan, K. S., Hultgren, S. J. & 3 others, Larsson, C., Almqvist, F. & Stallings, C. L., 21 May 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 21, p. 10510-10517 8 p.

Research output: Contribution to journalArticle

Open Access
8 Citations (Scopus)
Open Access
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2 Citations (Scopus)
123 Downloads (Pure)

Diversity-oriented synthesis of bicyclic fragments containing privileged azines

Luise, N. & Wyatt, P. G., 15 Jan 2019, In : Bioorganic & Medicinal Chemistry Letters. 29, 2, p. 248-251 4 p.

Research output: Contribution to journalArticle

Open Access
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2 Citations (Scopus)
146 Downloads (Pure)

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

Thomas, M. G., De Rycker, M., Ajakane, M., Albrecht, S., Álvarez-Pedraglio, A. I., Boesche, M., Brand, S., Campbell, L., Cantizani-Perez, J., Cleghorn, L. A. T., Copley, R. C. B., Crouch, S. D., Daugan, A., Drewes, G., Ferrer, S., Ghidelli-Disse, S., Gonzalez, S., Gresham, S. L., Hill, A. P., Hindley, S. J. & 32 others, Lowe, R. M., MacKenzie, C. J., MacLean, L., Manthri, S., Martin, F., Miguel-Siles, J., Nguyen, V. L., Norval, S., Osuna-Cabello, M., Woodland, A., Patterson, S., Pena, I., Quesada-Campos, M. T., Reid, I. H., Revill, C., Riley, J., Ruiz-Gomez, J. R., Shishikura, Y., Simeons, F. R. C., Smith, A., Smith, V. C., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Underwood, T., Gray, D. W., Fiandor, J. M., Gilbert, I. H., Wyatt, P. G., Read, K. D. & Miles, T. J., 14 Feb 2019, In : Journal of Medicinal Chemistry. 62, 3, p. 1180-1202 23 p.

Research output: Contribution to journalArticle

Open Access
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4 Citations (Scopus)
26 Downloads (Pure)

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase

Torrie, L., Zuccotto, F., Robinson, D., Gray, D., Gilbert, I. & De Rycker, M., 31 May 2019, In : PLoS ONE. 14, 5, p. 1-16 16 p., e0217828.

Research output: Contribution to journalArticle

Open Access
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2 Citations (Scopus)
104 Downloads (Pure)

Identification of Novel Trypanosoma cruzi Proteasome Inhibitors Using a Luminescence-Based High-Throughput Screening Assay

Zmuda, F., Sastry, L., Shepherd, S. M., Jones, D., Scott, A., Craggs, P. D., Cortes, A., Gray, D. W., Torrie, L. S. & De Rycker, M., Sep 2019, In : Antimicrobial Agents and Chemotherapy. 63, 9, 15 p., e00309-19.

Research output: Contribution to journalArticle

Open Access
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3 Citations (Scopus)
93 Downloads (Pure)

Influence of type 2 diabetes on muscle deoxygenation during ramp incremental cycle exercise

Gildea, N., Rocha, J., McDermott, A., O'Shea, D., Green, S. & Egaña, M., Nov 2019, In : Respiratory Physiology & Neurobiology. 269, p. 1-7 7 p., 103258.

Research output: Contribution to journalArticle

1 Citation (Scopus)

Inhibition of CorA dependent Magnesium Homeostasis is cidal in Mycobacterium tuberculosis

Park, Y., Ahn, Y-M., Jonnala, S., Oh, S., Fisher, J. M., Goodwin, M. B., Loerger, T. R., Via, L. E., Bayliss, T., Green, S. R., Ray, P. C., Wyatt, P. G., Barry, C. E. & Boshoff, H. I., 23 Sep 2019, In : Antimicrobial Agents and Chemotherapy. 63, 10, p. 1-14 14 p., e01006-19.

Research output: Contribution to journalArticle

Open Access
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Loss of CRMP2 O-GlcNAcylation leads to reduced novel object recognition performance in mice

Muha, V., Williamson, R., Hills, R., McNeilly, A., McWilliams, T. G., Alonso, J., Schimpl, M., Leney, A. C., Heck, A. J. R., Sutherland, C., Read, K., McCrimmon, R., Brooks, S. P. & van Aalten, D., 27 Nov 2019, In : Open Biology. 9, 11, p. 1-15 15 p.

Research output: Contribution to journalArticle

Open Access
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1 Citation (Scopus)
63 Downloads (Pure)

Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis

Baragaña, B., Forte, B., Choi, R., Nakazawa Hewitt, S., Bueren-Calabuig, J. A., Pisco, J. P., Peet, C., Dranow, D. M., Robinson, D. A., Jansen, C., Norcross, N. R., Vinayak, S., Anderson, M., Brooks, C. F., Cooper, C. A., Damerow, S., Delves, M., Dowers, K., Duffy, J., Edwards, T. E. & 57 others, Hallyburton, I., Horst, B. G., Hulverson, M. A., Ferguson, L., Jiménez-Díaz, M. B., Jumani, R. S., Lorimer, D. D., Love, M. S., Maher, S., Matthews, H., McNamara, C. W., Miller, P., O'Neill, S., Ojo, K. K., Osuna-Cabello, M., Pinto, E., Post, J., Riley, J., Rottmann, M., Sanz, L. M., Scullion, P., Sharma, A., Shepherd, S. M., Shishikura, Y., Simeons, F. R. C., Stebbins, E. E., Stojanovski, L., Straschil, U., Tamaki, F. K., Tamjar, J., Torrie, L. S., Vantaux, A., Witkowski, B., Wittlin, S., Yogavel, M., Zuccotto, F., Angulo-Barturen, I., Sinden, R., Baum, J., Gamo, F-J., Mäser, P., Kyle, D. E., Winzeler, E. A., Myler, P. J., Wyatt, P. G., Floyd, D., Matthews, D., Sharma, A., Striepen, B., Huston, C. D., Gray, D. W., Fairlamb, A. H., Pisliakov, A. V., Walpole, C., Read, K. D., Van Voorhis, W. C. & Gilbert, I. H., 2 Apr 2019, In : Proceedings of the National Academy of Sciences. 116, 14, p. 7015-7020 6 p.

Research output: Contribution to journalArticle

Open Access
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11 Citations (Scopus)
243 Downloads (Pure)

Metabolism of deltamethrin and cis- and trans-permethrin by human expressed cytochrome P450 and carboxylesterase enzymes

Hedges, L., Brown, S., MacLeod, A. K., Vardy, A., Doyle, E., Song, G., Moreau, M., Yoon, M., Osimitz, T. G. & Lake, B. G., 4 Jun 2019, In : Xenobiotica. 49, 5, p. 521-527 7 p.

Research output: Contribution to journalArticle

6 Citations (Scopus)

Methyl sulfonamide substituents improve the pharmacokinetic properties of bicyclic 2-pyridone based: Chlamydia trachomatis inhibitors

Kulén, M., Núñez-Otero, C., Cairns, A. G., Silver, J., Lindgren, A. E. G., Wede, E., Singh, P., Vielfort, K., Bahnan, W., Good, J. A. D., Svensson, R., Bergström, S., Gylfe, Å. & Almqvist, F., 2019, In : MedChemComm. 10, 11, p. 1966-1987 22 p.

Research output: Contribution to journalArticle

Open Access
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Novel pharmacological actions of Trequinsin Hydrochloride improve human sperm cell motility and function

McBrinn, R. C., Fraser, J., Hope, A. G., Gray, D. W., Barratt, C. L. R., Martins da Silva, S. J. & Brown, S. G., Dec 2019, In : British Journal of Pharmacology. 176, 23, p. 4521-4536 16 p.

Research output: Contribution to journalArticle

Open Access
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Optimisation of a Key Cross-Coupling Reaction Towards the Synthesis of a Promising Antileishmanial Compound

Velasco, R. F., Guerrero, C., Fra, G., Moure, A., Miguel-Siles, J., Quesada-Campos, M. T., Ruiz-Gomez, J. R., Gilbert, I. H., Thomas, M. G. & Miles, T. J., 2 May 2019, In : Tetrahedron Letters. 60, 18, p. 1243-1247 5 p.

Research output: Contribution to journalArticle

Open Access
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1 Citation (Scopus)
141 Downloads (Pure)
Open Access
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9 Citations (Scopus)
174 Downloads (Pure)

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

Wyllie, S., Brand, S., Thomas, M., De Rycker, M., Chung, C-W., Peña, I., Bingham, R., Bueren-Calabuig, J., Cantizani, J., Cebrian, D., Craggs, P. D., Ferguson, L., Goswami, P., Hobrath, J., Howe, J., Jeacock, L., Ko, E. J., Korczynska, J., MacLean, L., Manthri, S. & 29 others, Santos Martinez, M., Mata-Cantero, L., Moniz, S., Nuhs, A., Osuna-Cabello, M., Pinto, E., Riley, J., Robinson, S., Rowland, P., Simeons, F., Shishikura, Y., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Viayna Gaza, E., Wall, R., Zuccotto, F., Horn, D., Ferguson, M., Fairlamb, A., Fiandor, J. M., Martín, J., Gray, D., Miles, T. J., Gilbert, I., Read, K., Marco, M. & Wyatt, P., 7 May 2019, In : Proceedings of the National Academy of Sciences. 116, 19, p. 9318-9323 6 p., 201820175.

Research output: Contribution to journalArticle

Open Access
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19 Citations (Scopus)
132 Downloads (Pure)

Pyridine-Fused 2-Pyridones via Povarov and A3 Reactions: Rapid Generation of Highly Functionalized Tricyclic Heterocycles Capable of Amyloid Fibril Binding

Singh, P., Adolfsson, D. E., Ådén, J., Cairns, A. G., Bartens, C., Brännström, K., Olofsson, A. & Almqvist, F., 5 Apr 2019, In : Journal of Organic Chemistry. 84, 7, p. 3887-3903 17 p.

Research output: Contribution to journalArticle

3 Citations (Scopus)

Research techniques made simple: An introduction to drug discovery for dermatology

Bell, M., Webster, L. & Woodland, A., Nov 2019, In : Journal of Investigative Dermatology. 139, 11, p. 2252-2257.e1 6 p.

Research output: Contribution to journalArticle

Sertraline Delivered in Phosphatidylserine Liposomes Is Effective in an Experimental Model of Visceral Leishmaniasis

Romanelli, M. M., da Costa-Silva, T. A., Cunha-Junior, E., Dias Ferreira, D., Guerra, J. M., Galisteo, A. J., Pinto, E. G., Barbosa, L. R. S., Torres-Santos, E. C. & Tempone, A. G., 29 Oct 2019, In : Frontiers in Cellular and Infection Microbiology. 9, p. 1-12 12 p., 353.

Research output: Contribution to journalArticle

Open Access
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Structure‐based design, synthesis and biological evaluation of bis‐tetrahydropyran furan acetogenin mimics targeting the trypanosomatid F1 component of ATP synthase

Zacharova, M. K., Tulloch, L. B., Gould, E. R., Fraser, A. L., King, E. F., Menzies, S. K., Smith, T. K. & Florence, G. J., 1 Sep 2019, In : European Journal of Organic Chemistry. 2019, 31-32, p. 5434-5440 7 p.

Research output: Contribution to journalArticle

Open Access
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86 Downloads (Pure)

Structure-guided enhancement of selectivity of chemical probe inhibitors targeting bacterial seryl-tRNA synthetase

Cain, R., Salimraj, R., Punekar, A., Belini, D., Fishwick, C. W. G., Czaplewski, L., Scott, D. J., Harris, G., Dowson, C. G., Lloyd, A. J. & Roper, D. I., 18 Oct 2019, In : Journal of Medicinal Chemistry. 62, 21, p. 9703-9717 15 p.

Research output: Contribution to journalArticle

Substituted Aminoacetamides as Novel Leads for Malaria Treatment

Norcross, N., Wilson, C., Baragana, B., Hallyburton, I., Osuna-Cabello, M., Norval, S., Riley, J., Fletcher, D., Sinden, R., Delves, M. J., Ruecker, A., Duffy, S., Meister, S., Antonova-Koch, Y., Crespo, B., de Cózar, C., Sanz, L., Gamo, F-J., Avery, V. M., Frearson, J. A. & 8 others, Gray, D., Fairlamb, A., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P., Read, K. & Gilbert, I., 17 Jul 2019, In : ChemMedChem. 14, 14, p. 1329-1335 7 p.

Research output: Contribution to journalArticle

Open Access
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2 Citations (Scopus)
49 Downloads (Pure)

Synthesis of Densely Functionalized N-Alkenyl 2-Pyridones via Benzyne-Induced Ring Opening of Thiazolino-Fused 2-Pyridones

Singh, P., Cairns, A. G., Adolfsson, D. E., Ådén, J., Sauer, U. H. & Almqvist, F., 16 Sep 2019, In : Organic Letters. 21, 17, p. 6946-6950 5 p.

Research output: Contribution to journalArticle

1 Citation (Scopus)

Translation of Diverse Aramid- And 1,3-Dicarbonyl-peptides by Wild Type Ribosomes in Vitro

Ad, O., Hoffman, K. S., Cairns, A. G., Featherston, A. L., Miller, S. J., Söll, D. & Schepartz, A., 24 Jul 2019, In : ACS Central Science. 5, 7, p. 1289-1294 6 p.

Research output: Contribution to journalArticle

Open Access
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10 Citations (Scopus)
5 Downloads (Pure)

Trypanosoma cruzi phosphomannomutase and guanosine diphosphate-mannose pyrophosphorylase ligandability assessment

Zmuda, F., Shepherd, S. M., Ferguson, M. A. J., Gray, D. W., Torrie, L. S. & De Rycker, M., Oct 2019, In : Antimicrobial Agents and Chemotherapy. 63, 10, p. 1-11 11 p., e01082-19.

Research output: Contribution to journalArticle

Open Access
File
1 Citation (Scopus)
83 Downloads (Pure)

Viral mimetic priming enhances α-synuclein-induced degeneration: Implications for Parkinson's disease

Olsen, L. K., Cairns, A. G., Ådén, J., Moriarty, N., Cabre, S., Alamilla, V. R., Almqvist, F., Dowd, E. & McKernan, D. P., Aug 2019, In : Brain, Behavior, and Immunity. 80, p. 525-535 11 p.

Research output: Contribution to journalArticle

2 Citations (Scopus)
2018

2,4-Diamino-6-methylpyrimidines for the potential treatment of Chagas’ disease

Thomas, M. G., De Rycker, M., Cotillo Torrejon, I., Thomas, J., Riley, J., Spinks, D., Read, K. D., Miles, T. J., Gilbert, I. H. & Wyatt, P. G., 1 Oct 2018, In : Bioorganic & Medicinal Chemistry Letters. 28, 18, p. 3025-3030 6 p.

Research output: Contribution to journalArticle

Open Access
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50 Downloads (Pure)

2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization

Murugesan, D., Ray, P. C., Bayliss, T., Prosser, G. A., Harrison, J. R., Green, K., Soares De Melo, C., Feng, T. S., Street, L. J., Chibale, K., Warner, D. F., Mizrahi, V., Epemolu, O., Scullion, P., Ellis, L., Riley, J., Shishikura, Y., Ferguson, L., Osuna-Cabello, M., Read, K. D. & 10 others, Green, S. R., Lamprecht, D. A., Steyn, A. J. C., Ioerger, T. R., Sacchettini, J., Rhee, K. Y., Arora, K., Barry, C. E., Wyatt, P. G. & Boshoff, H. I. M., 8 Jun 2018, In : ACS Infectious Diseases. 4, 6, p. 954-969 16 p.

Research output: Contribution to journalArticle

Open Access
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10 Citations (Scopus)
141 Downloads (Pure)

3-Fluoro-4-hydroxyprolines: Synthesis, conformational analysis and stereoselective recognition by the VHL E3 ubiquitin ligase for targeted protein degradation

Testa, A., Lucas, X., Castro, G., Chan, K. H., Wright, J., Runcie, A., Gadd, M., Harrison, W. T. A., Ko, E. J., Fletcher, D. & Ciulli, A., 25 Jul 2018, In : Journal of the American Chemical Society. 140, 29, p. 9299-9313 15 p.

Research output: Contribution to journalArticle

Open Access
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26 Citations (Scopus)
152 Downloads (Pure)