Publications

2020

Cyril Fersing et al. (2020) Antikinetoplastid SAR study in 3-nitroimidazopyridine series: Identification of a novel non-genotoxic and potent anti-T. b. brucei hit-compound with improved pharmacokinetic properties. Eur J Med Chem. (in press) https://pubmed.ncbi.nlm.nih.gov/32795774/

Michael G Thomas et al. (2020) Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent In Vitro Antileishmanial Activity: Initial SAR and Assessment of In Vivo Activity. J Med Chem. (in press) https://pubmed.ncbi.nlm.nih.gov/32663005/

Cyril Fersing et al. (2020) 8-Alkynyl-3-nitroimidazopyridines display potent antitrypanosomal activity against both T. b. brucei and cruzi. Eur J Med Chem. 202:112558. https://pubmed.ncbi.nlm.nih.gov/32652409/

Julian Pedron et al. (2020) New 8-Nitroquinolinone Derivative Displaying Submicromolar in Vitro Activities against Both Trypanosoma brucei and cruzi. ACS Med Chem Lett.11: 464-472. https://pubmed.ncbi.nlm.nih.gov/32292551/

Richard J. Wall, Sandra Carvalho, Rachel Milne, Juan A. Bueren-Calabuig, Sonia Moniz, Juan Cantizani-Perez,Lorna MacLean, Albane Kessler, Ignacio Cotillo Torrejon, Lalitha Sastry, Sujatha Manthri, Stephen Patterson,Fabio Zuccotto, Stephen Thompson, Julio Martin, Maria Marco, Timothy J. Miles, Manu De Rycker, Michael G. Thomas, Alan H. Fairlamb, Ian H. Gilbert and Susan Wyllie (2020) The Qi site of cytochrome b is a promiscuous drug target in Trypanosoma cruzi and Leishmania donovani. ACS Infect Dis. 6: 515-528. https://pubmed.ncbi.nlm.nih.gov/31967783

2019

Susan WyllieStephen BrandMichael ThomasManu De Rycker et al. (2019) Preclinical candidate for the treatment visceral leishmaniasis acts through proteasome inhibition. PNAS. https://www.ncbi.nlm.nih.gov/pubmed/30962368

Corpas-Lopez, V., Moniz, S., Thomas, M., Wall, R. J., Torrie, L. S., Zander-Dinse, D. Tinti, M., Brand, S., Stojanovski, L., Manthri, S., Hallyburton, I., Zuccotto, F., Wyatt, P. G., De Rycker, M., Horn, D., Ferguson, M. A. J., Clos, J., Read, K. D., Fairlamb, A.H., Gilbert, I. H. and Wyllie, S. (2019) Pharmacological validation of N-myristoyltransferase as a drug target in Leishmania donovani. ACS Infect Dis. 5: 111–122. https://www.ncbi.nlm.nih.gov/pubmed/30380837

2018

Fersing, C., Basmaciyan, L., Boudot, C., Pedron, J., Hutter, S., Cohen, A., Castera-Ducros, C., Primas, N., Laget, M., Casanova, M., Bourgeade-Delmas, S., Piednoel, M., Sournia-Saquet, A., Belle Mbou, V., Courtioux, B., Boutet-Robinet, E., Since, M., Milne, R., Wyllie, S., Fairlamb, A. H., Valentin, A., Rathelot, P., Verhaeghe, P., Vanelle, P., Azas, N. (2018) Non-genotoxic 3-nitroimidazo[1,2-a]pyridines are NTR1 substrates that display potent in vitro antileishmanial activity. ACS Med Chem Lett. 10: 34-39. https://www.ncbi.nlm.nih.gov/pubmed/30655943

Webster, L. A., Thomas, M., Urbaniak, M., Wyllie, S., Ong, H. B., Tinti, M., Fairlamb, A. H., Boesche, M., Ghidelli-Disse, S., Drewes, G. and Gilbert, I. H. (2018) Development of Chemical Proteomics for the Folateome and Analysis of the Kinetoplastid Folateome. ACS Infect Dis. 4: 1475-1486. https://www.ncbi.nlm.nih.gov/pubmed/30264983

Pedron, J., Boudot, C., Bourgeade-Delmas, S. et al. (2018) Antitrypanosomatid Pharmacomodulation at Position 3 of the 8-Nitroquinolin-2(1H)-one Scaffold Using Palladium-Catalysed Cross-Coupling Reactions. ChemMedChem. 13: 2217-2228. https://www.ncbi.nlm.nih.gov/pubmed/30221468

Wall, R.J., Rico, E., Lukac, I., Zuccotto, F., Elg, S., Gilbert, I. H., Freund, Y., Alley, M. R. K., Field, M. C., Wyllie, S. and Horn D. (2018) Clinical and veterinary trypanocidal benzoxaboroles target CPSF3. PNAS 115: 9616-9621. https://www.ncbi.nlm.nih.gov/pubmed/30185555

Fersing, C., Boudot, C., Pedron, J. et al. (2018) 8-Aryl-6-chloro-3-nitro-2-(phenylsulfonylmethyl)imidazo[1,2-a]pyridines as potent antitrypanosomatid molecules bioactivated by type I nitroreductases. Eur J Med Chem. 157:115-126. https://www.ncbi.nlm.nih.gov/pubmed/30092366

Wyllie, S. Thomas, M., Patterson, S. et al. (2018) Cyclin-dependent kinase 12, a novel drug target for visceral leishmaniasis. Nature 560:192-197. https://www.ncbi.nlm.nih.gov/pubmed/30046105

Pedron, J., Boudot, C., Hutter, S. et al. (2018) Novel 8-nitroquinolin-2(1H)-ones as NTR-bioactivated antikinetoplastid molecules: Synthesis, electrochemical and SAR study. Eur J Med Chem. 155:135-152. https://www.ncbi.nlm.nih.gov/pubmed/29885575

Wall, R. J., Moniz, S., Thomas, M. G., Norval, S., Ko, E. J., Marco, M., Miles, T. J., Gilbert, I. H., Horn, D., Fairlamb, A. H. and Wyllie S. (2018) Anti-trypanosomal 8-hydroxy naphthyridines are chelators of divalent transition metals. Antimicrob Agents Chemother. 62. pii: e00235-18. https://www.ncbi.nlm.nih.gov/pubmed/29844044

2017

Torrie, L. S, Brand, S. Robinson, D. A. et al. (2017) Chemical Validation of Methionyl-tRNA Synthetase as a Druggable Target in Leishmania donovani. ACS Infect Dis. 3: 718-727. https://www.ncbi.nlm.nih.gov/pubmed/28967262

Field, M. C., Horn, D., Fairlamb, A. H., Ferguson, M. A. J., Gray, D. W., Read, K. D., De Rycker, M., Torrie, L. S., Wyatt, P. G., Wyllie, S. and Gilbert, I. H. (2016) Antitrypanosomatid drug discovery: An ongoing challenge and a continuing need. Nature Rev. Microbiol. 15, 217-231. https://www.ncbi.nlm.nih.gov/pubmed/28579611

2016

Wyllie, S., Norval, S., Roberts, A. J., Patterson, S., Foth, B. J., Berriman, M., Read, K. D. and Fairlamb, A. H.   (2016) Activation of bicyclic nitro-drugs by a novel nitroreductase (NTR2) in Leishmania. PLoS Pathog. e1005971. https://www.ncbi.nlm.nih.gov/pubmed/27812217