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Mapping the genomic landscape of multidrug resistance in Plasmodium falciparum and its impact on parasite fitness.
Mok S, Yeo T, Hong D, Shears MJ, Ross LS, Ward KE, Dhingra SK, Kanai M, Bridgford JL, Tripathi AK, Mlambo G, Burkhard AY, Ansbro MR, Fairhurst KJ, Gil-Iturbe E, Park H, Rozenberg FD, Kim J, Mancia F, Fairhurst RM, Quick M, Uhlemann AC, Sinnis P, Fidock DA. Mok S, et al. Among authors: fairhurst kj. Sci Adv. 2023 Nov 10;9(45):eadi2364. doi: 10.1126/sciadv.adi2364. Epub 2023 Nov 8. Sci Adv. 2023. PMID: 37939186 Free PMC article.
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. Qiu D, et al. Among authors: fairhurst kj. Nat Commun. 2022 Sep 30;13(1):5746. doi: 10.1038/s41467-022-33403-9. Nat Commun. 2022. PMID: 36180431 Free PMC article.
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362.
Lowe MA, Cardenas A, Valentin JP, Zhu Z, Abendroth J, Castro JL, Class R, Delaunois A, Fleurance R, Gerets H, Gryshkova V, King L, Lorimer DD, MacCoss M, Rowley JH, Rosseels ML, Royer L, Taylor RD, Wong M, Zaccheo O, Chavan VP, Ghule GA, Tapkir BK, Burrows JN, Duffey M, Rottmann M, Wittlin S, Angulo-Barturen I, Jiménez-Díaz MB, Striepen J, Fairhurst KJ, Yeo T, Fidock DA, Cowman AF, Favuzza P, Crespo-Fernandez B, Gamo FJ, Goldberg DE, Soldati-Favre D, Laleu B, de Haro T. Lowe MA, et al. Among authors: fairhurst kj. J Med Chem. 2022 Oct 27;65(20):14121-14143. doi: 10.1021/acs.jmedchem.2c01336. Epub 2022 Oct 10. J Med Chem. 2022. PMID: 36216349 Free PMC article.
Mitigating the risk of antimalarial resistance via covalent dual-subunit inhibition of the Plasmodium proteasome.
Deni I, Stokes BH, Ward KE, Fairhurst KJ, Pasaje CFA, Yeo T, Akbar S, Park H, Muir R, Bick DS, Zhan W, Zhang H, Liu YJ, Ng CL, Kirkman LA, Almaliti J, Gould AE, Duffey M, O'Donoghue AJ, Uhlemann AC, Niles JC, da Fonseca PCA, Gerwick WH, Lin G, Bogyo M, Fidock DA. Deni I, et al. Among authors: fairhurst kj. Cell Chem Biol. 2023 May 18;30(5):470-485.e6. doi: 10.1016/j.chembiol.2023.03.002. Epub 2023 Mar 23. Cell Chem Biol. 2023. PMID: 36963402 Free PMC article.
Mapping the genomic landscape of multidrug resistance in Plasmodium falciparum and its impact on parasite fitness.
Mok S, Yeo T, Hong D, Shears MJ, Ross LS, Ward KE, Dhingra SK, Kanai M, Bridgford JL, Tripathi AK, Mlambo G, Burkhard AY, Fairhurst KJ, Gil-Iturbe E, Park H, Rozenberg FD, Kim J, Mancia F, Quick M, Uhlemann AC, Sinnis P, Fidock DA. Mok S, et al. Among authors: fairhurst kj. bioRxiv [Preprint]. 2023 Jun 3:2023.06.02.543338. doi: 10.1101/2023.06.02.543338. bioRxiv. 2023. PMID: 37398288 Free PMC article. Updated. Preprint.
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. Xie SC, et al. Among authors: fairhurst kj. Res Sq [Preprint]. 2023 Jul 27:rs.3.rs-3198291. doi: 10.21203/rs.3.rs-3198291/v1. Res Sq. 2023. PMID: 37546892 Free PMC article. Updated. Preprint.
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. Xie SC, et al. Among authors: fairhurst kj. Nat Commun. 2024 Jan 31;15(1):937. doi: 10.1038/s41467-024-45224-z. Nat Commun. 2024. PMID: 38297033 Free PMC article.
Activity refinement of aryl amino acetamides that target the P. falciparum STAR-related lipid transfer 1 protein.
Nguyen W, Boulet C, Dans MG, Loi K, Jarman KE, Watson GM, Tham WH, Fairhurst KJ, Yeo T, Fidock DA, Wittlin S, Chowdury M, de Koning-Ward TF, Chen G, Yan D, Charman SA, Baud D, Brand S, Jackson PF, Cowman AF, Gilson PR, Sleebs BE. Nguyen W, et al. Among authors: fairhurst kj. Eur J Med Chem. 2024 Apr 15;270:116354. doi: 10.1016/j.ejmech.2024.116354. Epub 2024 Mar 25. Eur J Med Chem. 2024. PMID: 38554474 Free article.