Read, Kevin

Professor

20082022
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Research Output 2008 2019

32 Citations (Scopus)

1-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes and 6-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes: a new series of potent and selective triple reuptake inhibitors

Micheli, F., Cavanni, P., Arban, R., Benedetti, R., Bertani, B., Bettati, M., Bettelini, L., Bonanomi, G., Braggio, S., Checchia, A., Davalli, S., Di Fabio, R., Fazzolari, E., Fontana, S., Marchioro, C., Minick, D., Negri, M., Oliosi, B., Read, K. D., Sartori, I. & 6 others, Tedesco, G., Tarsi, L., Terreni, S., Visentini, F., Zocchi, A. & Zonzini, L., 25 Mar 2010, In : Journal of Medicinal Chemistry. 53, 6, p. 2534-2551 18 p.

Research output: Contribution to journalArticle

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
7 Citations (Scopus)
99 Downloads (Pure)

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

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

Research output: Contribution to journalArticle

Open Access
File
Quinazolinones
Structure-Activity Relationship
Mycobacterium tuberculosis
Adenosine Triphosphate
Allosteric Site
42 Citations (Scopus)

6-(3,4-dichlorophenyl)-1-[(methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: a new potent and selective triple reuptake inhibitor

Micheli, F., Cavanni, P., Andreotti, D., Arban, R., Benedetti, R., Bertani, B., Bettati, M., Bettelini, L., Bonanomi, G., Braggio, S., Carletti, R., Checchia, A., Corsi, M., Fazzolari, E., Fontana, S., Marchioro, C., Merlo-Pich, E., Negri, M., Oliosi, B., Ratti, E. & 11 others, Read, K. D., Roscic, M., Sartori, I., Spada, S., Tedesco, G., Tarsi, L., Terreni, S., Visentini, F., Zocchi, A., Zonzini, L. & Di Fabio, R., 8 Jul 2010, In : Journal of Medicinal Chemistry. 53, 13, p. 4989-5001 13 p.

Research output: Contribution to journalArticle

25 Downloads (Pure)

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

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

Research output: Contribution to journalArticle

Open Access
File
Kynurenine 3-Monooxygenase
Kynurenine
Neurodegenerative Diseases
Huntington Disease
Prodrugs
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
25 Citations (Scopus)
77 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
8 Citations (Scopus)
101 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
157 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 others, Norval, S., Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P. M., Churcher, T. S., Sala, K. A., Zakutansky, S. E., Belén Jiménez-Díaz, M., Maria Sanz, L., Riley, J., Basak, R., Campbell, M., Avery, V. M., Sauerwein, R. W., Dechering, K. J., Noviyanti, R., Campo, B., Frearson, J. A., Angulo-Barturen, I., Ferrer-Bazaga, S., Javier Gamo, F., Wyatt, P. G., Leroy, D., Siegl, P., Delves, M. J., Kyle, D. E., Wittlin, S., Marfurt, J., Price, R. N., Sinden, R. E., Winzeler, E. A., Charman, S. A., Bebrevska, L., Gray, D. W., Campbell, S., Fairlamb, A. H., Willis, P. A., Rayner, J. C., Fidock, D. A., Read, K. D. & Gilbert, I. H., 18 Jun 2015, In : Nature. 522, 7556, p. 315-320 6 p.

Research output: Contribution to journalArticle

102 Citations (Scopus)
201 Downloads (Pure)
Open Access
File
Drug Discovery
Public Health
Neglected Diseases
Disease Eradication
African Trypanosomiasis
39 Citations (Scopus)
198 Downloads (Pure)

Aryl Phosphoramidates of 5-Phospho Erythronohydroxamic Acid, A New Class of Potent Trypanocidal Compounds

Ruda, G. F., Wong, P. E., Alibu, V. P., Norval, S., Read, K. D., Barrett, M. P. & Gilbert, I. H., 2010, In : Journal of Medicinal Chemistry. 53, 16, p. 6071-6078 8 p.

Research output: Contribution to journalArticle

Open Access
File
52 Citations (Scopus)

Assessing brain free fraction in early drug discovery

Read, K. D. & Braggio, S., Mar 2010, In : Expert Opinion on Drug Metabolism & Toxicology. 6, 3, p. 337-344 8 p.

Research output: Contribution to journalReview article

383 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 others, Hopkins, A. L., 13 Dec 2012, In : Nature. 492, 7428, p. 215-+ 8 p.

Research output: Contribution to journalArticle

13 Citations (Scopus)
226 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 others, Wernimont, 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
32 Citations (Scopus)

Cell-penetrant, nanomolar O-GlcNAcase inhibitors selective against lysosomal hexosaminidases

Dorfmueller, H. C., Borodkin, V. S., Schimpl, M., Zheng, X., Kime, R., Read, K. D. & van Aalten, D. M. F., 24 Nov 2010, In : Chemistry & Biology. 17, 11, p. 1250-1255 6 p.

Research output: Contribution to journalArticle

Central nervous system (CNS) exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous (IV) dosing in mice

Dow, G. S., Milner, E., Caridha, D., Gardner, S., Lanteri, C., Kozar, M., Mannila, A., McCalmont, W., Melendez, V., Moon, J., Read, K., Norval, S., Roncal, N., Shackleford, D., Sousa, J., Stouten, J., White, K., Zeng, Q. & Charman, S., Nov 2010, p. 213-213. 1 p.

Research output: Contribution to conferenceAbstract

15 Citations (Scopus)

Central nervous system exposure of next generation quinoline methanols is reduced relative to mefloquine after intravenous dosing in mice

Dow, G. S., Milner, E., Bathurst, I., Bhonsle, J., Caridha, D., Gardner, S., Gerena, L., Kozar, M., Lanteri, C., Mannila, A., McCalmont, W., Moon, J., Read, K. D., Norval, S., Roncal, N., Shackleford, D. M., Sousa, J., Steuten, J., White, K. L., Zeng, Q. & 1 others, Charman, S. A., 6 Jun 2011, In : Malaria Journal. 10, p. - 11 p., 150.

Research output: Contribution to journalArticle

9 Citations (Scopus)

Characterization of in vivo metabolites of WR319691, a novel compound with activity against Plasmodium falciparum

Milner, E., Sousa, J., Pybus, B., Melendez, V., Gardner, S., Grauer, K., Moon, J., Carroll, D., Auschwitz, J., Gettayacamin, M., Lee, P., Leed, S., McCalmont, W., Norval, S., Tungtaeng, A., Zeng, Q., Kozar, M., Read, K. D., Li, Q. & Dow, G., 2011, In : European Journal of Drug Metabolism and Pharmacokinetics. 36, 3, p. 151-158 8 p.

Research output: Contribution to journalArticle

5 Citations (Scopus)
90 Downloads (Pure)
Open Access
File
Metabolites
Drug Users
Metabolism
Opioid Analgesics
Urine
4 Citations (Scopus)
125 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
33 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

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 others, Norval, S., Zuccotto, F., Thomas, J., Simeons, F., Stojanovski, L., Osuna-Cabello, M., Brock, P. M., Churcher, T. S., Sala, K. A., Zakutansky, S. E., Jiménez-Díaz, M. B., Sanz, L. M., Riley, J., Basak, R., Campbell, M., Avery, V. M., Sauerwein, R. W., Dechering, K. J., Noviyanti, R., Campo, B., Frearson, J. A., Angulo-Barturen, I., Ferrer-Bazaga, S., Javier Gamo, F., Wyatt, P. G., Leroy, D., Siegl, P., Delves, M. J., Kyle, D. E., Wittlin, S., Marfurt, J., Price, R. N., Sinden, R. E., Winzeler, E. A., Charman, S. A., Bebrevska, L., Gray, D. W., Campbell, S., Fairlamb, A. H., Willis, P. A., Rayner, J. C., Fidock, D. A., Read, K. D. & Gilbert, I. H., 25 May 2016, In : Nature. 537, 7618, p. 122 1 p.

Research output: Contribution to journalArticle

Antimalarials
Drug Discovery
Biological Science Disciplines
Proteins
corrigendum
16 Citations (Scopus)
86 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
65 Citations (Scopus)

Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

Sokolova, A. Y., Wyllie, S., Patterson, S., Oza, S. L., Read, K. D. & Fairlamb, A. H., Jul 2010, In : Antimicrobial Agents and Chemotherapy. 54, 7, p. 2893-2900 8 p.

Research output: Contribution to journalArticle

17 Citations (Scopus)
250 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 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., 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
25 Citations (Scopus)
2 Downloads (Pure)

Design, Synthesis and Biological Evaluation of Novel Inhibitors of Trypanosoma brucei Pteridine Reductase 1

Spinks, D., Ong, H. B., Mpamhanga, C. P., Shanks, E. J., Robinson, D. A., Collie, I. T., Read, K. D., Frearson, J. A., Wyatt, P. G., Brenk, R., Fairlamb, A. H. & Gilbert, I. H., 7 Feb 2011, In : ChemMedChem. 6, 2, p. 302-308 7 p.

Research output: Contribution to journalArticle

28 Citations (Scopus)
6 Downloads (Pure)
4 Citations (Scopus)
133 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
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
8 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
8 Citations (Scopus)
113 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 others, Shishikura, 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
72 Citations (Scopus)
374 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
21 Citations (Scopus)
118 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 others, Gray, 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
19 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
1 Citation (Scopus)
70 Downloads (Pure)
Open Access
File
Lysosphingolipid Receptors
Drug Discovery
Modulators
Skin
Pharmaceutical Preparations
3 Citations (Scopus)
124 Downloads (Pure)
Open Access
File
Lysosphingolipid Receptors
Modulators
Esters
Plasma (human)
Butyrylcholinesterase
41 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
35 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 others, Epemolu, 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
39 Citations (Scopus)

Evaluation of direct transport pathways of glycine receptor antagonists and an angiotensin antagonist from the nasal cavity to the central nervous system in the rat model

Charlton, S. T., Whetstone, J., Fayinka, S. T., Read, K. D., Illum, L. & Davis, S. S., Jul 2008, In : Pharmaceutical Research. 25, 7, p. 1531-1543 13 p.

Research output: Contribution to journalArticle

27 Citations (Scopus)
104 Downloads (Pure)
Open Access
File
Ubiquitin-Protein Ligases
Structure-Activity Relationship
Proteolysis
Ligands
Tumor Suppressor Proteins
15 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 others, Rodriguez, 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
4 Citations (Scopus)
106 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
53 Citations (Scopus)

Identification of a kappa-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis

Jones, D. C., Hallyburton, I., Stojanovski, L., Read, K. D., Frearson, J. A. & Fairlamb, A. H., 15 Nov 2010, In : Biochemical Pharmacology. 80, 10, p. 1478-1486 9 p.

Research output: Contribution to journalArticle

4 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 others, Lowe, R. M., MacKenzie, C. J., MacLean, L., Manthri, S., Martin, F., Miguel-Siles, J., Nguyen, V. L., Norval, S., Osuna-Cabello, M., Woodland, A., Patterson, S., Pena, I., Quesada-Campos, M. T., Reid, I. H., Revill, C., Riley, J., Ruiz-Gomez, J. R., Shishikura, Y., Simeons, F. R. C., Smith, A., Smith, V. C., Spinks, D., Stojanovski, L., Thomas, J., Thompson, S., Underwood, T., Gray, D. W., Fiandor, J. M., Gilbert, I. H., Wyatt, P. G., Read, K. D. & Miles, T. J., 14 Feb 2019, In : Journal of Medicinal Chemistry. 62, 3, p. 1180-1202 23 p.

Research output: Contribution to journalArticle

Visceral Leishmaniasis
Leishmania major
Leishmania donovani
Standard of Care
Solubility
5 Citations (Scopus)
105 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 others, Guijarro, L., Read, K., Green, S., Hipskind, P., Parish, T. & Wyatt, P., 9 Aug 2018, In : Journal of Medicinal Chemistry. 61, 15, p. 6592-6608 17 p.

Research output: Contribution to journalArticle

Open Access
File
Thiophenes
Morpholinos
Mycobacterium tuberculosis
Electron Transport Complex IV
Structure-Activity Relationship
2 Citations (Scopus)

In Vitro and In Vivo studies of trypanocidal activity of dietary isothiocyanates

Steverding, D., Michaels, S. & Read, K. D., 22 Jan 2014, In : Planta Medica.

Research output: Contribution to journalLetter

Isothiocyanates
Trypanosoma brucei brucei
Trypanosomiasis
HL-60 Cells
Parasitemia
30 Citations (Scopus)
54 Downloads (Pure)
Open Access
File
African Trypanosomiasis
Trypanosoma brucei brucei
Sulfonamides
Central Nervous System
Neurologic Mutant Mice