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Page 1
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.
Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer.
Gonzalvez F, Vincent S, Baker TE, Gould AE, Li S, Wardwell SD, Nadworny S, Ning Y, Zhang S, Huang WS, Hu Y, Li F, Greenfield MT, Zech SG, Das B, Narasimhan NI, Clackson T, Dalgarno D, Shakespeare WC, Fitzgerald M, Chouitar J, Griffin RJ, Liu S, Wong KK, Zhu X, Rivera VM. Gonzalvez F, et al. Among authors: gould ae. Cancer Discov. 2021 Jul;11(7):1672-1687. doi: 10.1158/2159-8290.CD-20-1683. Epub 2021 Feb 25. Cancer Discov. 2021. PMID: 33632773
Discovery and optimization of pyrazolopyrimidine sulfamates as ATG7 inhibitors.
Huang SC, Adhikari S, Brownell JE, Calderwood EF, Chouitar J, D'Amore NR, England DB, Foley K, Harrison SJ, LeRoy PJ, Lok D, Lublinsky A, Ma LT, Menon S, Yang Y, Zhang J, Gould AE. Huang SC, et al. Among authors: gould ae. Bioorg Med Chem. 2020 Oct 1;28(19):115681. doi: 10.1016/j.bmc.2020.115681. Epub 2020 Aug 4. Bioorg Med Chem. 2020. PMID: 32912429 Free article.
21 results