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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: uhlemann ac. 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.
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, Terrell SM, Boucher MJ, Cieplak P, Kumpornsin K, Lee MCS, Linington RG, Long JZ, Uhlemann AC, Weerapana E, Fidock DA, Bogyo M. Yoo E, et al. Among authors: uhlemann ac. Cell Chem Biol. 2020 Feb 20;27(2):143-157.e5. doi: 10.1016/j.chembiol.2020.01.001. Epub 2020 Jan 23. Cell Chem Biol. 2020. PMID: 31978322 Free PMC article.
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, Wicht KJ, Siciliano G, Bösche M, Yeo T, Kumar TRS, Mok S, Carpenter EF, Giddins MJ, Sanz O, Ottilie S, Alano P, Chibale K, Llinás M, Uhlemann AC, Delves M, Tobin AB, Doerig C, Winzeler EA, Lee MCS, Niles JC, Fidock DA. Vanaerschot M, et al. Among authors: uhlemann ac. Cell Chem Biol. 2020 Jul 16;27(7):806-816.e8. doi: 10.1016/j.chembiol.2020.04.001. Epub 2020 Apr 30. Cell Chem Biol. 2020. PMID: 32359426 Free PMC article.
3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum.
Knaab TC, Held J, Burckhardt BB, Rubiano K, Okombo J, Yeo T, Mok S, Uhlemann AC, Lungerich B, Fischli C, Pessanha de Carvalho L, Mordmüller B, Wittlin S, Fidock DA, Kurz T. Knaab TC, et al. Among authors: uhlemann ac. J Med Chem. 2021 Mar 25;64(6):3035-3047. doi: 10.1021/acs.jmedchem.0c01744. Epub 2021 Mar 5. J Med Chem. 2021. PMID: 33666415 Free PMC article.
Repositioning and Characterization of 1-(Pyridin-4-yl)pyrrolidin-2-one Derivatives as Plasmodium Cytoplasmic Prolyl-tRNA Synthetase Inhibitors.
Okaniwa M, Shibata A, Ochida A, Akao Y, White KL, Shackleford DM, Duffy S, Lucantoni L, Dey S, Striepen J, Yeo T, Mok S, Aguiar ACC, Sturm A, Crespo B, Sanz LM, Churchyard A, Baum J, Pereira DB, Guido RVC, Dechering KJ, Wittlin S, Uhlemann AC, Fidock DA, Niles JC, Avery VM, Charman SA, Laleu B. Okaniwa M, et al. Among authors: uhlemann ac. ACS Infect Dis. 2021 Jun 11;7(6):1680-1689. doi: 10.1021/acsinfecdis.1c00020. Epub 2021 Apr 30. ACS Infect Dis. 2021. PMID: 33929818 Free PMC article.
The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance.
Murithi JM, Pascal C, Bath J, Boulenc X, Gnädig NF, Pasaje CFA, Rubiano K, Yeo T, Mok S, Klieber S, Desert P, Jiménez-Díaz MB, Marfurt J, Rouillier M, Cherkaoui-Rbati MH, Gobeau N, Wittlin S, Uhlemann AC, Price RN, Wirjanata G, Noviyanti R, Tumwebaze P, Cooper RA, Rosenthal PJ, Sanz LM, Gamo FJ, Joseph J, Singh S, Bashyam S, Augereau JM, Giraud E, Bozec T, Vermat T, Tuffal G, Guillon JM, Menegotto J, Sallé L, Louit G, Cabanis MJ, Nicolas MF, Doubovetzky M, Merino R, Bessila N, Angulo-Barturen I, Baud D, Bebrevska L, Escudié F, Niles JC, Blasco B, Campbell S, Courtemanche G, Fraisse L, Pellet A, Fidock DA, Leroy D. Murithi JM, et al. Among authors: uhlemann ac. Sci Transl Med. 2021 Jul 21;13(603):eabg6013. doi: 10.1126/scitranslmed.abg6013. Sci Transl Med. 2021. PMID: 34290058 Free PMC article.
193 results