Publications

Hoo, R., Ruiz-Morales, E. R., Kelava, I., Rawat, M., Mazzeo, C. I., Tuck, E., Sancho-Serra, C., Chelaghma, S., Predeus, A. V., Murray, S., Fernandez-Antoran, D., Waller, R. F., Álvarez-Errico, D., Lee, M. C. S., & Vento-Tormo, R.

Cell Systems, 2024 May 15;15(5):425-444.e9. doi: 10.1016/j.cels.2024.04.002.

Generation of a mutator parasite to drive resistome discovery in Plasmodium falciparum.

Kümpornsin K, Kochakarn T, Yeo T, Okombo J, Luth MR, Hoshizaki J, Rawat M, Pearson RD, Schindler KA, Mok S, Park H, Uhlemann AC, Jana GP, Maity BC, Laleu B, Chenu E, Duffy J, Moliner Cubel S, Franco V, Gomez-Lorenzo MG, Gamo FJ, Winzeler EA, Fidock DA, Chookajorn T, Lee MCS.

Nature communications 2023 May 27;14(1):3059. doi: 10.1038/s41467-023-38774-1.

A transcriptional switch controls sex determination in Plasmodium falciparum.

Gomes AR, Marin-Menendez A, Adjalley SH, Bardy C, Cassan C, Lee MCS and Talman AM

Nature 2022;612;7940;528-533

A manually curated annotation characterises genomic features of P. falciparum lncRNAs.

Hoshizaki J, Adjalley SH, Thathy V, Judge K, Berriman M, Reid AJ and Lee MCS

BMC genomics 2022;23;1;780

Efficient generation of mNeonGreen Plasmodium falciparum reporter lines enables quantitative fitness analysis.

Hoshizaki J, Jagoe H and Lee MCS

Frontiers in cellular and infection microbiology 2022;12;981432

Barcoding Genetically Distinct Plasmodium falciparum Strains for Comparative Assessment of Fitness and Antimalarial Drug Resistance.

Carrasquilla M, Drammeh NF, Rawat M, Sanderson T, Zenonos Z, Rayner JC and Lee MCS

mBio 2022;13;5;e0093722

Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy.

Xie SC, Metcalfe RD, Dunn E, Morton CJ, Huang SC, Puhalovich T, Du Y, Wittlin S, Nie S, Luth MR, Ma L, Kim MS, Pasaje CFA, Kumpornsin K, Giannangelo C, Houghton FJ, Churchyard A, Famodimu MT, Barry DC, Gillett DL, Dey S, Kosasih CC, Newman W, Niles JC, Lee MCS, Baum J, Ottilie S, Winzeler EA, Creek DJ, Williamson N, Parker MW, Brand S, Langston SP, Dick LR, Griffin MDW, Gould AE, Tilley L.

Science 2022;376;6597;1074-1079

CRISPR/Cas9 Editing of the Plasmodium falciparum Genome.

Adjalley S and Lee MCS

Methods in molecular biology (Clifton, N.J.) 2022;2470;221-239

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics.

Cowell AN, Istvan ES, Lukens AK, Gomez-Lorenzo MG, Vanaerschot M, Sakata-Kato T, Flannery EL, Magistrado P, Owen E, Abraham M, LaMonte G, Painter HJ, Williams RM, Franco V, Linares M, Arriaga I, Bopp S, Corey VC, Gnädig NF, Coburn-Flynn O, Reimer C, Gupta P, Murithi JM, Moura PA, Fuchs O, Sasaki E, Kim SW, Teng CH, Wang LT, Akidil A, Adjalley S, Willis PA, Siegel D, Tanaseichuk O, Zhong Y, Zhou Y, Llinás M, Ottilie S, Gamo FJ, Lee MCS, Goldberg DE, Fidock DA, Wirth DF, Winzeler EA.

Science. 2018 Jan 12;359(6372):191-199. doi: 10.1126/science.aan4472.

Quinoxaline-based anti-schistosomal compounds have potent anti-plasmodial activity.

Rawat M, Padalino G, Adika E, Okombo J, Yeo T, Brancale A, Fidock DA, Hoffmann KF, Lee MCS.

PLoS Pathog. 2025 Feb 3;21(2):e1012216. doi: 10.1371/journal.ppat.1012216.

Drug resistance-associated mutations in Plasmodium UBP-1 disrupt its essential deubiquitinating activity.

Smith CJ, Eavis H, Briggs C, Henrici R, Karpiyevich M, Ansbro MR, Hoshizaki J, van der Heden van Noort GJ, Ascher DB, Sutherland CJ, Lee MCS, Artavanis-Tsakonas K

J Biol Chem. 2025 Feb 3:108266. doi: 10.1016/j.jbc.2025.108266

YAT2150 is irresistible in Plasmodium falciparum and active against Plasmodium vivax and Leishmania clinical isolates.

Bouzón-Arnáiz I, Rawat M, Coyle R, Feufack-Donfack LB, Ea M, Orban A, Popovici J, Román-Álamo L, Fallica AN, Domínguez-Asenjo B, Moreno J, Arce EM, Mallo-Abreu A, Muñoz-Torrero D, Lee MCS, Fernàndez-Busquets X.

Sci Rep. 2025 Jan 23;15(1):2941. doi: 10.1038/s41598-025-85346-y

2,8-Disubstituted-1,5-naphthyridines as Dual Inhibitors of Plasmodium falciparum Phosphatidylinositol-4-kinase and Hemozoin Formation with In Vivo Efficacy.

Dziwornu GA, Seanego D, Fienberg S, Clements M, Ferreira J, Sypu VS, Samanta S, Bhana AD, Korkor CM, Garnie LF, Teixeira N, Wicht KJ, Taylor D, Olckers R, Njoroge M, Gibhard L, Salomane N, Wittlin S, Mahato R, Chakraborty A, Sevilleno N, Coyle R, Lee MCS, Godoy LC, Pasaje CF, Niles JC, Reader J, van der Watt M, Birkholtz LM, Bolscher JM, de Bruijni MHC, Coulson LB, Basarab GS, Ghorpade SR, Chibale K.

J Med Chem. 2024 Jul 11;67(13):11401-11420. doi: 10.1021/acs.jmedchem.4c01154.

Systematic in vitro evolution in Plasmodium falciparum reveals key determinants of drug resistance.

Luth MR, Godinez-Macias KP, Chen D, Okombo J, Thathy V, Cheng X, Daggupati S, Davies H, Dhingra SK, Economy JM, Edgar RCS, Gomez-Lorenzo MG, Istvan ES, Jado JC, LaMonte GM, Melillo B, Mok S, Narwal SK, Ndiaye T, Ottilie S, Palomo Diaz S, Park H, Peña S, Rocamora F, Sakata-Kato T, Small-Saunders JL, Summers RL, Tumwebaze PK, Vanaerschot M, Xia G, Yeo T, You A, Gamo FJ, Goldberg DE, Lee MCS, McNamara CW, Ndiaye D, Rosenthal PJ, Schreiber SL, Serra G, De Siqueira-Neto JL, Skinner-Adams TS, Uhlemann AC, Kato N, Lukens AK, Wirth DF, Fidock DA, Winzeler EA.

Science. 2024 Nov 29;386(6725):eadk9893. doi: 10.1126/science.adk9893.

A novel 4-aminoquinoline chemotype with multistage antimalarial activity and lack of cross-resistance with PfCRT and PfMDR1 mutants.

Ferreira LT, Cassiano GC, Alvarez LCS, Okombo J, Calit J, Fontinha D, Gil-Iturbe E, Coyle R, Andrade CH, Sunnerhagen P, Bargieri DY, Prudêncio M, Quick M, Cravo PV, Lee MCS, Fidock DA, Costa FTM.

PLoS Pathog. 2024 Oct 29;20(10):e1012627. doi: 10.1371/journal.ppat.1012627.

β-Carboline-3-carboxamide Antimalarials: Structure-Activity Relationship, ADME-Tox Studies, and Resistance Profiling.

Mathew J, Zhou B, Haney RS, Kunz KA, Do Amaral LS, Roy Chowdhury R, Butler JH, Li H, Chakraborty AJ, Tabassum A, Bremers EK, Merino EF, Coyle R, Lee MCS, Baud D, Brand S, Totrov M, Cassera MB, Carlier PR.

ACS Infect Dis. 2024 Nov 8;10(11):3951-3962. doi: 10.1021/acsinfecdis.4c00653.

Reaction hijacking inhibition of Plasmodium falciparum asparagine tRNA synthetase.

Xie SC, Wang Y, Morton CJ, Metcalfe RD, Dogovski C, Pasaje CFA, Dunn E, Luth MR, Kumpornsin K, Istvan ES, Park JS, Fairhurst KJ, Ketprasit N, Yeo T, Yildirim O, Bhebhe MN, Klug DM, Rutledge PJ, Godoy LC, Dey S, De Souza ML, Siqueira-Neto JL, Du Y, Puhalovich T, Amini M, Shami G, Loesbanluechai D, Nie S, Williamson N, Jana GP, Maity BC, Thomson P, Foley T, Tan DS, Niles JC, Han BW, Goldberg DE, Burrows J, Fidock DA, Lee MCS, Winzeler EA, Griffin MDW, Todd MH, Tilley L.

Nature communications 2024;15;1;937

hERG, Plasmodium Life Cycle, and Cross Resistance Profiling of New Azabenzimidazole Analogues of Astemizole.

Mambwe, D., Coertzen, D., Leshabane, M., Mulubwa, M., Njoroge, M., Gibhard, L., Girling, G., Wicht, K. J., Lee, M. C. S., Wittlin, S., Moreira, D. R. M., Birkholtz, L. M., & Chibale, K.

ACS Med Chem Lett. 2024 Mar 18;15(4):463-469. doi: 10.1021/acsmedchemlett.3c00496

Acute response to pathogens in the early human placenta at single-cell resolution .

Cell Systems, 2024 May 15;15(5):425-444.e9. doi: 10.1016/j.cels.2024.04.002.

Propensity of selecting mutant parasites for the antimalarial drug cabamiquine.

Stadler E, Maiga M, Friedrich L, Thathy V, Demarta-Gatsi C, Dara A, Sogore F, Striepen J, Oeuvray C, Djimdé AA, Lee MCS, Dembélé L, Fidock DA, Khoury DS, Spangenberg T.

Nature communications 2023;Aug 25;14(1):5205. doi: 10.1038/s41467-023-40974-8

Activity of Ivermectin and Its Metabolites against Asexual Blood Stage Plasmodium falciparum and Its Interactions with Antimalarial Drugs.

Yipsirimetee A, Tipthara P, Hanboonkunupakarn B, Tripura R, Lek D, Kümpornsin K, Lee MCS, Sattabongkot J, Dondorp AM, White NJ, Kobylinski KC, Tarning J, Chotivanich K.

Antimicrobial agents and chemotherapy 2023;e0173022

Generation of a mutator parasite to drive resistome discovery in Plasmodium falciparum.

Kümpornsin K, Kochakarn T, Yeo T, Okombo J, Luth MR, Hoshizaki J, Rawat M, Pearson RD, Schindler KA, Mok S, Park H, Uhlemann AC, Jana GP, Maity BC, Laleu B, Chenu E, Duffy J, Moliner Cubel S, Franco V, Gomez-Lorenzo MG, Gamo FJ, Winzeler EA, Fidock DA, Chookajorn T, Lee MCS.

Nature communications 2023 May 27;14(1):3059. doi: 10.1038/s41467-023-38774-1.

Advances in malaria pharmacology and the online guide to MALARIA PHARMACOLOGY: IUPHAR review 38.

Armstrong JF, Campo B, Alexander SPH, Arendse LB, Cheng X, Davenport AP, Faccenda E, Fidock DA, Godinez-Macias KP, Harding SD, Kato N, Lee MCS, Luth MR, Mazitschek R, Mittal N, Niles JC, Okombo J, Ottilie S, Pasaje CFA, Probst AS, Rawat M, Rocamora F, Sakata-Kato T, Southan C, Spedding M, Tye MA, Yang T, Zhao N, Davies JA.

British Journal of Pharmacology 2023 Aug;180(15):1899-1929. doi: 10.1111/bph.16144.

Integrative Genetic Manipulation of Plasmodium cynomolgi Reveals Multidrug Resistance-1 Y976F Associated With Increased In Vitro Susceptibility to Mefloquine.

Ward KE, Christensen P, Racklyeft A, Dhingra SK, Chua ACY, Remmert C, Suwanarusk R, Matheson J, Blackman MJ, Kaneko O, Kyle DE, Lee MCS, Moon RW, Snounou G, Rénia L, Fidock DA, Russell B, Bifani P.

The Journal of Infectious Diseases 2023;227;10;1121-1126

Cytoplasmic isoleucyl tRNA synthetase as an attractive multistage antimalarial drug target.

Istvan ES, Guerra F, Abraham M, Huang KS, Rocamora F, Zhao H, Xu L, Pasaje C, Kumpornsin K, Luth MR, Cui H, Yang T, Palomo Diaz S, Gomez-Lorenzo MG, Qahash T, Mittal N, Ottilie S, Niles J, Lee MCS, Llinas M, Kato N, Okombo J, Fidock DA, Schimmel P, Gamo FJ, Goldberg DE, Winzeler EA.

Science Translational Medicine 2023;15;686;eadc9249

A transcriptional switch controls sex determination in Plasmodium falciparum.

Gomes AR, Marin-Menendez A, Adjalley SH, Bardy C, Cassan C, Lee MCS and Talman AM

Nature 2022;612;7940;528-533

A manually curated annotation characterises genomic features of P. falciparum lncRNAs.

Hoshizaki J, Adjalley SH, Thathy V, Judge K, Berriman M, Reid AJ and Lee MCS

BMC genomics 2022;23;1;780

A G358S mutation in the Plasmodium falciparum Na+ pump PfATP4 confers clinically-relevant resistance to cipargamin.

Qiu D, Pei JV, Rosling JEO, Thathy V, Li D, Xue Y, Tanner JD, Penington JS, Aw YTV, Aw JYH, Xu G, Tripathi AK, Gnadig NF, Yeo T, Fairhurst KJ, Stokes BH, Murithi JM, Kümpornsin K, Hasemer H, Dennis ASM, Ridgway MC, Schmitt EK, Straimer J, Papenfuss AT, Lee MCS, Corry B, Sinnis P, Fidock DA, van Dooren GG, Kirk K, Lehane AM.

Nature communications 2022;13;1;57463

Efficient generation of mNeonGreen Plasmodium falciparum reporter lines enables quantitative fitness analysis.

Hoshizaki J, Jagoe H and Lee MCS

Frontiers in cellular and infection microbiology 2022;12;981432

Barcoding Genetically Distinct Plasmodium falciparum Strains for Comparative Assessment of Fitness and Antimalarial Drug Resistance.

Carrasquilla M, Drammeh NF, Rawat M, Sanderson T, Zenonos Z, Rayner JC and Lee MCS

mBio 2022;13;5;e0093722

Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy.

Science 2022;376;6597;1074-1079

CRISPR/Cas9 Editing of the Plasmodium falciparum Genome.

Adjalley S and Lee MCS

Methods in molecular biology (Clifton, N.J.) 2022;2470;221-239

Lumefantrine attenuates Plasmodium falciparum artemisinin resistance during the early ring stage.

Kümpornsin K, Loesbanluechai D, de Cozar C, Kotanan N, Chotivanich K, White NJ, Wilairat P, Gomez-Lorenzo MG, Gamo FJ, Sanz LM et al.

International journal for parasitology. Drugs and drug resistance 2021;17;186-190

Prioritization of Molecular Targets for Antimalarial Drug Discovery.

Forte B, Ottilie S, Plater A, Campo B, Dechering KJ, Gamo FJ, Goldberg DE, Istvan ES, Lee M, Lukens AK et al.

ACS infectious diseases 2021;7;10;2764-2776

Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention.

Summers RL, Pasaje CFA, Pisco JP, Striepen J, Luth MR, Kumpornsin K, Carpenter EF, Munro JT, Lin D, Plater A et al.

Cell chemical biology 2021;29;2;191-201.e8

Scientists on a RAMPAGE to find apicomplexan transcription start sites.

Hoshizaki J and Lee MCS

Nature reviews. Microbiology 2021;19;8;483

MalDA, Accelerating Malaria Drug Discovery.

Yang T, Ottilie S, Istvan ES, Godinez-Macias KP, Lukens AK, Baragaña B, Campo B, Walpole C, Niles JC, Chibale K et al.

Trends in parasitology 2021;37;6;493-507

The Key Glycolytic Enzyme Phosphofructokinase Is Involved in Resistance to Antiplasmodial Glycosides.

Fisher GM, Cobbold SA, Jezewski A, Carpenter EF, Arnold M, Cowell AN, Tjhin ET, Saliba KJ, Skinner-Adams TS, Lee MCS et al.

mBio 2020;11;6

Defining multiplicity of vector uptake in transfected Plasmodium parasites.

Carrasquilla M, Adjalley S, Sanderson T, Marin-Menendez A, Coyle R, Montandon R, Rayner JC, Pance A and Lee MCS

Scientific reports 2020;10;1;10894

Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity.

Vanaerschot M, Murithi JM, Pasaje CFA, Ghidelli-Disse S, Dwomoh L, Bird M, Spottiswoode N, Mittal N, Arendse LB, Owen ES et al.

Cell chemical biology 2020;27;7;806-816.e8

Insights into the intracellular localization, protein associations and artemisinin resistance properties of Plasmodium falciparum K13.

Gnädig NF, Stokes BH, Edwards RL, Kalantarov GF, Heimsch KC, Kuderjavy M, Crane A, Lee MCS, Straimer J, Becker K et al.

PLoS pathogens 2020;16;4;e1008482

Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway.

LaMonte GM, Rocamora F, Marapana DS, Gnädig NF, Ottilie S, Luth MR, Worgall TS, Goldgof GM, Mohunlal R, Santha Kumar TR et al.

Nature communications 2020;11;1;1780

The Antimalarial Natural Product Salinipostin A Identifies Essential α/β Serine Hydrolases Involved in Lipid Metabolism in P. falciparum Parasites.

Yoo E, Schulze CJ, Stokes BH, Onguka O, Yeo T, Mok S, Gnädig NF, Zhou Y, Kurita K, Foe IT et al.

Cell chemical biology 2020;27;2;143-157.e5

Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery.

Murithi JM, Owen ES, Istvan ES, Lee MCS, Ottilie S, Chibale K, Goldberg DE, Winzeler EA, Llinás M, Fidock DA and Vanaerschot M

Cell chemical biology 2019;27;2;158-171.e3

Nedd8 hydrolysis by UCH proteases in Plasmodium parasites.

Karpiyevich M, Adjalley S, Mol M, Ascher DB, Mason B, van der Heden van Noort GJ, Laman H, Ovaa H, Lee MCS and Artavanis-Tsakonas K

PLoS pathogens 2019;15;10;e1008086

Cutting back malaria: CRISPR/Cas9 genome editing of Plasmodium.

Lee MCS, Lindner SE, Lopez-Rubio JJ and Llinás M

Briefings in functional genomics 2019;18;5;281-289

Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics

Cowell, A. N., Istvan, E. S., Lukens, A. K., Gomez-Lorenzo, M. G., Vanaerschot, M., Sakata-Kato, T., Flannery, E. L., Magistrado, P., Owen, E., Abraham, M., LaMonte, G., Painter, H. J., Williams, R. M., Franco, V., Linares, M., Arriaga, I., Bopp, S., Corey, V. C., Gnädig, N. F., Coburn-Flynn, O., … Winzeler, E. A.

Science, 359(6372), 191–199 (2018)

Identification and Mechanistic Understanding of Dihydroorotate Dehydrogenase Point Mutations in Plasmodium falciparum that Confer in Vitro Resistance to the Clinical Candidate DSM265

White, J., Dhingra, S. K., Deng, X., El Mazouni, F., Lee, M. C. S., Afanador, G. A., Lawong, A., Tomchick, D. R., Ng, C. L., Bath, J., Rathod, P. K., Fidock, D. A., & Phillips, M. A.

ACS infectious diseases, 5(1), 90–101 (2018)

A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue

Sonoiki, E., Ng, C. L., Lee, M. C., Guo, D., Zhang, Y. K., Zhou, Y., Alley, M. R., Ahyong, V., Sanz, L. M., Lafuente-Monasterio, M. J., Dong, C., Schupp, P. G., Gut, J., Legac, J., Cooper, R. A., Gamo, F. J., DeRisi, J., Freund, Y. R., Fidock, D. A., & Rosenthal, P. J.

Nature communications, 8, 14574 (2017)

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodiumphosphatidylinositol 4-kinase

Paquet, T., Le Manach, C., Cabrera, D. G., Younis, Y., Henrich, P. P., Abraham, T. S., Lee, M. C. S., Basak, R., Ghidelli-Disse, S., Lafuente-Monasterio, M. J., Bantscheff, M., Ruecker, A., Blagborough, A. M., Zakutansky, S. E., Zeeman, A. M., White, K. L., Shackleford, D. M., Mannila, J., Morizzi, J., Scheurer, C., … Chibale, K.

Science translational medicine, 9(387), eaad9735 (2017)

A broad analysis of resistance development in the malaria parasite

Corey, V. C., Lukens, A. K., Istvan, E. S., Lee, M. C. S., Franco, V., Magistrado, P., Coburn-Flynn, O., Sakata-Kato, T., Fuchs, O., Gnädig, N. F., Goldgof, G., Linares, M., Gomez-Lorenzo, M. G., De Cózar, C., Lafuente-Monasterio, M. J., Prats, S., Meister, S., Tanaseichuk, O., Wree, M., Zhou, Y., … Winzeler, E. A

Nature communications, 7, 11901 (2016)

CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs

Ng, C. L., Siciliano, G., Lee, M. C., de Almeida, M. J., Corey, V. C., Bopp, S. E., Bertuccini, L., Wittlin, S., Kasdin, R. G., Le Bihan, A., Clozel, M., Winzeler, E. A., Alano, P., & Fidock, D. A

Molecular microbiology, 101(3), 381–393 (2016)

UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes

Lim, M. Y., LaMonte, G., Lee, M. C. S., Reimer, C., Tan, B. H., Corey, V., Tjahjadi, B. F., Chua, A., Nachon, M., Wintjens, R., Gedeck, P., Malleret, B., Renia, L., Bonamy, G. M. C., Ho, P. C., Yeung, B. K. S., Chow, E. D., Lim, L., Fidock, D. A., Diagana, T. T., … Bifani, P

Nature microbiology, 1, 16166. (2016)

A novel multiple-stage antimalarial agent that inhibits protein synthesis

Baragaña, B., Hallyburton, I., Lee, M. et al.

Nature 522, 315–320 (2015).

Profiling the Essential Nature of Lipid Metabolism in Asexual Blood and Gametocyte Stages of Plasmodium falciparum

Gulati, S., Ekland, E. H., Ruggles, K. V., Chan, R. B., Jayabalasingham, B., Zhou, B., Mantel, P. Y., Lee, M. C., Spottiswoode, N., Coburn-Flynn, O., Hjelmqvist, D., Worgall, T. S., Marti, M., Di Paolo, G., & Fidock, D. A