David Gray

2025

Characterisation of RNA guanine-7 methyltransferase (RNMT) using a small molecule approach

Pearson, L.-A., Petit, A.-P., Mendoza Martinez, C., Bellany, F., Lin, D., Niven, S., Swift, R., Eadsforth, T., Fyfe, P., Paul, M., Postis, V., Hu, X., Cowling, V. & Gray, D. (Lead / Corresponding author), 17 Feb 2025, In: Biochemical Journal. 482, 4, p. 209-224 16 p., BCJ20240608.

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

Open Access

File

9 Downloads (Pure)

Pharmacological and structural understanding of the Trypanosoma cruzi proteasome provides key insights for developing site-specific inhibitors

Eadsforth, T., Torrie, L., Rowland, P., Edgar, E. V., MacLean, L., Paterson, C., Robinson, D. A., Shepherd, S. M., Thomas, J., Thomas, M., Gray, D., Postis, V. & De Rycker, M. (Lead / Corresponding author), Jan 2025, In: Journal of Biological Chemistry. 301, 1, 17 p., 108049.

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

Open Access

File

2 Citations (Scopus)

15 Downloads (Pure)

2024

Application of an NMR/Crystallography Fragment Screening Platform for the Assessment and Rapid Discovery of New HIV-CA Binding Fragments

Lang, S., Fletcher, D. A., Petit, A.-P., Luise, N., Fyfe, P., Zuccotto, F., Porter, D., Hope, A., Bellany, F., Kerr, C., Mackenzie, C. J., Wyatt, P. G. & Gray, D. W. (Lead / Corresponding author), 2 Jul 2024, In: ChemMedChem. 19, 13, 12 p., e202400025.

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

Open Access

File

1 Citation (Scopus)

85 Downloads (Pure)

HTS Library Plate Rejuvenation Using a DMSO-Rich Atmosphere

Hughes, F., Cookson, A. (Lead / Corresponding author), Tamaki, F., Bailey, C., Gray, D., Wrobel, K., Cookson, K., Bell, S. & Tarver, G., Dec 2024, In: SLAS Technology. 29, 6, 10 p., 100204.

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

Open Access

File

19 Downloads (Pure)

Identification and Validation of Compounds Targeting Leishmania major Leucyl-Aminopeptidase M17

Aguado, M. E., Carvalho, S., Valdés-Tresanco, M. E., Lin, D., Padilla-Mejia, N., Corpas-Lopez, V., Tesařová, M., Lukeš, J., Gray, D., González-Bacerio, J. (Lead / Corresponding author), Wyllie, S. (Lead / Corresponding author) & Field, M. C. (Lead / Corresponding author), 14 Jun 2024, In: ACS Infectious Diseases. 10, 6, p. 2002-2017 16 p.

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

Open Access

File

2 Citations (Scopus)

85 Downloads (Pure)

Identification of a potent and selective LAPTc inhibitor by RapidFire-Mass Spectrometry, with antichagasic activity

Izquierdo, M., Lin, D., O'Neill, S., Webster, L. A., Paterson, C., Thomas, J., Aguado, M. E., Colina Araújo, E., Alpízar-Pedraza, D., Joji, H., MacLean, L., Hope, A., Gray, D. W., Zoltner, M., Field, M. C., González-Bacerio, J. (Lead / Corresponding author) & De Rycker, M. (Lead / Corresponding author), 15 Feb 2024, In: PLoS Neglected Tropical Diseases. 18, 2, 20 p., e0011956.

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

Open Access

File

1 Citation (Scopus)

92 Downloads (Pure)

2023

Assessment of the drugability of initial malaria infection through miniaturized sporozoite assays and high-throughput screening

Miglianico, M., Bolscher, J. M., Vos, M. W., Koolen, K. J. M., de Bruijni, M., Rajagopal, D. S., Chen, E., Kiczun, M., Gray, D., Campo, B., Sauerwein, R. W. & Dechering, K. J. (Lead / Corresponding author), 23 Feb 2023, In: Communications Biology. 6, 10 p., 216.

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

Open Access

File

5 Citations (Scopus)

128 Downloads (Pure)

Design and synthesis of covalent inhibitors of FabA

Martin, J. S., Mackenzie, C. J., Lin, D., Homeyer, N., Gray, D. W., Zuccotto, F. & Gilbert, I. H. (Lead / Corresponding author), 11 Apr 2023, In: ACS Omega. 8, 14, p. 12787–12804 18 p.

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

Open Access

File

1 Citation (Scopus)

128 Downloads (Pure)

Design of the Global Health chemical diversity library v2 for screening against infectious diseases

Wilson, C., Gardner, J. M. F., Gray, D., Baragana, B., Wyatt, P., Cookson, A., Thompson, S., Mendoza Martinez, C., Bodkin, M., Gilbert, I. (Lead / Corresponding author) & Tarver, G. (Lead / Corresponding author), 27 Dec 2023, In: PLoS Neglected Tropical Diseases. 17, 12, 13 p., e0011799.

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

Open Access

File

4 Citations (Scopus)

117 Downloads (Pure)

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. (Lead / Corresponding author), 16 Jul 2021, In: PLoS ONE. 16, 7, 25 p., e0253364.

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

Open Access

File

60 Citations (Scopus)

168 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. (Lead / Corresponding author), Cowling, V. & Fordyce, E. (Lead / Corresponding author), Jul 2021, In: SLAS Discovery. 26, 6, p. 749-756 8 p.

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

Open Access

File

28 Citations (Scopus)

142 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. (Lead / Corresponding author), 25 Mar 2021, In: PLoS ONE. 16, 3, 18 p., e0248119.

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

Open Access

File

2 Citations (Scopus)

167 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. (Lead / Corresponding author), 11 Oct 2021, In: PLoS Neglected Tropical Diseases. 15, 10, 14 p., e0009870.

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

Open Access

File

7 Citations (Scopus)

88 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. (Lead / Corresponding author), 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

14 Citations (Scopus)

135 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. (Lead / Corresponding author), 1 Oct 2020, In: SLAS Discovery. 25, 9, p. 1064-1071 8 p.

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

Open Access

File

13 Citations (Scopus)

71 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. (Lead / Corresponding author), Fairlamb, A. H. & De Rycker, M. (Lead / Corresponding author), 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

13 Citations (Scopus)

156 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. (Lead / Corresponding author), 22 Oct 2020, In: Nature Communications. 11, 16 p., 5348.

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

Open Access

File

47 Citations (Scopus)

282 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. (Lead / Corresponding author), 18 Nov 2019, In: FEBS Journal. 286, 22, p. 4509-4524 16 p.

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

Open Access

File

6 Citations (Scopus)

338 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. (Lead / Corresponding author), Read, K. D. (Lead / Corresponding author) & Miles, T. J. (Lead / Corresponding author), 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

41 Citations (Scopus)

362 Downloads (Pure)

Identification of inhibitors of an unconventional Trypanosoma brucei kinetochore kinase

Torrie, L., Zuccotto, F., Robinson, D., Gray, D., Gilbert, I. (Lead / Corresponding author) & De Rycker, M. (Lead / Corresponding author), 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

4 Citations (Scopus)

175 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. (Lead / Corresponding author), 12 Mar 2019, In: Molecules. 24, 5, p. 1-16 16 p., 996.

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

Open Access

File

7 Citations (Scopus)

219 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. (Lead / Corresponding author), Torrie, L. S. & De Rycker, M. (Lead / Corresponding author), Sept 2019, In: Antimicrobial Agents and Chemotherapy. 63, 9, 15 p., e00309-19.

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

Open Access

File

19 Citations (Scopus)

167 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. (Lead / Corresponding author), 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

111 Citations (Scopus)

628 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. (Lead / Corresponding author), Marco, M. (Lead / Corresponding author) & Wyatt, P. (Lead / Corresponding author), 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

135 Citations (Scopus)

298 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 others, Gray, D., Fairlamb, A., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P., Read, K. (Lead / Corresponding author) & Gilbert, I. (Lead / Corresponding author), 17 Jul 2019, In: ChemMedChem. 14, 14, p. 1329-1335 7 p.

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

Open Access

File

5 Citations (Scopus)

148 Downloads (Pure)

Trypanosoma cruzi phosphomannomutase and guanosine diphosphate-mannose pyrophosphorylase ligandability assessment

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

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

Open Access

File

7 Citations (Scopus)

114 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 others, Berriman, 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. (Lead / Corresponding author), Read, K. D. (Lead / Corresponding author) & Gilbert, I. H. (Lead / Corresponding author), 9 Aug 2018, In: Nature. 560, 7717, p. 192-197 6 p.

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

Open Access

File

126 Citations (Scopus)

978 Downloads (Pure)

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

MacLean, L. (Lead / Corresponding author), Thomas, J., Lewis, M. D., Cotillo, I., Gray, D. (Lead / Corresponding author) & 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

84 Citations (Scopus)

247 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 others, Wernimont, A., Walpole, C., Stacy, R., Barrett, L., Gilbert, I. H. & Van Voorhis, W. C. (Lead / Corresponding author), 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

45 Citations (Scopus)

376 Downloads (Pure)

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

Martins Da Silva, S. J. (Lead / Corresponding author), 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

21 Citations (Scopus)

283 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. (Lead / Corresponding author), 1 Dec 2017, In: SLAS Discovery. 22, 10, p. 1193-1202 10 p.

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

Open Access

File

43 Citations (Scopus)

485 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. (Lead / Corresponding author), 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

11 Citations (Scopus)

228 Downloads (Pure)

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

Baragaña, B., Hallyburton, I., Lee, M., 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. (Lead / Corresponding author) & Gilbert, I. H., 1 Sept 2016, In: Nature. 537, 7618, p. 122 1 p.

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

3 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 others, Gray, D. W., Fairlamb, A. H., Waterson, D., Campbell, S. F., Willis, P., Read, K. D. (Lead / Corresponding author) & Gilbert, I. H. (Lead / Corresponding author), 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

76 Citations (Scopus)

324 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. (Lead / Corresponding author), 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

6 Citations (Scopus)

203 Downloads (Pure)

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

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

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

Open Access

File

61 Citations (Scopus)

231 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 others, Javier Gamo, F., Frearson, J. A., Gray, D. W., Fairlamb, A. H., Winzeler, E. A., Waterson, D., Campbell, S. F., Willis, P., Read, K. D. (Lead / Corresponding author) & Gilbert, I. H. (Lead / Corresponding author), 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

13 Citations (Scopus)

766 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 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. (Lead / Corresponding author) & Gilbert, I. H. (Lead / Corresponding author), 18 Jun 2015, In: Nature. 522, 7556, p. 315-320 6 p.

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

363 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. (Lead / Corresponding author), 25 Sept 2015, In: PLoS Neglected Tropical Diseases. 9, 9, 17 p., e0004094.

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

37 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. (Lead / Corresponding author), Nov 2015, In: ChemMedChem. 10, 11, p. 1809-1820 12 p.

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

14 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 others, Julio Martin, J. (Lead / Corresponding author), 2015, In: Scientific Reports. 5, 12 p., 8771.

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

Open Access

File

224 Citations (Scopus)

402 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. (Lead / Corresponding author), 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

1 Citation (Scopus)

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

8 Citations (Scopus)

233 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. (Lead / Corresponding author), 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

60 Citations (Scopus)

396 Downloads (Pure)

2013

Comparison of a high-throughput high-content intracellular Leishmania donovani assay with an axenic amastigote assay.

De Rycker, M. (Lead / Corresponding author), 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

130 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. (Lead / Corresponding author) & Schneider, G. (Lead / Corresponding author), 2013, In: ACS Chemical Biology. n/a, cb4005063.

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

35 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

45 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

20 Citations (Scopus)

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

De Rycker, M. (Lead / Corresponding author), 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

31 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

11 Citations (Scopus)

Gray, David

Research output

Search results