Malaria

Displaying 1 - 44 of 44CSV
Woodland, J. G., Coertzen, D., Wicht, K. J., Hidalgo, V. F., Pasaje, C. F. A., Godoy, L. C., Qahash, T., Mmonwa, M. M., Dziwornu, G. A., Wambua, L., Harries, S., Korkor, C. M., Njoroge, M., Krugmann, L., Taylor, D., Leshabane, M., Langeveld, H., Rabie, T., Reader, J., … Chibale, K. (2025). The ATM Kinase Inhibitor AZD0156 Is a Potent Inhibitor of Plasmodium Phosphatidylinositol 4‐Kinase (PI4Kβ) and Is an Attractive Candidate for Medicinal Chemistry Optimization Against Malaria. Angewandte Chemie International Edition. Portico. https://doi.org/10.1002/anie.202425206
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Proellochs, N. I., Andolina, C., Ramjith, J., Stoter, R., van Gemert, G.-J., Graumans, W., Campino, S., Vanheer, L. N., Okitwi, M., Tumwebaze, P. K., Conrad, M. D., Clark, T. G., Fidock, D. A., Ménard, D., Mok, S., & Bousema, T. (2025). Gametocyte production and transmission fitness of African and Asian Plasmodium falciparum isolates with differential susceptibility to artemisinins. Antimicrobial Agents and Chemotherapy. https://doi.org/10.1128/aac.01930-24
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Awalt, J. K., Ooi, Z. K., Ashton, T. D., Mansouri, M., Calic, P. P. S., Zhou, Q., Vasanthan, S., Lee, S., Loi, K., Jarman, K. E., Penington, J. S., Qiu, D., Zhang, X., Lehane, A. M., Mao, E. Y., Gancheva, M. R., Wilson, D. W., Giannangelo, C., MacRaild, C. A., … Sleebs, B. E. (2025). Optimization and Characterization of N-Acetamide Indoles as Antimalarials That Target PfATP4. Journal of Medicinal Chemistry, 68(8), 8933–8966. https://doi.org/10.1021/acs.jmedchem.5c00614
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Godinez-Macias, K. P., Chen, D., Wallis, J. L., Siegel, M. G., Adam, A., Bopp, S., Carolino, K., Coulson, L. B., Durst, G., Thathy, V., Esherick, L., Farringer, M. A., Flannery, E. L., Forte, B., Liu, T., Godoy Magalhaes, L., Gupta, A. K., Istvan, E. S., Jiang, T., … Winzeler, E. A. (2025). Revisiting the Plasmodium falciparum druggable genome using predicted structures and data mining. Npj Drug Discovery, 2(1). https://doi.org/10.1038/s44386-025-00006-5
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Rawat, M., Padalino, G., Adika, E., Okombo, J., Yeo, T., Brancale, A., Fidock, D. A., Hoffmann, K. F., & Lee, M. C. S. (2025). Quinoxaline-based anti-schistosomal compounds have potent anti-plasmodial activity. PLOS Pathogens, 21(2), e1012216. https://doi.org/10.1371/journal.ppat.1012216
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Hagenah, L. M., Yeo, T., Schindler, K. A., Jeon, J. H., Bloxham, T. S., Small-Saunders, J. L., Mok, S., & Fidock, D. A. (2024). Plasmodium falciparum African PfCRT Mutant Isoforms Conducive to Piperaquine Resistance Are Infrequent and Impart a Major Fitness Cost. The Journal of Infectious Diseases. https://doi.org/10.1093/infdis/jiae617
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Gomez-Gonzalez, P.-J., Gupta, A., Drought, L. G., Patel, A., Okombo, J., van der Watt, M., Walker-Gray, R., Schindler, K. A., Burkhard, A. Y., Yeo, T., Narwal, S. K., Bloxham, T. S., Flueck, C., Walker, E. M., Rey, J. A., Fairhurst, K. J., Reader, J., Park, H., Pollard, H. G., … Baker, D. A. (2024). Inhibitors of malaria parasite cyclic nucleotide phosphodiesterases block asexual blood-stage development and mosquito transmission. Science Advances, 10(49). https://doi.org/10.1126/sciadv.adq1383
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Bestgen, B., Jones, S., Thathy, V., Kuemmerle, A., Barcelo, C., Haouala, A., Gossen, D., Marx, M. W., Di Resta, I., Szramowska, M., Webster, R. A., Llewellyn, S., Ritacco, D. A., Yeo, T., Leroy, D., Barber, B. E., Fidock, D. A., Griffin, P., Lickliter, J., & Chalon, S. (2024). Safety, tolerability, pharmacokinetics, and antimalarial activity of MMV533: a phase 1a first-in-human, randomised, ascending dose and food effect study, and a phase 1b Plasmodium falciparum volunteer infection study. The Lancet Infectious Diseases. https://doi.org/10.1016/s1473-3099(24)00664-9
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Luth, M. R., Godinez-Macias, K. P., Chen, D., Okombo, J., Thathy, V., Cheng, X., Daggupati, S., Davies, H., Dhingra, S. K., Economy, J. M., Edgar, R. C. S., Gomez-Lorenzo, M. G., Istvan, E. S., Jado, J. C., LaMonte, G. M., Melillo, B., Mok, S., Narwal, S. K., Ndiaye, T., … Winzeler, E. A. (2024). Systematic in vitro evolution in Plasmodium falciparum reveals key determinants of drug resistance. Science, 386(6725). https://doi.org/10.1126/science.adk9893
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Ferreira, L. T., Cassiano, G. C., Alvarez, L. C. S., Okombo, J., Calit, J., Fontinha, D., Gil-Iturbe, E., Coyle, R., Andrade, C. H., Sunnerhagen, P., Bargieri, D. Y., Prudêncio, M., Quick, M., Cravo, P. V., Lee, M. C. S., Fidock, D. A., & Costa, F. T. M. (2024). A novel 4-aminoquinoline chemotype with multistage antimalarial activity and lack of cross-resistance with PfCRT and PfMDR1 mutants. PLOS Pathogens, 20(10), e1012627. https://doi.org/10.1371/journal.ppat.1012627
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Brettell, S. B., Janha, O., Begen, A., Cann, G., Sharma, S., Olaniyan, N., Yelland, T., Hole, A. J., Alam, B., Mayville, E., Gillespie, R., Capper, M., Fidock, D. A., Milligan, G., Clarke, D. J., Tobin, A. B., & Jamieson, A. G. (2024). Targeting PfCLK3 with Covalent Inhibitors: A Novel Strategy for Malaria Treatment. Journal of Medicinal Chemistry, 67(21), 18895–18910. https://doi.org/10.1021/acs.jmedchem.4c01300
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Awalt, J. K., Su, W., Nguyen, W., Loi, K., Jarman, K. E., Penington, J. S., Ramesh, S., Fairhurst, K. J., Yeo, T., Park, H., Uhlemann, A.-C., Chandra Maity, B., De, N., Mukherjee, P., Chakraborty, A., Churchyard, A., Famodimu, M. T., Delves, M. J., Baum, J., … Sleebs, B. E. (2024). Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b. European Journal of Medicinal Chemistry, 280, 116921. https://doi.org/10.1016/j.ejmech.2024.116921
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Calic, P. P. S., Ashton, T. D., Mansouri, M., Loi, K., Jarman, K. E., Qiu, D., Lehane, A. M., Roy, S., Rao, G. P., Maity, B., Wittlin, S., Crespo, B., Gamo, F.-J., Deni, I., Fidock, D. A., Chowdury, M., de Koning-Ward, T. F., Cowman, A. F., Jackson, P. F., … Sleebs, B. E. (2024). Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3. European Journal of Medicinal Chemistry, 276, 116677. https://doi.org/10.1016/j.ejmech.2024.116677
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Lawong, A., Gahalawat, S., Ray, S., Ho, N., Han, Y., Ward, K. E., Deng, X., Chen, Z., Kumar, A., Xing, C., Hosangadi, V., Fairhurst, K. J., Tashiro, K., Liszczak, G., Shackleford, D. M., Katneni, K., Chen, G., Saunders, J., Crighton, E., … Phillips, M. A. (2024). Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria. Cell Chemical Biology, 31(8), 1503-1517.e19. https://doi.org/10.1016/j.chembiol.2024.07.001
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Rosado-Quiñones, A. M., Colón-Lorenzo, E. E., Pala, Z. R., Bosch, J., Kudyba, K., Kudyba, H., Leed, S. E., Roncal, N., Baerga-Ortiz, A., Roche-Lima, A., Gerena, Y., Fidock, D. A., Roth, A., Vega-Rodríguez, J., & Serrano, A. E. (2024). Novel hydrazone compounds with broad-spectrum antiplasmodial activity and synergistic interactions with antimalarial drugs. Antimicrobial Agents and Chemotherapy. https://doi.org/10.1128/aac.01643-23
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Nguyen, W., Boulet, C., Dans, M. G., Loi, K., Jarman, K. E., Watson, G. M., Tham, W.-H., Fairhurst, K. J., Yeo, T., Fidock, D. A., Wittlin, S., Chowdury, M., de Koning-Ward, T. F., Chen, G., Yan, D., Charman, S. A., Baud, D., Brand, S., Jackson, P. F., … Sleebs, B. E. (2024). Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein. European Journal of Medicinal Chemistry, 270, 116354. https://doi.org/10.1016/j.ejmech.2024.116354
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Rosenthal, P. J., Asua, V., Bailey, J. A., Conrad, M. D., Ishengoma, D. S., Kamya, M. R., Rasmussen, C., Tadesse, F. G., Uwimana, A., & Fidock, D. A. (2024). The emergence of artemisinin partial resistance in Africa: how do we respond? The Lancet Infectious Diseases. https://doi.org/10.1016/s1473-3099(24)00141-5
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Hagenah, L. M., Dhingra, S. K., Small-Saunders, J. L., Qahash, T., Willems, A., Schindler, K. A., Rangel, G. W., Gil-Iturbe, E., Kim, J., Akhundova, E., Yeo, T., Okombo, J., Mancia, F., Quick, M., Roepe, P. D., Llinás, M., & Fidock, D. A. (2024). Additional PfCRT mutations driven by selective pressure for improved fitness can result in the loss of piperaquine resistance and altered Plasmodium falciparum physiology. MBio, 15(1). https://doi.org/10.1128/mbio.01832-23
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Stadler, E., Maiga, M., Friedrich, L., Thathy, V., Demarta-Gatsi, C., Dara, A., Sogore, F., Striepen, J., Oeuvray, C., Djimdé, A. A., Lee, M. C. S., Dembélé, L., Fidock, D. A., Khoury, D. S., & Spangenberg, T. (2023). Propensity of selecting mutant parasites for the antimalarial drug cabamiquine. Nature Communications, 14(1). https://doi.org/10.1038/s41467-023-40974-8
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Kümpornsin, K., Kochakarn, T., Yeo, T., Okombo, J., Luth, M. R., Hoshizaki, J., Rawat, M., Pearson, R. D., Schindler, K. A., Mok, S., Park, H., Uhlemann, A.-C., Jana, G. P., Maity, B. C., Laleu, B., Chenu, E., Duffy, J., Moliner Cubel, S., Franco, V., … Lee, M. C. S. (2023). Generation of a mutator parasite to drive resistome discovery in Plasmodium falciparum. Nature Communications, 14(1). https://doi.org/10.1038/s41467-023-38774-1
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Bopp, S., Pasaje, C. F. A., Summers, R. L., Magistrado-Coxen, P., Schindler, K. A., Corpas-Lopez, V., Yeo, T., Mok, S., Dey, S., Smick, S., Nasamu, A. S., Demas, A. R., Milne, R., Wiedemar, N., Corey, V., Gomez-Lorenzo, M. D. G., Franco, V., Early, A. M., Lukens, A. K., … Wirth, D. F. (2023). Potent acyl-CoA synthetase 10 inhibitors kill Plasmodium falciparum by disrupting triglyceride formation. Nature Communications, 14(1). https://doi.org/10.1038/s41467-023-36921-2
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Mok, S., Yeo, T., Hong, D., Shears, M. J., Ross, L. S., Ward, K. E., Dhingra, S. K., Kanai, M., Bridgford, J. L., Tripathi, A. K., Mlambo, G., Burkhard, A. Y., Ansbro, M. R., Fairhurst, K. J., Gil-Iturbe, E., Park, H., Rozenberg, F. D., Kim, J., Mancia, F., … Fidock, D. A. (2023). Mapping the genomic landscape of multidrug resistance in Plasmodium falciparum and its impact on parasite fitness. Science Advances, 9(45). https://doi.org/10.1126/sciadv.adi2364
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Namazzi, R., Idro, R., Kalibala, D., Ssenkusu, J., Akun, P., Mboizi, V., Gondwe, T. N., Munube, D., Kasirye, P., Nabaggala, C., John, C. C., Green, N. S., Robberstat, B., Hensbroek, B. van, Kuile, F. ter, Phiri, K. S., & Opoka, R. (2023). Malaria in Children with Sickle Cell Anaemia in Areas with Low, Moderate and High Transmission in Uganda. Blood, 142(Supplement 1), 5327–5327. https://doi.org/10.1182/blood-2023-189066
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Mihreteab, S., Platon, L., Berhane, A., Stokes, B. H., Warsame, M., Campagne, P., Criscuolo, A., Ma, L., Petiot, N., Doderer-Lang, C., Legrand, E., Ward, K. E., Zehaie Kassahun, A., Ringwald, P., Fidock, D. A., & Ménard, D. (2023). Increasing Prevalence of Artemisinin-Resistant HRP2-Negative Malaria in Eritrea. New England Journal of Medicine, 389(13), 1191–1202. https://doi.org/10.1056/nejmoa2210956
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Ward, K. E., Christensen, P., Racklyeft, A., Dhingra, S. K., Chua, A. C. Y., Remmert, C., Suwanarusk, R., Matheson, J., Blackman, M. J., Kaneko, O., Kyle, D. E., Lee, M. C. S., Moon, R. W., Snounou, G., Rénia, L., Fidock, D. A., Russell, B., & Bifani, P. (2022). Integrative Genetic Manipulation of Plasmodium cynomolgi Reveals Multidrug Resistance-1 Y976F Associated With Increased In Vitro Susceptibility to Mefloquine. The Journal of Infectious Diseases, 227(10), 1121–1126. https://doi.org/10.1093/infdis/jiac469
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Deni, I., Stokes, B. H., Ward, K. E., Fairhurst, K. J., Pasaje, C. F. A., Yeo, T., Akbar, S., Park, H., Muir, R., Bick, D. S., Zhan, W., Zhang, H., Liu, Y. J., Ng, C. L., Kirkman, L. A., Almaliti, J., Gould, A. E., Duffey, M., O’Donoghue, A. J., … Fidock, D. A. (2023). Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome. Cell Chemical Biology, 30(5), 470-485.e6. https://doi.org/10.1016/j.chembiol.2023.03.002
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Ashton, T. D., Dans, M. G., Favuzza, P., Ngo, A., Lehane, A. M., Zhang, X., Qiu, D., Chandra Maity, B., De, N., Schindler, K. A., Yeo, T., Park, H., Uhlemann, A.-C., Churchyard, A., Baum, J., Fidock, D. A., Jarman, K. E., Lowes, K. N., Baud, D., … Sleebs, B. E. (2023). Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4. Journal of Medicinal Chemistry, 66(5), 3540–3565. https://doi.org/10.1021/acs.jmedchem.2c02092
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Laleu, B., Rubiano, K., Yeo, T., Hallyburton, I., Anderson, M., Crespo‐Fernandez, B., Gamo, F., Antonova‐Koch, Y., Orjuela‐Sanchez, P., Wittlin, S., Jana, G. P., Maity, B. C., Chenu, E., Duffy, J., Sjö, P., Waterson, D., Winzeler, E., Guantai, E., Fidock, D. A., & Hansson, T. G. (2022). Exploring a Tetrahydroquinoline Antimalarial Hit from the Medicines for Malaria Pathogen Box and Identification of its Mode of Resistance as PfeEF2. ChemMedChem, 17(22). Portico. https://doi.org/10.1002/cmdc.202200393
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Okombo, J., Mok, S., Qahash, T., Yeo, T., Bath, J., Orchard, L. M., Owens, E., Koo, I., Albert, I., Llinás, M., & Fidock, D. A. (2022). Piperaquine-resistant PfCRT mutations differentially impact drug transport, hemoglobin catabolism and parasite physiology in Plasmodium falciparum asexual blood stages. PLOS Pathogens, 18(10), e1010926. https://doi.org/10.1371/journal.ppat.1010926
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Lowe, M. A., Cardenas, A., Valentin, J.-P., Zhu, Z., Abendroth, J., Castro, J. L., Class, R., Delaunois, A., Fleurance, R., Gerets, H., Gryshkova, V., King, L., Lorimer, D. D., MacCoss, M., Rowley, J. H., Rosseels, M.-L., Royer, L., Taylor, R. D., Wong, M., … de Haro, T. (2022). Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362. Journal of Medicinal Chemistry, 65(20), 14121–14143. https://doi.org/10.1021/acs.jmedchem.2c01336
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Qiu, D., Pei, J. V., Rosling, J. E. O., Thathy, V., Li, D., Xue, Y., Tanner, J. D., Penington, J. S., Aw, Y. T. V., Aw, J. Y. H., Xu, G., Tripathi, A. K., Gnadig, N. F., Yeo, T., Fairhurst, K. J., Stokes, B. H., Murithi, J. M., Kümpornsin, K., Hasemer, H., … Lehane, A. M. (2022). A G358S mutation in the Plasmodium falciparum Na+ pump PfATP4 confers clinically-relevant resistance to cipargamin. Nature Communications, 13(1). https://doi.org/10.1038/s41467-022-33403-9
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Xu, Y., Zhou, Z., Brooks, B., Ferguson, T., Obliosca, J., Huang, J., Kaneko, I., Iwanaga, S., Yuda, M., Tsuji, Y., Zhang, H., Luo, C. C., Jiang, X., Kong, X.-P., Tsuji, M., & Tison, C. K. (2022). Layer-by-Layer Delivery of Multiple Antigens Using Trimethyl Chitosan Nanoparticles as a Malaria Vaccine Candidate. Frontiers in Immunology, 13. https://doi.org/10.3389/fimmu.2022.900080
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Summers, R. L., Pasaje, C. F. A., Pisco, J. P., Striepen, J., Luth, M. R., Kumpornsin, K., Carpenter, E. F., Munro, J. T., Lin, D., Plater, A., Punekar, A. S., Shepherd, A. M., Shepherd, S. M., Vanaerschot, M., Murithi, J. M., Rubiano, K., Akidil, A., Ottilie, S., Mittal, N., … Lukens, A. K. (2022). Chemogenomics identifies acetyl-coenzyme A synthetase as a target for malaria treatment and prevention. Cell Chemical Biology, 29(2), 191-201.e8. https://doi.org/10.1016/j.chembiol.2021.07.010
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Nair, M. S., Huang, Y., Fidock, D. A., Towler, M. J., & Weathers, P. J. (2022). Artemisia annua L. hot-water extracts show potent activity in vitro against Covid-19 variants including delta. Journal of Ethnopharmacology, 284, 114797. https://doi.org/10.1016/j.jep.2021.114797
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Small-Saunders, J. L., Hagenah, L. M., Wicht, K. J., Dhingra, S. K., Deni, I., Kim, J., Vendome, J., Gil-Iturbe, E., Roepe, P. D., Mehta, M., Mancia, F., Quick, M., Eppstein, M. J., & Fidock, D. A. (2022). Evidence for the early emergence of piperaquine-resistant Plasmodium falciparum malaria and modeling strategies to mitigate resistance. PLOS Pathogens, 18(2), e1010278. https://doi.org/10.1371/journal.ppat.1010278
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Kanai, M., Yeo, T., Asua, V., Rosenthal, P. J., Fidock, D. A., & Mok, S. (2022). Comparative Analysis of Plasmodium falciparum Genotyping via SNP Detection, Microsatellite Profiling, and Whole-Genome Sequencing. Antimicrobial Agents and Chemotherapy, 66(1). https://doi.org/10.1128/aac.01163-21
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Paloque, L., Coppée, R., Stokes, B. H., Gnädig, N. F., Niaré, K., Augereau, J.-M., Fidock, D. A., Clain, J., & Benoit-Vical, F. (2022). Mutation in the Plasmodium falciparum BTB/POZ Domain of K13 Protein Confers Artemisinin Resistance. Antimicrobial Agents and Chemotherapy, 66(1). https://doi.org/10.1128/aac.01320-21
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McCarthy, J. S., Yalkinoglu, Ö., Odedra, A., Webster, R., Oeuvray, C., Tappert, A., Bezuidenhout, D., Giddins, M. J., Dhingra, S. K., Fidock, D. A., Marquart, L., Webb, L., Yin, X., Khandelwal, A., & Bagchus, W. M. (2021). Safety, pharmacokinetics, and antimalarial activity of the novel plasmodium eukaryotic translation elongation factor 2 inhibitor M5717: a first-in-human, randomised, placebo-controlled, double-blind, single ascending dose study and volunteer infection study. The Lancet Infectious Diseases, 21(12), 1713–1724. https://doi.org/10.1016/s1473-3099(21)00252-8
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Xie, S. C., Metcalfe, R. D., Mizutani, H., Puhalovich, T., Hanssen, E., Morton, C. J., Du, Y., Dogovski, C., Huang, S.-C., Ciavarri, J., Hales, P., Griffin, R. J., Cohen, L. H., Chuang, B.-C., Wittlin, S., Deni, I., Yeo, T., Ward, K. E., Barry, D. C., … Tilley, L. (2021). Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome. Proceedings of the National Academy of Sciences, 118(39). https://doi.org/10.1073/pnas.2107213118
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Forte, B., Ottilie, S., Plater, A., Campo, B., Dechering, K. J., Gamo, F. J., Goldberg, D. E., Istvan, E. S., Lee, M., Lukens, A. K., McNamara, C. W., Niles, J. C., Okombo, J., Pasaje, C. F. A., Siegel, M. G., Wirth, D., Wyllie, S., Fidock, D. A., Baragaña, B., … Gilbert, I. H. (2021). Prioritization of Molecular Targets for Antimalarial Drug Discovery. ACS Infectious Diseases, 7(10), 2764–2776. https://doi.org/10.1021/acsinfecdis.1c00322
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