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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. Nat Commun. 2022 Sep 30;13(1):5746. doi: 10.1038/s41467-022-33403-9. Nat Commun. 2022. PMID: 36180431 Free PMC article.
Optimization of 2,3-Dihydroquinazolinone-3-carboxamides as Antimalarials Targeting PfATP4.
Ashton TD, Dans MG, Favuzza P, Ngo A, Lehane AM, Zhang X, Qiu D, Chandra Maity B, De N, Schindler KA, Yeo T, Park H, Uhlemann AC, Churchyard A, Baum J, Fidock DA, Jarman KE, Lowes KN, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. Ashton TD, et al. Among authors: qiu d. J Med Chem. 2023 Mar 9;66(5):3540-3565. doi: 10.1021/acs.jmedchem.2c02092. Epub 2023 Feb 22. J Med Chem. 2023. PMID: 36812492 Free PMC article.
Discovery of antiplasmodial pyridine carboxamides and thiocarboxamides.
Redway A, Spry C, Brown A, Wiedemann U, Fathoni I, Garnie LF, Qiu D, Egan TJ, Lehane AM, Jackson Y, Saliba KJ, Downer-Riley N. Redway A, et al. Among authors: qiu d. Int J Parasitol Drugs Drug Resist. 2024 Aug;25:100536. doi: 10.1016/j.ijpddr.2024.100536. Epub 2024 Apr 3. Int J Parasitol Drugs Drug Resist. 2024. PMID: 38663046 Free PMC article.
Optimization of pyrazolopyridine 4-carboxamides with potent antimalarial activity for which resistance is associated with the P. falciparum transporter ABCI3.
Calic PPS, Ashton TD, Mansouri M, Loi K, Jarman KE, Qiu D, Lehane AM, Roy S, Rao GP, Maity B, Wittlin S, Crespo B, Gamo FJ, Deni I, Fidock DA, Chowdury M, de Koning-Ward TF, Cowman AF, Jackson PF, Baud D, Brand S, Laleu B, Sleebs BE. Calic PPS, et al. Among authors: qiu d. Eur J Med Chem. 2024 Oct 5;276:116677. doi: 10.1016/j.ejmech.2024.116677. Epub 2024 Jul 14. Eur J Med Chem. 2024. PMID: 39024967 Free article.
Property and Activity Refinement of Dihydroquinazolinone-3-carboxamides as Orally Efficacious Antimalarials that Target PfATP4.
Ashton TD, Calic PPS, Dans MG, Ooi ZK, Zhou Q, Palandri J, Loi K, Jarman KE, Qiu D, Lehane AM, Maity BC, De N, Giannangelo C, MacRaild CA, Creek DJ, Mao EY, Gancheva MR, Wilson DW, Chowdury M, de Koning-Ward TF, Famodimu MT, Delves MJ, Pollard H, Sutherland CJ, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. Ashton TD, et al. Among authors: qiu d. J Med Chem. 2024 Aug 22;67(16):14493-14523. doi: 10.1021/acs.jmedchem.4c01241. Epub 2024 Aug 12. J Med Chem. 2024. PMID: 39134060 Free PMC article.
Lactam Truncation Yields a Dihydroquinazolinone Scaffold with Potent Antimalarial Activity that Targets PfATP4.
Ashton TD, Calic PPS, Dans MG, Kang Ooi Z, Zhou Q, Loi K, Jarman KE, Palandri J, Qiu D, Lehane AM, Maity B, De N, Famodimu MT, Delves MJ, Mao EY, Gancheva MR, Wilson DW, Chowdury M, de Koning-Ward TF, Baud D, Brand S, Jackson PF, Cowman AF, Sleebs BE. Ashton TD, et al. Among authors: qiu d. ChemMedChem. 2024 Dec 16;19(24):e202400549. doi: 10.1002/cmdc.202400549. Epub 2024 Oct 29. ChemMedChem. 2024. PMID: 39210733 Free PMC article.
1,995 results