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A potent and selective reaction hijacking inhibitor of Plasmodium falciparum tyrosine tRNA synthetase exhibits single dose oral efficacy in vivo.
Xie SC, Tai CW, Morton CJ, Ma L, Huang SC, Wittlin S, Du Y, Hu Y, Dogovski C, Salimimarand M, Griffin R, England D, de la Cruz E, Deni I, Yeo T, Burkhard AY, Striepen J, Schindler KA, Crespo B, Gamo FJ, Khandokar Y, Hutton CA, Rabie T, Birkholtz LM, Famodimu MT, Delves MJ, Bolsher J, Koolen KMJ, van der Laak R, Aguiar ACC, Pereira DB, Guido RVC, Creek DJ, Fidock DA, Dick LR, Brand SL, Gould AE, Langston S, Griffin MDW, Tilley L. Xie SC, et al. Among authors: gould ae. PLoS Pathog. 2024 Dec 9;20(12):e1012429. doi: 10.1371/journal.ppat.1012429. eCollection 2024 Dec. PLoS Pathog. 2024. PMID: 39652589 Free PMC article.
Identification of Small Molecule Inhibitors of PPM1D Using a Novel Drug Discovery Platform.
Jiang W, Shaw S, Rush J, Dumont N, Kim J, Singh R, Skepner A, Khodier C, Raffier C, Yan N, Schluter C, Yu X, Szuchnicki M, Sathappa M, Kahn J, Sperling AS, McKinney DC, Gould AE, Garvie CW, Miller PG. Jiang W, et al. Among authors: gould ae. bioRxiv [Preprint]. 2024 May 21:2024.05.20.595001. doi: 10.1101/2024.05.20.595001. bioRxiv. 2024. PMID: 38826457 Free PMC article. Preprint.
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: gould ae. 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.
Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non-small cell lung cancer.
Huang WS, Li F, Gong Y, Zhang Y, Youngsaye W, Xu Y, Zhu X, Greenfield MT, Kohlmann A, Taslimi PM, Toms A, Zech SG, Zhou T, Das B, Jang HG, Tugnait M, Ye YE, Gonzalvez F, Baker TE, Nadworny S, Ning Y, Wardwell SD, Zhang S, Gould AE, Hu Y, Lane W, Skene RJ, Zou H, Clackson T, Narasimhan NI, Rivera VM, Dalgarno DC, Shakespeare WC. Huang WS, et al. Among authors: gould ae. Bioorg Med Chem Lett. 2023 Jan 15;80:129084. doi: 10.1016/j.bmcl.2022.129084. Epub 2022 Nov 21. Bioorg Med Chem Lett. 2023. PMID: 36423823 Free article.
Susceptibilities of Ugandan Plasmodium falciparum Isolates to Proteasome Inhibitors.
Garg S, Kreutzfeld O, Chelebieva S, Tumwebaze PK, Byaruhanga O, Okitwi M, Orena S, Katairo T, Nsobya SL, Conrad MD, Aydemir O, Legac J, Gould AE, Bayles BR, Bailey JA, Duffey M, Lin G, Kirkman LA, Cooper RA, Rosenthal PJ. Garg S, et al. Among authors: gould ae. Antimicrob Agents Chemother. 2022 Oct 18;66(10):e0081722. doi: 10.1128/aac.00817-22. Epub 2022 Sep 12. Antimicrob Agents Chemother. 2022. PMID: 36094216 Free PMC article.
Reaction hijacking of tyrosine tRNA synthetase as a new whole-of-life-cycle antimalarial strategy.
Xie SC, Metcalfe RD, Dunn E, Morton CJ, Huang SC, Puhalovich T, Du Y, Wittlin S, Nie S, Luth MR, Ma L, Kim MS, Pasaje CFA, Kumpornsin K, Giannangelo C, Houghton FJ, Churchyard A, Famodimu MT, Barry DC, Gillett DL, Dey S, Kosasih CC, Newman W, Niles JC, Lee MCS, Baum J, Ottilie S, Winzeler EA, Creek DJ, Williamson N, Parker MW, Brand S, Langston SP, Dick LR, Griffin MDW, Gould AE, Tilley L. Xie SC, et al. Among authors: gould ae. Science. 2022 Jun 3;376(6597):1074-1079. doi: 10.1126/science.abn0611. Epub 2022 Jun 2. Science. 2022. PMID: 35653481 Free PMC article.
Design of proteasome inhibitors with oral efficacy in vivo against Plasmodium falciparum and selectivity over the human proteasome.
Xie SC, Metcalfe RD, Mizutani H, Puhalovich T, Hanssen E, Morton CJ, Du Y, Dogovski C, Huang SC, Ciavarri J, Hales P, Griffin RJ, Cohen LH, Chuang BC, Wittlin S, Deni I, Yeo T, Ward KE, Barry DC, Liu B, Gillett DL, Crespo-Fernandez BF, Ottilie S, Mittal N, Churchyard A, Ferguson D, Aguiar ACC, Guido RVC, Baum J, Hanson KK, Winzeler EA, Gamo FJ, Fidock DA, Baud D, Parker MW, Brand S, Dick LR, Griffin MDW, Gould AE, Tilley L. Xie SC, et al. Among authors: gould ae. Proc Natl Acad Sci U S A. 2021 Sep 28;118(39):e2107213118. doi: 10.1073/pnas.2107213118. Proc Natl Acad Sci U S A. 2021. PMID: 34548400 Free PMC article.
23 results