Exploration and characterization of the antimalarial activity of cyclopropyl carboxamides that target the mitochondrial protein, cytochrome b

Authors: Awalt, Jon Kyle, Su, Wenyin, Nguyen, William, Loi, Katie, Jarman, Kate E., Penington, Jocelyn S., Ramesh, Saishyam, Fairhurst, Kate J., Yeo, Tomas, Park, Heekuk, Uhlemann, Anne-Catrin, Chandra Maity, Bikash, De, Nirupam, Mukherjee, Partha, Chakraborty, Arnish, Churchyard, Alisje, Famodimu, Mufuliat T., Delves, Michael J., Baum, Jake, Mittal, Nimisha, Winzeler, Elizabeth A., Papenfuss, Anthony T., Chowdury, Mrittika, de Koning-Ward, Tania F., Maier, Alexander G., van Dooren, Giel G., Baud, Delphine, Brand, Stephen, Fidock, David A., Jackson, Paul F., Cowman, Alan F., Dans, Madeline G., Sleebs, Brad E.

Source: In European Journal of Medicinal Chemistry 15 December 2024 280

Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria

Authors: Lawong, Aloysus, Gahalawat, Suraksha, Ray, Sneha, Ho, Nhi, Han, Yan, Ward, Kurt E., Deng, Xiaoyi, Chen, Zhe, Kumar, Ashwani, Xing, Chao, Hosangadi, Varun, Fairhurst, Kate J., Tashiro, Kyuto, Liszczak, Glen, Shackleford, David M., Katneni, Kasiram, Chen, Gong, Saunders, Jessica, Crighton, Elly, Casas, Arturo, Robinson, Joshua J., Imlay, Leah S., Zhang, Xiaoyu, Lemoff, Andrew, Zhao, Zhiyu, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Wittlin, Sergio, Campbell, Simon F., Fidock, David A., Laleu, Benoît, Charman, Susan A., Ready, Joseph M., Phillips, Margaret A.

Source: In Cell Chemical Biology 15 August 2024 31(8):1503-1517

Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein

Authors: Nguyen, William ^{a, b}, Boulet, Coralie ^c, Dans, Madeline G. ^{a, b}, Loi, Katie ^{a, b}, Jarman, Kate E. ^{a, b}, Watson, Gabrielle M. ^{a, b}, Tham, Wai-Hong ^{a, b}, Fairhurst, Kate J. ^d, Yeo, Tomas ^d, Fidock, David A. ^{d, e}, Wittlin, Sergio ^{f, g}, Chowdury, Mrittika ^{h, i}, de Koning-Ward, Tania F. ^{h, i}, Chen, Gong ^j, Yan, Dandan ^j, Charman, Susan A. ^j, Baud, Delphine ^k, Brand, Stephen ^k, Jackson, Paul F. ^l, Cowman, Alan F. ^{a, b}, Gilson, Paul R. ^c, Sleebs, Brad E. ^{a, b, ⁎}

Source: In European Journal of Medicinal Chemistry 15 April 2024 270

Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome

Authors: Deni, Ioanna, Stokes, Barbara H., Ward, Kurt E., Fairhurst, Kate J., Pasaje, Charisse Flerida A., Yeo, Tomas, Akbar, Shirin, Park, Heekuk, Muir, Ryan, Bick, Daniella S., Zhan, Wenhu, Zhang, Hao, Liu, Yi Jing, Ng, Caroline L., Kirkman, Laura A., Almaliti, Jehad, Gould, Alexandra E., Duffey, Maëlle, O'Donoghue, Anthony J., Uhlemann, Anne-Catrin, Niles, Jacquin C., da Fonseca, Paula C.A., Gerwick, William H., Lin, Gang, Bogyo, Matthew, Fidock, David A.

Source: In Cell Chemical Biology 18 May 2023 30(5):470-485

Anti-plasmodial limonoids from Khaya anthotheca (Welw.) C.DC.

Authors: Obbo, Christopher J.D., Mwangi, Elizabeth M., Kariuki, Samuel T., Gathirwa, Jeremiah W., Fairhurst, Kate J., Burkhard, Anna Y., Fidock, David A., Sadgrove, Nicholas, Langat, Moses K., Mas-Claret, Eduard, Mulholland, Dulcie A.

Source: In Phytochemistry Letters June 2024 61:1-6

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

Authors: Qiu, Deyun, Pei, Jinxin V., Rosling, James E. O., Thathy, Vandana, Li, Dongdi, Xue, Yi, Tanner, John D., Penington, Jocelyn Sietsma, Aw, Yi Tong Vincent, Aw, Jessica Yi Han, Xu, Guoyue, Tripathi, Abhai K., Gnadig, Nina F., Yeo, Tomas, Fairhurst, Kate J., Stokes, Barbara H., Murithi, James M., Kümpornsin, Krittikorn, Hasemer, Heath, Dennis, Adelaide S. M.

Source: Nature Communications; 9/30/2022, Vol. 13 Issue 1, p1-18, 18p

Subject Terms: PLASMODIUM falciparum, PLASMODIUM, ORAL drug administration, PARASITES, TOXOPLASMA gondii, ADENOSINE triphosphatase

Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362

Authors: Lowe, Martin A., Cardenas, Alvaro, Valentin, Jean-Pierre, Zhu, Zhaoning, Abendroth, Jan, Castro, Jose L., Class, Reiner, Delaunois, Annie, Fleurance, Renaud, Gerets, Helga, Gryshkova, Vitalina, King, Lloyd, Lorimer, Donald D., MacCoss, Malcolm, Rowley, Julian H., Rosseels, Marie-Luce, Royer, Leandro, Taylor, Richard D., Wong, Melanie, Zaccheo, Oliver, Chavan, Vishal P., Ghule, Gokul A., Tapkir, Bapusaheb K., Burrows, Jeremy N., Duffey, Maëlle, Rottmann, Matthias, Wittlin, Sergio, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Striepen, Josefine, Fairhurst, Kate J., Yeo, Tomas, Fidock, David A., Cowman, Alan F., Favuzza, Paola, Crespo-Fernandez, Benigno, Gamo, Francisco Javier, Goldberg, Daniel E., Soldati-Favre, Dominique, Laleu, Benoît, de Haro, Teresa

Source: Journal of Medicinal Chemistry; October 2022, Vol. 65 Issue: 20 p14121-14143, 23p

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Inhibitors of malaria parasite cyclic nucleotide phosphodiesterases block asexual blood-stage development and mosquito transmission.

Authors: Gomez-Gonzalez, Paula-Josefina¹, Gupta, Antima¹, Drought, Laura G.¹, Patel, Avnish¹, Okombo, John^2,3, van der Watt, Mariëtte⁴, Walker-Gray, Ryan¹, Schindler, Kyra A.^2,3, Burkhard, Anna Y.^2,3, Yeo, Tomas^2,3, Narwal, Sunil K.^2,3, Bloxham, Talia S.^3,5, Flueck, Christian¹, Walker, Eloise M.¹, Rey, Joshua A.¹, Fairhurst, Kate J.^2,3, Reader, Janette^4,6, Park, Heekuk^3,5, Pollard, Harry G.¹, Stewart, Lindsay B.¹

Source: Science Advances. 12/6/2024, Vol. 10 Issue 49, p1-19. 19p.

Subject Terms: *CYCLIC nucleotide phosphodiesterases, *PLASMODIUM, *WHOLE genome sequencing, *PARASITE life cycles, *DRUG discovery

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