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Optimization of TopoIV Potency, ADMET Properties, and hERG Inhibition of 5-Amino-1,3-dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Identification of a Lead with In Vivo Efficacy against MRSA.
J Med Chem. 2021 Oct 28;64(20):15214-15249. doi: 10.1021/acs.jmedchem.1c01250. Epub 2021 Oct 6.
J Med Chem. 2021.
PMID: 34614347
1,3-Dioxane-Linked Novel Bacterial Topoisomerase Inhibitors: Expanding Structural Diversity and the Antibacterial Spectrum.
Lu Y, Mann CA, Nolan S, Collins JA, Parker E, Papa J, Vibhute S, Jahanbakhsh S, Thwaites M, Hufnagel D, Hazbón MH, Moreno J, Stedman TT, Wittum T, Wozniak DJ, Osheroff N, Yalowich JC, Mitton-Fry MJ.
Lu Y, et al.
ACS Med Chem Lett. 2022 May 9;13(6):955-963. doi: 10.1021/acsmedchemlett.2c00111. eCollection 2022 Jun 9.
ACS Med Chem Lett. 2022.
PMID: 35707162
Free PMC article.
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Novel bacterial topoisomerase inhibitors derived from isomannide.
Okumu A, Lu Y, Dellos-Nolan S, Papa JL, Koci B, Cockroft NT, Gallucci J, Wozniak DJ, Yalowich JC, Mitton-Fry MJ.
Okumu A, et al. Among authors: papa jl.
Eur J Med Chem. 2020 Aug 1;199:112324. doi: 10.1016/j.ejmech.2020.112324. Epub 2020 Apr 28.
Eur J Med Chem. 2020.
PMID: 32402932
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Dioxane-Linked Amide Derivatives as Novel Bacterial Topoisomerase Inhibitors against Gram-Positive Staphylococcus aureus.
Lu Y, Papa JL, Nolan S, English A, Seffernick JT, Shkolnikov N, Powell J, Lindert S, Wozniak DJ, Yalowich J, Mitton-Fry MJ.
Lu Y, et al. Among authors: papa jl.
ACS Med Chem Lett. 2020 Oct 19;11(12):2446-2454. doi: 10.1021/acsmedchemlett.0c00428. eCollection 2020 Dec 10.
ACS Med Chem Lett. 2020.
PMID: 33335666
Free PMC article.
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hsa-miR-9-3p and hsa-miR-9-5p as Post-Transcriptional Modulators of DNA Topoisomerase IIα in Human Leukemia K562 Cells with Acquired Resistance to Etoposide.
Kania EE, Carvajal-Moreno J, Hernandez VA, English A, Papa JL, Shkolnikov N, Ozer HG, Yilmaz AS, Yalowich JC, Elton TS.
Kania EE, et al. Among authors: papa jl.
Mol Pharmacol. 2020 Mar;97(3):159-170. doi: 10.1124/mol.119.118315. Epub 2019 Dec 13.
Mol Pharmacol. 2020.
PMID: 31836624
Free PMC article.
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CRISPR/Cas9 Genome Editing of the Human Topoisomerase IIα Intron 19 5' Splice Site Circumvents Etoposide Resistance in Human Leukemia K562 Cells.
Hernandez VA, Carvajal-Moreno J, Papa JL, Shkolnikov N, Li J, Ozer HG, Yalowich JC, Elton TS.
Hernandez VA, et al. Among authors: papa jl.
Mol Pharmacol. 2021 Mar;99(3):226-241. doi: 10.1124/molpharm.120.000173. Epub 2021 Jan 14.
Mol Pharmacol. 2021.
PMID: 33446509
Free PMC article.
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Innate immune control of influenza virus interspecies adaptation.
Denz PJ, Speaks S, Kenney AD, Eddy AC, Papa JL, Roettger J, Scace SC, Hemann EA, Forero A, Webby RJ, Bowman AS, Yount JS.
Denz PJ, et al. Among authors: papa jl.
bioRxiv [Preprint]. 2023 Aug 23:2023.08.23.554491. doi: 10.1101/2023.08.23.554491.
bioRxiv. 2023.
PMID: 37662304
Free PMC article.
Preprint.
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