Gray, David

Research output

Research output per year 1992 2015 2016 2017 2019 2021 2021

• 59 Article
• 3 Comment/debate
• 1 Review article
• 1 Exhibition

Research output per year

Research output per year

Search results

• 2021

  Biochemical characterization of protease activity of Nsp3 from SARS-CoV-2 and its inhibition by nanobodies

  Armstrong, L. A., Lange, S. M., de Cesare, V., Matthews, S. P., Nirujogi, R. S., Cole, I., Hope, A., Cunningham, F., Toth, R., Mukherjee, R., Bojkova, D., Gruber, F., Gray, D., Wyatt, P. G., Cinatl, J., Dikic, I., Davies, P. & Kulathu, Y., 16 Jul 2021, In: PLoS ONE. 16, 7, 25 p., e0253364.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Single-Domain Antibodies 100%
  • SARS Virus 99%
  • Papain 75%
  • Peptide Hydrolases 56%
  • Polyubiquitin 14%
  14 Citations (Scopus)

  49 Downloads (Pure)

• Development of a High-Throughput Screening Assay to Identify Inhibitors of the SARS-CoV-2 Guanine-N7 Methyltransferase Using RapidFire Mass Spectrometry

  Pearson, L-A., Green, C., Lin, D., Petit, A-P., Gray, D., Cowling, V. & Fordyce, E., Jul 2021, In: SLAS Discovery. 26, 6, p. 749-756 8 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • rapidFire Mass Spectrometry 100%
  • High-Throughput Screening Assays 69%
  • Severe Acute Respiratory Syndrome 63%
  • Coronavirus 61%
  • Guanine 58%
  8 Citations (Scopus)

  45 Downloads (Pure)

• Drug screening to identify compounds to act as co-therapies for the treatment of Burkholderia species

  Barker, S., Harding, S. V., Gray, D., Richards, M. I., Atkins, H. S. & Harmer, N. J., 25 Mar 2021, In: PLoS ONE. 16, 3, 18 p., e0248119.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Chloroxine 100%
  • chloroxine 76%
  • Ceftazidime 72%
  • Burkholderia 70%
  • ceftazidime 61%
  2 Citations (Scopus)

  56 Downloads (Pure)

• Live-imaging rate-of-kill compound profiling for Chagas disease drug discovery with a new automated high-content assay

  Svensen, N., Wyllie, S., Gray, D. W. & De Rycker, M., 11 Oct 2021, In: PLoS Neglected Tropical Diseases. 15, 10, 14 p., e0009870.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Chagas Disease 100%
  • Clinical Trials 88%
  • Drug Discovery 86%
  • Parasites 69%
  • Trypanosoma cruzi 67%
  3 Citations (Scopus)

  25 Downloads (Pure)

• Structure-Activity Relationships of Pyrazolo[1,5-a]pyrimidin-7(4H)-ones as Antitubercular Agents

  Oh, S., Libardo, M. D. J., Azeeza, S., Pauly, G. T., Roma, J. S. O., Sajid, A., Tateishi, Y., Duncombe, C., Goodwin, M., Ioerger, T. R., Wyatt, P. G., Ray, P. C., Gray, D. W., Boshoff, H. I. M. & Barry, C. E., 12 Feb 2021, In: ACS Infectious Diseases. 7, 2, p. 479-492 14 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • pyrazolo(1,5-a)pyrimidin-7(4H)-one 100%
  • Antitubercular Agents 61%
  • Structure-Activity Relationship 48%
  • Mycobacterium tuberculosis 39%
  • isoprene 33%
  2 Citations (Scopus)

  34 Downloads (Pure)
• 2020

  Development of a High-Throughput Screening Assay to Identify Inhibitors of the Major M17-Leucyl Aminopeptidase from Trypanosoma cruzi Using RapidFire Mass Spectrometry

  Izquierdo, M., Lin, D., O'Neill, S., Zoltner, M., Webster, L., Hope, A., Gray, D. W., Field, M. C. & González-Bacerio, J., 1 Oct 2020, In: SLAS Discovery. 25, 9, p. 1064-1071 8 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • rapidFire Mass Spectrometry 100%
  • Leucyl Aminopeptidase 74%
  • High-Throughput Screening Assays 69%
  • Trypanosoma cruzi 59%
  • High Throughput Screening 52%
  5 Citations (Scopus)

  23 Downloads (Pure)

• 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 journal › Article › peer-review

  Open Access

  File

  • Methionine-tRNA Ligase 100%
  • Allosteric Site 80%
  • Binding Sites 43%
  • Trypanosoma cruzi 34%
  • Enzymes 25%
  5 Citations (Scopus)

  75 Downloads (Pure)

• Targeting N-myristoylation for therapy of B-cell lymphomas

  Beauchamp, E., Yap, M. C., Iyer, A., Perinpanayagam, M. A., Gamma, J. M., Vincent, K. M., Lakshmanan, M., Raju, A., Tergaonkar, V., Tan, S. Y., Lim, S. T., Dong, W-F., Postovit, L. M., Read, K. D., Gray, D. W., Wyatt, P. G., Mackey, J. R. & Berthiaume, L. G., 22 Oct 2020, In: Nature Communications. 11, 16 p., 5348.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Myristoylation 100%
  • glycylpeptide N-tetradecanoyltransferase 62%
  • B-Cell Lymphoma 61%
  • therapy 56%
  • cancer 55%
  11 Citations (Scopus)

  77 Downloads (Pure)
• 2019

  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 journal › Article › peer-review

  Open Access

  File

  • D-alanylalanine synthetase 100%
  • Burkholderia pseudomallei 74%
  • Drug Target 59%
  • Antimicrobial Agent 36%
  • Chemical Library 35%
  2 Citations (Scopus)

  149 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 othersLowe, 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 journal › Article › peer-review

  Open Access

  File

  • Visceral Leishmaniasis 100%
  • Pipeline 94%
  • Metabolic 66%
  • Solubility 51%
  • Drug 43%
  22 Citations (Scopus)

  202 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 journal › Article › peer-review

  Open Access

  File

  • kinetochores 100%
  • Kinetochores 99%
  • Trypanosoma brucei brucei 98%
  • Trypanosoma brucei 93%
  • phosphotransferases (kinases) 64%
  4 Citations (Scopus)

  112 Downloads (Pure)

• Identification of Leishmania major UDP-Sugar Pyrophosphorylase Inhibitors Using Biosensor-Based Small Molecule Fragment Library Screening

  Prakash, O., Führing, J., Post, J., Shepherd, S. M., Eadsforth, T. C., Gray, D., Fedorov, R. & Routier, F. H., 12 Mar 2019, In: Molecules. 24, 5, p. 1-16 16 p., 996.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Uridine Diphosphate Sugars 100%
  • Small Molecule Libraries 80%
  • Leishmania major 76%
  • Biosensing Techniques 69%
  • UTP-Glucose-1-Phosphate Uridylyltransferase 62%
  6 Citations (Scopus)

  157 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 journal › Article › peer-review

  Open Access

  File

  • High-Throughput Screening Assays 100%
  • Trypanosoma cruzi 85%
  • Proteasome Inhibitors 84%
  • Luminescence 78%
  • Proteasome Endopeptidase Complex 73%
  11 Citations (Scopus)

  99 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 othersHallyburton, 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 journal › Article › peer-review

  Open Access

  File

  • Lysine-tRNA Ligase 100%
  • Cryptosporidiosis 77%
  • cladosporin 62%
  • Cryptosporidium parvum 60%
  • Malaria 52%
  54 Citations (Scopus)

  340 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 othersSantos 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 journal › Article › peer-review

  Open Access

  File

  • Leishmania infantum 100%
  • Visceral Leishmaniasis 89%
  • Proteasome Endopeptidase Complex 76%
  • Leishmania donovani 66%
  • Parasites 60%
  72 Citations (Scopus)

  166 Downloads (Pure)

• 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 othersGray, 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 journal › Article › peer-review

  Open Access

  File

  • Antimalarial 100%
  • Drug Target 95%
  • Mammalian Cell 86%
  • Germ Cells 82%
  • Malaria 76%
  2 Citations (Scopus)

  60 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, 11 p., e01082-19.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • phosphomannomutase 100%
  • Guanosine Diphosphate Mannose 97%
  • mannose 1-phosphate guanylyltransferase 94%
  • Trypanosoma cruzi 68%
  • Chagas Disease 33%
  7 Citations (Scopus)

  81 Downloads (Pure)
• 2018

  Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

  Wyllie, S., Thomas, M., Patterson, S., Crouch, S., De Rycker, M., Lowe, R., Gresham, S., Urbaniak, M. D., Otto, T. D., Stojanovski, L., Simeons, F. R. C., Manthri, S., MacLean, L. M., Zuccotto, F., Homeyer, N., Pflaumer, H., Boesche, M., Sastry, L., Connolly, P., Albrecht, S., & 12 othersBerriman, M., Drewes, G., Gray, D. W., Ghidelli-Disse, S., Dixon, S., Fiandor, J. M., Wyatt, P. G., Ferguson, M. A. J., Fairlamb, A. H., Miles, T. J., Read, K. D. & Gilbert, I. H., 9 Aug 2018, In: Nature. 560, 7717, p. 192-197 6 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Visceral Leishmaniasis 100%
  • Cyclin-Dependent Kinases 95%
  • Pharmaceutical Preparations 33%
  • Toxicology 26%
  • Parasites 22%
  82 Citations (Scopus)

  612 Downloads (Pure)

• Development of Trypanosoma cruzi in vitro assays to identify compounds suitable for progression in Chagas’ disease drug discovery

  MacLean, L., Thomas, J., Lewis, M. D., Cotillo, I., Gray, D. & De Rycker, M., 12 Jul 2018, In: PLoS Neglected Tropical Diseases. 12, 7, p. 1-22 22 p., e0006612.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • posaconazole 100%
  • Trypanosoma cruzi 85%
  • Chagas Disease 84%
  • Drug Discovery 72%
  • Parasites 50%
  49 Citations (Scopus)

  158 Downloads (Pure)
• 2017

  Biochemical and Structural Characterization of Selective Allosteric Inhibitors of the Plasmodium falciparum Drug Target, Prolyl-tRNA-synthetase

  Nakazawa Hewitt, S., Dranow, D. M., Horst, B. G., Abendroth, J. A., Forte, B., Hallyburton, I., Jansen, C., Baragana, B., Choi, R., Rivas, K., Hulverson, M. A., Dumais, M., Edwards, T. E., Lorimer, D. D., Fairlamb, A., Gray, D., Read, K., Lehane, A. M., Kirk, K., Myler, P. J., & 6 othersWernimont, A., Walpole, C., Stacy, R., Barrett, L., Gilbert, I. H. & Van Voorhis, W. C., 13 Jan 2017, In: ACS Infectious Diseases. 3, 1, p. 34-44 11 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • prolyl T RNA synthetase 100%
  • Pharmaceutical Chemistry 71%
  • Plasmodium falciparum 54%
  • Malaria 47%
  • halofuginone 45%
  30 Citations (Scopus)

  307 Downloads (Pure)

• Drug discovery for male subfertility using high-throughput screening: a new approach to an unsolved problem

  Martins Da Silva, S. J., Brown, S. G., Sutton, K., King, L. V., Ruso, H., Gray, D. W., Wyatt, P. G., Kelly, M. C., Barratt, C. L. R. & Hope, A. G., May 2017, In: Human Reproduction. 32, 5, p. 974-984 11 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Male Infertility 100%
  • Drug Discovery 89%
  • Spermatozoa 80%
  • Sperm-Ovum Interactions 32%
  • Fluorescence 26%
  15 Citations (Scopus)

  183 Downloads (Pure)

• Identifying Inhibitors of Inflammation: A Novel High-Throughput MALDI-TOF Screening Assay for Salt-Inducible Kinases (SIKs)

  Heap, R. E., Hope, A. G., Pearson, L-A., Reyskens, K. M. S. E., McElroy, S. P., Hastie, C. J., Porter, D. W., Arthur, J. S. C., Gray, D. W. & Trost, M., 1 Dec 2017, In: SLAS Discovery. 22, 10, p. 1193-1202 10 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Matrix-Assisted Laser Desorption-Ionization Mass Spectrometry 100%
  • Salts 73%
  • Phosphotransferases 64%
  • Time-of-Flight Mass Spectrometry 62%
  • Inflammation 49%
  34 Citations (Scopus)

  375 Downloads (Pure)
• 2016

  A substrate mimic allows high-throughput assay of the FabA protein and consequently the identification of a novel inhibitor of Pseudomonas aeruginosa FabA

  Moynié, L., Hope, A. G., Finzel, K., Schmidberger, J., Leckie, S. M., Schneider, G., Burkart, M. D., Smith, A. D., Gray, D. W. & Naismith, J. H., 16 Jan 2016, In: Journal of Molecular Biology. 428, 1, p. 108-120 13 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • 2-acetamidoethanethiol 100%
  • human FASN protein 47%
  • Pseudomonas aeruginosa 45%
  • Acyl Carrier Protein 38%
  • Enzyme Assays 27%
  3 Citations (Scopus)

  179 Downloads (Pure)

• 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 othersNorval, 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 journal › Article › peer-review

  • Antimalarials 100%
  • Drug Discovery 92%
  • Biological Science Disciplines 56%
  • Proteins 33%
  2 Citations (Scopus)

• Discovery of a quinoline-4-carboxamide derivative with a novel mechanism of action, multistage antimalarial activity, and potent in vivo efficacy

  Baragaña, B., Norcross, N. R., Wilson, C., Porzelle, A., Hallyburton, I., Grimaldi, R., Osuna-Cabello, M., Norval, S., Riley, J., Stojanovski, L., Simeons, F. R. C., Wyatt, P. G., Delves, M. J., Meister, S., Duffy, S., Avery, V. M., Winzeler, E. A., Sinden, R. E., Wittlin, S., Frearson, J. A., & 7 othersGray, D. W., Fairlamb, A. H., Waterson, D., Campbell, S. F., Willis, P., Read, K. D. & Gilbert, I. H., 10 Nov 2016, In: Journal of Medicinal Chemistry. 59, 21, p. 9672-9685 14 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • DDD107498 100%
  • quinoline-4-carboxamide 98%
  • Peptide Elongation Factor 2 64%
  • Antiplasmodic 58%
  • Antimalarials 46%
  45 Citations (Scopus)

  220 Downloads (Pure)

• Identification of novel inhibitors of the type I interferon induction pathway using cell-based high-throughput screening

  Gage, Z. O., Vasou, A., Gray, D. W., Randall, R. E. & Adamson, C. S., 1 Oct 2016, In: Journal of Biomolecular Screening. 21, 9, p. 978-988 11 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Interferon Type I 100%
  • High Throughput Screening 90%
  • Interferons 77%
  • Molecule 29%
  • enhanced green fluorescent protein 26%
  5 Citations (Scopus)

  165 Downloads (Pure)

• Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade

  De Rycker, M., Thomas, J., Riley, J., Brough, S. J., Miles, T. J. & Gray, D. W., 15 Apr 2016, In: PLoS Neglected Tropical Diseases. 10, 4, 19 p., e0004584.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Trypanosoma cruzi 100%
  • Chagas Disease 98%
  • Libraries 73%
  • Clemastine 71%
  • azelastine 66%
  45 Citations (Scopus)

  169 Downloads (Pure)

• Trisubstituted Pyrimidines as Efficacious and Fast-acting Antimalarials

  Norcross, N. R., Baragana, B., Wilson, C., Hallyburton, I., Osuna-Cabello, M., Norval, S., Riley, J., Stojanovski, L., Simeons, F. R. C., Porzelle, A., Grimaldi, R., Wittlin, S., Duffy, S., Avery, V. M., Meister, S., Sanz, L., Jimenez-Diaz, B., Angulo-Barturen, I., Ferrer, S., Santos Marinez, M., & 10 othersJavier Gamo, F., Frearson, J. A., Gray, D. W., Fairlamb, A. H., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P., Read, K. D. & Gilbert, I. H., 14 Jul 2016, In: Journal of Medicinal Chemistry. 59, 13, p. 6101-6120 20 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Pyrimidines 100%
  • Antimalarial 83%
  • Antimalarials 77%
  • Clearance 75%
  • Cytochrome P450 74%
  9 Citations (Scopus)

  327 Downloads (Pure)
• 2015

  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 othersNorval, 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 journal › Article › peer-review

  • DDD107498 100%
  • Antimalarials 46%
  • Malaria 25%
  • Parasites 23%
  • Peptide Elongation Factor 2 21%
  254 Citations (Scopus)

• Development and validation of a novel Leishmania donovani screening cascade for high-throughput screening using a novel axenic assay with high predictivity of Leishmanicidal intracellular activity

  Nühs, A., De Rycker, M., Manthri, S., Comer, E., Scherer, C. A., Schreiber, S. L., Ioset, J-R. & Gray, D. W., 25 Sep 2015, In: PLoS Neglected Tropical Diseases. 9, 9, 17 p., e0004094.

  Research output: Contribution to journal › Article › peer-review

  • Leishmania donovani 100%
  • Parasites 61%
  • drug 50%
  • Leishmania 42%
  • Drug Discovery 38%
  33 Citations (Scopus)

• 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 journal › Article › peer-review

  • 1H-pyrazolo(3,4-b)pyridine 100%
  • Trypanosoma brucei brucei 84%
  • Protein Kinases 59%
  • Pyridine 45%
  • Growth 32%
  11 Citations (Scopus)

• 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 othersJulio Martin, J., 2015, In: Scientific Reports. 5, 12 p., 8771.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • High-Throughput Screening Assays 100%
  • Leishmania donovani 95%
  • Trypanosoma brucei brucei 91%
  • Trypanosoma cruzi 85%
  • Cytochromes 80%
  180 Citations (Scopus)

  312 Downloads (Pure)
• 2014

  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 journal › Article › peer-review

• High-throughput chemical screening for antivirulence developmental phenotypes in Trypanosoma brucei.

  McGregor, P., Ivens, A., Shave, S., Collie, I., Gray, D., Auer, M. & Matthews, K. R., Mar 2014, In: Eukaryotic Cell. 13, 3, p. 412-426 15 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • Trypanosoma brucei brucei 100%
  • Trypanosoma 64%
  • Phenotype 46%
  • Parasites 42%
  • Small Molecule Libraries 36%
  8 Citations (Scopus)

  194 Downloads (Pure)

• Identification of small molecule inhibitors of pre-mRNA splicing

  Pawellek, A., McElroy, S., Samatov, T., Mitchell, L., Woodland, A., Ryder, U., Gray, D., Lührmann, R. & Lamond, A. I., 12 Dec 2014, In: Journal of Biological Chemistry. 289, 50, p. 34683-34698 16 p.

  Research output: Contribution to journal › Article › peer-review

  Open Access

  File

  • RNA Precursors 100%
  • Spliceosomes 48%
  • Molecule 30%
  • RNA Splicing 23%
  • HEK293 Cells 19%
  51 Citations (Scopus)

  296 Downloads (Pure)
• 2013

  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., Jul 2013, In: Antimicrobial Agents and Chemotherapy. 57, 7, p. 2913-2922 10 p.

  Research output: Contribution to journal › Article › peer-review

  • Leishmania donovani 100%
  • Parasites 61%
  • Neglected Diseases 32%
  • Visceral Leishmaniasis 30%
  • Leishmania 28%
  117 Citations (Scopus)

• Discovery of an Allosteric Inhibitor Binding Site in 3-Oxo-acyl-ACP Reductase from Pseudomonas aeruginosa

  Cukier, C. D., Hope, A. G., Elamin, A. A., Moynie, L., Schnell, R., Schach, S., Kneuper, H., Singh, M., Naismith, J. H., Lindqvist, Y., Gray, D. W. & Schneider, G., 2013, In: ACS Chemical Biology. n/a, cb4005063.

  Research output: Contribution to journal › Article › peer-review

  • Acyl Carrier Protein 100%
  • Pseudomonas aeruginosa 59%
  • Oxidoreductases 58%
  • Fatty Acids 54%
  • Fatty Acid 51%
  25 Citations (Scopus)
• 2012

  Allosteric competitive inhibitors of the glucose-1-phosphate Thymidylyltransferase (RmlA) from  seudomonas aeruginosa

  Alphey, M. S., Pirrie, L., Torrie, L. S., Boulkeroua, W. A., Gardiner, M., Sarkar, A., Maringer, M., Oehlmann, W., Brenk, R., Scherman, M. S., McNeil, M., Rejzek, M., Field, R. A., Singh, M., Gray, D., Westwood, N. J. & Naismith, J. H., 2012, In: ACS Chemical Biology.

  Research output: Contribution to journal › Article › peer-review

  • glucose-1-phosphate thymidylyltransferase 100%
  • glucose-1-phosphate 74%
  • Rhamnose 65%
  • Crystallography 48%
  • High Throughput Screening 48%
  32 Citations (Scopus)

• Assessment of pseudomonas aeruginosa N-5,N-10-methylenetetrahydrofolate dehydrogenase - cyclohydrolase as a potential antibacterial drug target

  Eadsforth, T. C., Gardiner, M., Maluf, F. V., McElroy, S., James, D., Frearson, J., Gray, D. & Hunter, W. N., 2012, In: PLoS ONE. 7, 4, p. - 11 p., e35973.

  Research output: Contribution to journal › Article › peer-review

  • Methylenetetrahydrofolate Dehydrogenase (NADP) 100%
  • Pseudomonas aeruginosa 51%
  • Enzymes 30%
  • Pharmaceutical Preparations 22%
  • Drug Discovery 18%
  16 Citations (Scopus)

• A static-cidal assay for Trypanosoma brucei to aid hit prioritisation for progression into drug discovery programmes

  De Rycker, M., O'Neill, S., Joshi, D., Campbell, L., Gray, D. W. & Fairlamb, A. H., 29 Nov 2012, In: PLoS Neglected Tropical Diseases. 6, 11, p. e1932

  Research output: Contribution to journal › Article › peer-review

  • Trypanosoma brucei brucei 100%
  • Trypanosoma 96%
  • Drug Discovery 79%
  • African Trypanosomiasis 54%
  • Vector Borne Diseases 53%
  27 Citations (Scopus)
• 2010

  The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

  Rimland, J., Dunne, A., Hunjan, S. S., Sasse, R., Uings, I., Montanari, D., Caivano, M., Shah, P., Standing, D., Gray, D., Brown, D., Cairns, W., Trump, R., Smith, P. W., Bertheleme, N., D'Alessandro, P., Gul, S., Vimal, M., Smith, D. N. & Watson, S. P., Apr 2010, In: Bioorganic & Medicinal Chemistry Letters. 20, 7, p. 2340-3 4 p.

  Research output: Contribution to journal › Article › peer-review

  • Glucocorticoid Receptor Antagonist 100%
  • Structure-Activity Relationship 60%
  • Glucocorticoid Receptors 57%
  • Antagonist 47%
  • Molecule 17%
  9 Citations (Scopus)
• 2008

  Synthesis of 3-alkyl naphthalenes as novel estrogen receptor ligands

  Fang, J., Akwabi-Ameyaw, A., Britton, J. E., Katamreddy, S. R., Navas III, F., Miller, A. B., Williams, S. P., Gray, D. W., Orband-Miller, L. A., Shearin, J. & Heyer, D., 15 Sep 2008, In: Bioorganic & Medicinal Chemistry Letters. 18, 18, p. 5075-5077 3 p.

  Research output: Contribution to journal › Article › peer-review

  • Naphthalenes 100%
  • Estrogen 56%
  • Estrogen Receptors 49%
  • Naphthalene 47%
  • Alkynes 43%
  22 Citations (Scopus)
• 2007

  Design and synthesis of an array of selective androgen receptor modulators

  Trump, R. P., Blanc, J-B. E., Stewart, E. L., Brown, P. J., Caivano, M., Gray, D. W., Hoekstra, W. J., Willson, T. M., Han, B. & Turnbull, P., 2007, In: Journal of Combinatorial Chemistry. 9, 1, p. 107-14 8 p.

  Research output: Contribution to journal › Article › peer-review

  • Selective Androgen Receptor Modulator 100%
  • Androgen 75%
  • Androgen Receptor Antagonist 34%
  • Receptor Modulator 31%
  • Agent Interacting With Transmitter, Hormone or Drug Receptor 22%
  20 Citations (Scopus)

• Pharmacological properties of the enhanced-affinity glucocorticoid fluticasone furoate in vitro and in an in vivo model of respiratory inflammatory disease

  Salter, M., Biggadike, K., Matthews, J. L., West, M. R., Haase, M. V., Farrow, S. N., Uings, I. J. & Gray, D. W., 2007, In: American Journal of Physiology: Lung Cellular and Molecular Physiology. 293, 3, p. L660-7 8 p.

  Research output: Contribution to journal › Article › peer-review

  • fluticasone furoate 100%
  • Glucocorticoids 53%
  • Pharmacology 38%
  • In Vitro Techniques 25%
  • Glucocorticoid Receptors 14%
  141 Citations (Scopus)
• 2006

  Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines

  Wiethe, R. W., Stewart, E. L., Drewry, D. H., Gray, D. W., Mehbob, A. & Hoekstra, W. J., 15 Jul 2006, In: Bioorganic & Medicinal Chemistry Letters. 16, 14, p. 3777-9 3 p.

  Research output: Contribution to journal › Article › peer-review

  • Steroid Hormone 100%
  • Steroid Receptors 92%
  • Agent Interacting With Transmitter, Hormone or Drug Receptor 86%
  • Progesterone Receptors 82%
  • Drug Development 74%
  13 Citations (Scopus)

• GW627368X ((N-{2-[4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo[f]isoindol-2-yl)phenyl]acetyl} benzene sulphonamide): a novel, potent and selective prostanoid EP4 receptor antagonist

  Wilson, R. J., Giblin, G. M. P., Roomans, S., Rhodes, S. A., Cartwright, K-A., Shield, V. J., Brown, J., Wise, A., Chowdhury, J., Pritchard, S., Coote, J., Noel, L. S., Kenakin, T., Burns-Kurtis, C. L., Morrison, V., Gray, D. W. & Giles, H., 2006, In: British Journal of Pharmacology. 148, 3, p. 326-339 14 p.

  Research output: Contribution to journal › Article › peer-review

  • N-(2-(4-(4,9-diethoxy-1-oxo-1,3-dihydro-2H-benzo(f)isoindol-2-yl)phenyl)acetyl)benzene sulphonamide 100%
  • Receptors, Prostaglandin E, EP4 Subtype 78%
  • Thromboxane Receptors 28%
  • Prostaglandins 22%
  • 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid 10%
  67 Citations (Scopus)
• 2005

  Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists

  Jones, D. G., Liang, X., Stewart, E. L., Noe, R. A., Kallander, L. S., Madauss, K. P., Williams, S. P., Thompson, S. K., Gray, D. W. & Hoekstra, W. J., 2005, In: Bioorganic & Medicinal Chemistry Letters. 15, 13, p. 3203-6 4 p.

  Research output: Contribution to journal › Article › peer-review

  • Mifepristone 100%
  • Agent Interacting With Transmitter, Hormone or Drug Receptor 63%
  • Progesterone Receptors 59%
  • Abortifacient 26%
  • Ketosteroids 23%
  29 Citations (Scopus)

• Evaluation of cell-based assays for steroid nuclear receptors delivered by recombinant baculoviruses

  Katso, R. M., Parham, J. H., Caivano, M., Clay, W. C., Condreay, J. P., Gray, D. W., Lindley, K. M., Mason, S. J., Rieger, J., Wakes, N. C., Cairns, W. J. & Merrihew, R. V., 2005, In: Journal of Biomolecular Screening. 10, 7, p. 715-24 10 p.

  Research output: Contribution to journal › Article › peer-review

  • progesterone receptor B 100%
  • Baculoviridae 74%
  • Steroid Receptors 73%
  • progesterone receptor A 68%
  • Cytoplasmic and Nuclear Receptors 63%
  19 Citations (Scopus)
• 2004

  Functional pharmacology of human prostanoid EP2 and EP4 receptors

  Wilson, R. J., Rhodes, S. A., Wood, R. L., Shield, V. J., Noel, L. S., Gray, D. W. & Giles, H., 6 Oct 2004, In: European Journal of Pharmacology. 501, 1-3, p. 49-58 10 p.

  Research output: Contribution to journal › Article › peer-review

  • Receptors, Prostaglandin E, EP2 Subtype 100%
  • Receptors, Prostaglandin E, EP4 Subtype 96%
  • Prostaglandins 54%
  • Pharmacology 38%
  • butaprost 29%
  48 Citations (Scopus)
• 1999

  Receptors mediating CGRP-induced relaxation in the rat isolated thoracic aorta and porcine isolated coronary artery differentiated by h(alpha) CGRP(8-37)

  Wisskirchen, F. M., Gray, D. W. & Marshall, I., Sep 1999, In: British Journal of Pharmacology. 128, 2, p. 283-92 10 p.

  Research output: Contribution to journal › Article › peer-review

  • calcitonin gene-related peptide (8-37) 100%
  • Calcitonin Gene-Related Peptide Receptors 96%
  • Calcitonin Gene-Related Peptide 75%
  • Thoracic Aorta 64%
  • Coronary Vessels 52%
  40 Citations (Scopus)