Read, Kevin

Professor

20082022
If you made any changes in Pure these will be visible here soon.

Research Output 2008 2019

Filter
Article
2019
29 Downloads (Pure)
Open Access
File
Lysosphingolipid Receptors
Drug Discovery
Modulators
Skin
Pharmaceutical Preparations
3 Citations (Scopus)

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 journalArticle

Visceral Leishmaniasis
Leishmania major
Leishmania donovani
Standard of Care
Solubility
49 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 journalArticle

Open Access
File
Lysine-tRNA Ligase
Cryptosporidiosis
Cryptosporidium parvum
Malaria
Plasmodium falciparum
40 Downloads (Pure)
Open Access
File
Leishmania donovani
Pharmacology
Parasites
Enzymes
Pharmaceutical Preparations
1 Citation (Scopus)
27 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 journalArticle

Open Access
File
Leishmania infantum
Visceral Leishmaniasis
Proteasome Endopeptidase Complex
Leishmania donovani
Parasites

Substituted aminoacetamides as novel leads for malaria

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., 12 Jun 2019, In : ChemMedChem. 16 p.

Research output: Contribution to journalArticle

Open Access
File
Antimalarials
Germ Cells
Malaria
Pharmacokinetics
Plasmodium falciparum
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

Chagas Disease
Parasites
Nifurtimox
Trypanosoma cruzi
Screening
2 Citations (Scopus)
61 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 othersGreen, 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
File
Quinazolinones
Structure-Activity Relationship
Mycobacterium tuberculosis
Adenosine Triphosphate
Allosteric Site
3 Citations (Scopus)
42 Downloads (Pure)

A Molecular Hybridization Approach for the Design of Potent, Highly Selective, and Brain-Penetrant N-Myristoyltransferase Inhibitors

Harrison, J. R., Brand, S., Smith, V., Robinson, D. A., Thompson, S., Smith, A., Davies, K., Mok, N., Torrie, L. S., Collie, I., Hallyburton, I., Norval, S., Simeons, F. R. C., Stojanovski, L., Frearson, J. A., Brenk, R., Wyatt, P. G., Gilbert, I. H. & Read, K. D., 12 Sep 2018, In : Journal of Medicinal Chemistry. 61, 18, p. 8374–8389 16 p.

Research output: Contribution to journalArticle

Open Access
File
African Trypanosomiasis
Trypanosoma brucei brucei
Crystallography
Central Nervous System Diseases
Peripheral Nervous System
2 Citations (Scopus)
52 Downloads (Pure)
Open Access
File
Metabolites
Drug Users
Metabolism
Opioid Analgesics
Urine
11 Citations (Scopus)
102 Downloads (Pure)

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 journalArticle

Open Access
File
Visceral Leishmaniasis
Cyclin-Dependent Kinases
Pharmaceutical Preparations
Toxicology
Parasites
1 Citation (Scopus)
39 Downloads (Pure)
Open Access
File
Lysosphingolipid Receptors
Modulators
Esters
Plasma (human)
Butyrylcholinesterase
19 Citations (Scopus)
62 Downloads (Pure)
Open Access
File
Ubiquitin-Protein Ligases
Structure-Activity Relationship
Proteolysis
Ligands
Tumor Suppressor Proteins
4 Citations (Scopus)
77 Downloads (Pure)

Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles

Zhang, N., Zoltner, M., Leung, K-F., Scullion, P., Hutchinson, S., Del Pino, R. C., Vincent, I. M., Zhang, Y-K., Freund, Y. R., Alley, M. R. K., Jacobs, R. T., Read, K. D., Barrett, M. P., Horn, D. & Field, M. C., 9 Feb 2018, In : PLoS Pathogens. 14, 2, p. 1-25 25 p., e1006850.

Research output: Contribution to journalArticle

Open Access
File
Trypanocidal Agents
Neglected Diseases
African Trypanosomiasis
Amine Oxidase (Copper-Containing)
Aldehyde Dehydrogenase
56 Downloads (Pure)

Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB

Cleghorn, L., Ray, P., Odingo, J., Kumar, A., Wescott, H., Korkegian, A., Masquelin, T., Lopez Moure, A., Wilson, C., Davis, S., Huggett, M., Turner, P., Smith, A., Epemolu, R., Zuccotto, F., Riley, J., Scullion, S., Shishikura, Y., Ferguson, L., Rullas, J. & 6 othersGuijarro, L., Read, K., Green, S., Hipskind, P., Parish, T. & Wyatt, P., 26 Jun 2018, In : Journal of Medicinal Chemistry.

Research output: Contribution to journalArticle

Open Access
File
Thiophenes
Morpholinos
Mycobacterium tuberculosis
Electron Transport Complex IV
Structure-Activity Relationship
4 Citations (Scopus)
75 Downloads (Pure)

Optimization of a “Bump-and-Hole” Approach to Allele-Selective BET Bromodomain Inhibition

Runcie, A., Zengerle, M., Chan, K. H., Testa, A., Van Beurden, L., Baud, M., Epemolu, R., Ellis, L., Read, K., Coulthard, V., Brien, A. & Ciulli, A., 9 Mar 2018, In : Chemical Science. 2018, 9, p. 2387-2634 18 p., 2452.

Research output: Contribution to journalArticle

Open Access
File
Benzodiazepines
Leucine
Proteins
Cell proliferation
Valine
1 Citation (Scopus)
53 Downloads (Pure)

Pharmacokinetics of β-Lactam Antibiotics: Clues from the Past to Help Discover Long-Acting Oral Drugs in the Future

Smith, P. W., Zuccotto, F., Bates, R. H., Martinez-Martinez, M. S., Read, K. D., Peet, C. & Epemolu, O., 24 Aug 2018, In : ACS Infectious Diseases. 9 p.

Research output: Contribution to journalArticle

Open Access
File
Lactams
Pharmacokinetics
Anti-Bacterial Agents
Pharmaceutical Preparations
Drug Discovery
8 Citations (Scopus)
43 Downloads (Pure)

The Anthelmintic Drug Niclosamide and Its Analogues Activate the Parkinson's Disease Associated Protein Kinase PINK1

Barini, E., Miccoli, A., Tinarelli, F., Mulholland, K., Kadri, H., Khanim, F., Stojanovski, L., Read, K. D., Burness, K., Blow, J. J., Mehellou, Y. & Muqit, M. M. K., 2 Mar 2018, In : ChemBioChem. 19, 5, p. 425-429 5 p.

Research output: Contribution to journalArticle

Open Access
File
Niclosamide
Anthelmintics
Protein Kinases
Parkinson Disease
Mitochondrial Membrane Potential
2017
11 Citations (Scopus)
191 Downloads (Pure)

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 journalArticle

Open Access
File
Pharmaceutical Chemistry
Plasmodium falciparum
Malaria
Crystallography
X Ray Crystallography
2 Citations (Scopus)
95 Downloads (Pure)

Chemical Validation of Methionyl tRNA Synthetase (MetRS) as a Druggable Target in Leishmania donovani

Torrie, L., Brand, S., Robinson, D., Ko, E. J., Stojanovski, L., Simeons, F. R. C., Wyllie, S., Thomas, J., Ellis, L., Osuna-Cabello, M., Epemolu, R., Nuehs, A., Riley, J., MacLean, L., Manthri, S., Read, K., Gilbert, I., Fairlamb, A. & De Rycker, M., Oct 2017, In : ACS Infectious Diseases. 3, 10, p. 718-727 10 p.

Research output: Contribution to journalArticle

Open Access
File
Methionine-tRNA Ligase
Leishmania donovani
Leishmania
Methionine
Animal Models
3 Citations (Scopus)
95 Downloads (Pure)

Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

Bayliss, T., Robinson, D., Smith, V., Brand, S., McElroy, S., Torrie, L., Mpamhanga, C., Norval, S., Stojanovski, L., Brenk, R., Frearson, J., Read, K., Gilbert, I. & Wyatt, P., 14 Dec 2017, In : Journal of Medicinal Chemistry. 60, 23, p. 9790-9806 17 p.

Research output: Contribution to journalArticle

Open Access
File
African Trypanosomiasis
Brain
Pharmaceutical Preparations
glycylpeptide N-tetradecanoyltransferase
DDD 85646
7 Citations (Scopus)
72 Downloads (Pure)

Discovery and Optimization of 5-Amino-1,2,3-triazole-4-carboxamide Series against Trypanosoma cruzi

Brand, S., Ko, E. J., Viayna, E., Thompson, S., Spinks, D., Thomas, M., Sandberg, L., Francisco, A. F., Jayawardhana, S., Smith, V. C., Jansen, C., De Rycker, M., Thomas, J., MacLean, L., Osuna-Cabello, M., Riley, J., Scullion, P., Stojanovski, L., Simeons, F. R. C., Epemolu, O. & 16 othersShishikura, Y., Crouch, S. D., Bakshi, T. S., Nixon, C. J., Reid, I. H., Hill, A. P., Underwood, T. Z., Hindley, S. J., Robinson, S. A., Kelly, J. M., Fiandor, J. M., Wyatt, P. G., Marco, M., Miles, T. J., Read, K. D. & Gilbert, I. H., 14 Sep 2017, In : Journal of Medicinal Chemistry. 60, 17, p. 7284-7299 16 p.

Research output: Contribution to journalArticle

Open Access
File
Triazoles
Trypanosoma cruzi
Parasites
Chagas Disease
Nifurtimox
29 Citations (Scopus)

Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis

Park, Y., Pacitto, A., Bayliss, T., Cleghorn, L. A. T., Wang, Z., Hartman, T., Arora, K., Ioerger, T. R., Sacchettini, J., Rizzi, M., Donini, S., Blundell, T. L., Ascher, D. B., Rhee, K., Breda, A., Zhou, N., Dartois, V., Jonnala, S. R., Via, L. E., Mizrahi, V. & 35 othersEpemolu, O., Stojanovski, L., Simeons, F., Osuna-Cabello, M., Ellis, L., MacKenzie, C. J., Smith, A. R. C., Davis, S. H., Murugesan, D., Buchanan, K. I., Turner, P. A., Huggett, M., Zuccotto, F., Rebollo-Lopez, M. J., Lafuente-Monasterio, M. J., Sanz, O., Diaz, G. S., Lelièvre, J., Ballell, L., Selenski, C., Axtman, M., Ghidelli-Disse, S., Pflaumer, H., Bösche, M., Drewes, G., Freiberg, G. M., Kurnick, M. D., Srikumaran, M., Kempf, D. J., Green, S. R., Ray, P. C., Read, K., Wyatt, P., Barry, C. E. & Boshoff, H. I., 13 Jan 2017, In : ACS Infectious Diseases. 3, 1, p. 18-33 16 p.

Research output: Contribution to journalArticle

Indazoles
Inosine Monophosphate
Sulfonamides
Mycobacterium tuberculosis
Oxidoreductases
2016
21 Citations (Scopus)
40 Downloads (Pure)

Activation of bicyclic nitro-drugs by a novel nitroreductase (NTR2) in Leishmania

Wyllie, S., Roberts, A. J., Norval, S., Patterson, S., Foth, B. J., Berriman, M., Read, K. D. & Fairlamb, A. H., 3 Nov 2016, In : PLoS Pathogens. 12, 11, p. 1-22 22 p., e1005971.

Research output: Contribution to journalArticle

Open Access
File
Nitroreductases
Leishmania
Nitro Compounds
Nifurtimox
Pharmaceutical Preparations
2 Citations (Scopus)

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 journalArticle

Antimalarials
Drug Discovery
Biological Science Disciplines
Proteins
corrigendum
18 Citations (Scopus)
71 Downloads (Pure)

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 journalArticle

Open Access
File
Peptide Elongation Factor 2
Antimalarials
Plasmodium falciparum
Malaria
Pharmacokinetics
14 Citations (Scopus)

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides

Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neilde, K., Cotillo, I., Rahmani Khajouei, M., Ferrins, L., Qureishi, S., Nguyen, N., Martinez-Martinez, M. S., Weaver, D. F., Kaiser, M., Riley, J., Thomas, J., De Rycker, M., Read, K. D., Flematti, G. R., Ryan, E., Tanghe, S. & 6 othersRodriguez, A., Charman, S. A., Kessler, A., Avery, V. M., Baell, J. B. & Piggott, M. J., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9686-9720 35 p.

Research output: Contribution to journalArticle

Trypanosomiasis
Neglected Diseases
African Trypanosomiasis
Trypanosoma brucei brucei
Chagas Disease
8 Citations (Scopus)
69 Downloads (Pure)

Metabolomics and lipidomics reveal perturbation of sphingolipid metabolism by a novel anti-trypanosomal 3-(oxazolo[4,5-b]pyridine-2-yl)anilide

Stoessel, D., Nowell, C. J., Jones, A. J., Ferrins, L., Ellis, K. M., Riley, J., Rahmani, R., Read, K. D., McConville, M. J., Avery, V. M., Baell, J. B. & Creek, D. J., Jul 2016, In : Metabolomics. 12, 7, 14 p., 126.

Research output: Contribution to journalArticle

Open Access
File
Anilides
Trypanosoma brucei brucei
Sphingolipids
Metabolomics
Ceramides
20 Citations (Scopus)
51 Downloads (Pure)

Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage

Francisco, A. F., Jayawardhana, S., Lewis, M. D., White, K. L., Shackleford, D. M., Chen, G., Saunders, J., Osuna-Cabello, M., Read, K. D., Charman, S. A., Chatelain, E. & Kelly, J. M., 17 Oct 2016, In : Scientific Reports. 6, p. 1-11 11 p., 35351.

Research output: Contribution to journalArticle

Open Access
File
Trypanosoma cruzi
Nifurtimox
Sulfones
Chagas Disease
Infection
40 Citations (Scopus)
82 Downloads (Pure)

Potent and selective chemical probe of hypoxic signaling downstream of HIF-α hydroxylation via VHL inhibition

Frost, J., Galdeano, C., Soares, P., Gadd, M. S., Grzes, K. M., Ellis, L., Epemolu, O., Shimamura, S., Bantscheff, M., Grandi, P., Read, K. D., Cantrell, D. A., Rocha, S. & Ciulli, A., 4 Nov 2016, In : Nature Communications. 7, p. 1-12 12 p., 13312.

Research output: Contribution to journalArticle

Open Access
File
Hydroxylation
hypoxia
probes
Prolyl-Hydroxylase Inhibitors
Prolyl Hydroxylases
26 Citations (Scopus)
64 Downloads (Pure)

The anti-tubercular drug delamanid as a potential oral treatment for visceral leishmaniasis

Patterson, S., Wyllie, S., Norval, S., Stojanovski, L., Simeons, F. R. C., Auer, J. L., Osuna-Cabello, M., Read, K. D. & Fairlamb, A. H., 24 May 2016, In : eLife. 5, p. 1-21 21 p., e09744.

Research output: Contribution to journalArticle

Open Access
File
Visceral Leishmaniasis
Hormesis
Pharmaceutical Preparations
Parasites
Nitroreductases
4 Citations (Scopus)
54 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 journalArticle

Open Access
File
Pyrimidines
Antimalarials
Plasmodium falciparum
Malaria
SCID Mice
2015
144 Citations (Scopus)

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 journalArticle

15 Citations (Scopus)

Development of a fluorescence-based Trypanosoma cruzi CYP51 inhibition assay for effective compound triaging in drug discovery programmes for Chagas disease

Riley, J., Brand, S., Voice, M., Caballero, I., Calvo, D. & Read, K. D., 22 Sep 2015, In : PLoS Neglected Tropical Diseases. 9, 9, 12 p., e0004014.

Research output: Contribution to journalArticle

Chagas Disease
Trypanosoma cruzi
Drug Discovery
Fluorescence
Pharmaceutical Preparations
6 Citations (Scopus)

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

Trypanosoma brucei brucei
Molecules
Scaffolds
Leishmania major
X ray crystallography
17 Citations (Scopus)

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

African Trypanosomiasis
Trypanosoma brucei brucei
Brain
Peptide Hydrolases
Central Nervous System
8 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 journalArticle

Trypanosoma brucei brucei
Scaffolds
Protein Kinases
Screening
Growth
2014
14 Citations (Scopus)
54 Downloads (Pure)

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

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

Research output: Contribution to journalArticle

Open Access
File
Pneumococcal Infections
C-Reactive Protein
Anti-Idiotypic Antibodies
Antibodies
25 Citations (Scopus)
25 Downloads (Pure)
Open Access
File
African Trypanosomiasis
Trypanosoma brucei brucei
Sulfonamides
Central Nervous System
Neurologic Mutant Mice
2013
37 Citations (Scopus)

Discovery of Β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor

Aristotelous, T., Ahn, S., Shukla, A. K., Gawron, S., Sassano, M. F., Kahsai, A. W., Wingler, L. M., Zhu, X., Tripathi-Shukla, P., Huang, X-P., Riley, J., Besnard, J., Read, K. D., Roth, B. L., Gilbert, I. H., Hopkins, A. L., Lefkowitz, R. J. & Navratilova, I., 2013, In : ACS Medicinal Chemistry Letters. 4, 10, p. 1005-1010 6 p.

Research output: Contribution to journalArticle

Biosensing Techniques
G-Protein-Coupled Receptors
Biosensors
Adrenergic Receptors
Screening
16 Citations (Scopus)

Structure-Activity Relationship Studies of Pyrrolone Antimalarial Agents

Murugesan, D., Kaiser, M., White, K. L., Norval, S., Riley, J., Wyatt, P. G., Charman, S. A., Read, K. D., Yeates, C. & Gilbert, I. H., 2013, In : ChemMedChem.

Research output: Contribution to journalArticle

Antimalarials
Structure-Activity Relationship
Parasites
Derivatives
Humulus
24 Citations (Scopus)
Antitubercular Agents
Visceral Leishmaniasis
Leishmania
Nitroreductases
Mycobacterium tuberculosis
2012
14 Citations (Scopus)

A comparative study of the CYP450 inhibition potential of marketed drugs using two fluorescence based assay platforms routinely used in the pharmaceutical industry

Kajbaf, M., Longhi, R., Montanari, D., Vinco, F., Rigo, M., Fontano, S. & Read, K. D., 2012, In : Drug Metabolism Letters. 5, 1, p. 30-39 10 p.

Research output: Contribution to journalArticle

Drug Industry
Drug interactions
Assays
Microsomes
Fluorescence
354 Citations (Scopus)

Automated design of ligands to polypharmacological profiles

Besnard, J., Ruda, G. F., Setola, V., Abecassis, K., Rodriguiz, R. M., Huang, X-P., Norval, S., Sassano, M. F., Shin, A. I., Webster, L. A., Simeons, F. R. C., Stojanovski, L., Prat, A., Seidah, N. G., Constam, D. B., Bickerton, G. R., Read, K. D., Wetsel, W. C., Gilbert, I. H., Roth, B. L. & 1 othersHopkins, A. L., 13 Dec 2012, In : Nature. 492, 7428, p. 215-+ 8 p.

Research output: Contribution to journalArticle

32 Citations (Scopus)

Combining PET biodistribution and equilibrium dialysis assays to assess the free brain concentration and BBB transport of CNS drugs

Gunn, R. N., Summerfield, S. G., Salinas, C. A., Read, K. D., Guo, Q., Searle, G. E., Parker, C. A., Jeffrey, P. & Laruelle, M., May 2012, In : Journal of Cerebral Blood Flow and Metabolism. 32, 5, p. 874-883 10 p.

Research output: Contribution to journalArticle

28 Citations (Scopus)
6 Downloads (Pure)
69 Citations (Scopus)
330 Downloads (Pure)

Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Brand, S., Cleghorn, L. A. T., McElroy, S. P., Robinson, D. A., Smith, V. C., Hallyburton, I., Harrison, J. R., Norcross, N. R., Spinks, D., Bayliss, T., Norval, S., Stojanovski, L., Torrie, L. S., Frearson, J. A., Brenk, R., Fairlamb, A. H., Ferguson, M. A. J., Read, K. D., Wyatt, P. G. & Gilbert, I. H., 12 Jan 2012, In : Journal of Medicinal Chemistry. 55, 1, p. 140-152 13 p.

Research output: Contribution to journalArticle

Open Access
File
22 Citations (Scopus)
292 Downloads (Pure)

Skin-targeted inhibition of PPAR β/δ by selective antagonists to treat PPAR β/δ-mediated psoriasis-like skin disease in vivo

Hack, K., Reilly, L., Palmer, C., Read, K., Norval, S., Kime, R., Booth, K. & Foerster, J., May 2012, In : PLoS ONE. 7, 5

Research output: Contribution to journalArticle

Open Access
File
psoriasis
Peroxisome Proliferator-Activated Receptors
skin diseases
Psoriasis
Skin Diseases
22 Citations (Scopus)

Synthesis and Evaluation of α-Thymidine Analogues as Novel Antimalarials

Cui, H., Carrero-Lérida, J., Silva, A. P. G., Whittingham, J. L., Brannigan, J. A., Ruiz-Pérez, L. M., Read, K. D., Wilson, K. S., González-Pacanowska, D. & Gilbert, I. H., 2012, In : Journal of Medicinal Chemistry. 55, 24, p. 10948-57 10 p.

Research output: Contribution to journalArticle

Antimalarials
Thymidine
dTMP kinase
Urea
Pyrimidine Nucleotides
71 Citations (Scopus)

The Anti-Trypanosome Drug Fexinidazole Shows Potential for Treating Visceral Leishmaniasis

Wyllie, S., Patterson, S., Stojanovski, L., Simeons, F. R. C., Norval, S., Kime, R., Read, K. D. & Fairlamb, A. H., 1 Feb 2012, In : Science Translational Medicine. 4, 119, p. - 7 p., 119re1.

Research output: Contribution to journalArticle