2023

Bopp, S. et al. (2023) Potent acyl-CoA synthetase 10 inhibitors kill Plasmodium falciparum by disrupting triglyceride formation. Nat. Commun. 14:1455. https://pubmed.ncbi.nlm.nih.gov/36927839/

Smith, R. et al. (2023) Chemical pulldown combined with mass spectrometry to identify the molecular targets of antimalarials in cell-free lysates. Star Protocols 4:102002. https://pubmed.ncbi.nlm.nih.gov/36609153/

2022 

Navidpour, L. et al. (2022) Antileishmanial Activities of ( Z)-2-(Nitroimidazolylmethylene)-3( 2H)-Benzofuranones: Synthesis, In Vitro Assessment, and Bioactivation by NTR 1 and 2. Antimicrob Agents Chemother. 66: e0058322. https://pubmed.ncbi.nlm.nih.gov/36286539/

Benns, HJ. et al. (2022) CRISPR based oligo recombineering prioritizes apicomplexan cysteines for drug discovery. Nat. Microbiol. 7:1891-1905. https://pubmed.ncbi.nlm.nih.gov/36266336/

Milne, R. et al. (2022) Toolkit of approaches to support target-focused drug discovery for Plasmodium falciparum lysyl tRNA synthetase. ACS Infect. Dis. 8:1962-1974. https://pubmed.ncbi.nlm.nih.gov/36037410/

Tamaki, F. et al. (2022) High-Throughput Screening Platform To Identify Inhibitors of Protein Synthesis with Potential for the Treatment of Malaria. Antimicrob Agents Chemother. (in press). https://pubmed.ncbi.nlm.nih.gov/35647647/

Altmann, S. et al., (2022) Oligo targeting for profiling drug resistance mutations in the parasitic trypanosomatids. Nucleic Acids Res. (in press). https://pubmed.ncbi.nlm.nih.gov/35524555/

Smith A, Wall RJ, Patterson S et al., (2022) Repositioning of a diaminothiazole series confirmed to target the cyclin-dependent kinase CRK12 for use in the treatment of African Animal Trypanosomiasis. J Med Chem. 65: 5606-5624. https://pubmed.ncbi.nlm.nih.gov/35303411/

2021

Mowbray, C. Braillard, S., Glossop, P.A., Whitlock, G.A., Jacobs, R.T., Speake, J., Pandi, B., Nare, B., Maes, L.J., Yardley, V., Freund, Y.R., Wall, R.J., Carvalho, S., Bello, D., Van den Kerkhof, M., Caljon, G., Gilbert, I.H., Corpas-Lopez, V., Lukac, I., Patterson, S., Zuccotto, F. and Wyllie, S (2021) DNDI-6148: A novel benzoxaborole preclinical candidate for the treatment of visceral leishmaniasis. J Med Chem. 64:16159-16176. https://pubmed.ncbi.nlm.nih.gov/34711050/

Svensen, N., Wyllie, S., Gray, D.W. and De Rycker, M. (2021) Live-imaging rate-of-kill compound profiling for Chagas disease drug discovery with a new automated high-content assay. PLoS Neglected Tropical Diseases 15(10):e0009870. https://pubmed.ncbi.nlm.nih.gov/34634052/

Lima, M., Tulloch, L.B., Corpas-Lopez, V., Carvalho S., Wall, R.J., Milne, R., Rico, E., Patterson, S., Gilbert, I.H., Moniz, S., MacLean, L., Morgillo, C., Horn, D., Zuccotto, F. and Wyllie, S (2021) Identification of a proteasome-targeting arylsulfonamide with potential for the treatment 1 of Chagas’ disease. Antimicrobial Agents and Chemotherapy. 66(1):e0153521. https://pubmed.ncbi.nlm.nih.gov/34606338/

Barbara Forte et al. (2021) Prioritization of molecular targets for anti-malaria drug discovery. ACS Infect Dis. 7(10):2764-2776. https://pubmed.ncbi.nlm.nih.gov/34523908/

Victoriano Corpas Lopez and Susan Wyllie (2021) Utilizing thermal proteome profiling to identify the molecular targets of anti-leishmanial compounds. Star Protocols. https://star-protocols.cell.com/protocols/948

Juliana da Silva Pacheco et al. (2021) Monocyclic Nitro-heteroaryl Nitrones with Dual Mechanism of Activation: Synthesis and Antileishmanial Activity. ACS Med. Chem. Lett. 12(9):1405-1412. https://pubs.acs.org/doi/10.1021/acsmedchemlett.1c00193

Magali Van den Kerkhof et al. (2021) Identification of Resistance Determinants for a Promising Antileishmanial Oxaborole Series. Microorganisms. 9:1408. https://pubmed.ncbi.nlm.nih.gov/34210040/

Tuo Yang et al. (2021) MalDA, Accelerating Malaria Drug Discovery. Trends in Parasitology. 37:493-507. https://pubmed.ncbi.nlm.nih.gov/33648890/

Luciana Paradela, Richard J. Wall, Sandra Carvalho, Giulia Chemi, Victoriano Corpas-Lopez, Eoin Moynihan, Davide Bello, Stephen Patterson, Lucia Guther, Alan H. Fairlamb, Michael Ferguson, Fabio Zuccotto, Julio Martin, Ian H. Gilbert and Susan Wyllie. (2021) Multiple unbiased approaches identify oxidosqualene cyclase as the molecular target of a promising anti-leishmanial. Cell Chem. Biol. 28:711-721. https://pubmed.ncbi.nlm.nih.gov/33691122/

Lauren B. Arendse, Susan Wyllie, Kelly Chibale and Ian H. Gilbert. (2021) Plasmodium Kinases as Potential Drug Targets for Malaria: Challenges and Opportunities. ACS Infect Dis. 7:518-534. https://pubmed.ncbi.nlm.nih.gov/33590753/

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. 206:112668. 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. 63:9523-9539. 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 Q_i 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 Wyllie, Stephen Brand, Michael Thomas, Manu 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