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Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center.
Freund YR, Akama T, Alley MR, Antunes J, Dong C, Jarnagin K, Kimura R, Nieman JA, Maples KR, Plattner JJ, Rock F, Sharma R, Singh R, Sanders V, Zhou Y. Freund YR, et al. Among authors: nieman ja. FEBS Lett. 2012 Sep 21;586(19):3410-4. doi: 10.1016/j.febslet.2012.07.058. Epub 2012 Jul 25. FEBS Lett. 2012. PMID: 22841723 Free article.
Discovery of a novel class of boron-based antibacterials with activity against gram-negative bacteria.
Hernandez V, Crépin T, Palencia A, Cusack S, Akama T, Baker SJ, Bu W, Feng L, Freund YR, Liu L, Meewan M, Mohan M, Mao W, Rock FL, Sexton H, Sheoran A, Zhang Y, Zhang YK, Zhou Y, Nieman JA, Anugula MR, Keramane el M, Savariraj K, Reddy DS, Sharma R, Subedi R, Singh R, O'Leary A, Simon NL, De Marsh PL, Mushtaq S, Warner M, Livermore DM, Alley MR, Plattner JJ. Hernandez V, et al. Among authors: nieman ja. Antimicrob Agents Chemother. 2013 Mar;57(3):1394-403. doi: 10.1128/AAC.02058-12. Epub 2013 Jan 7. Antimicrob Agents Chemother. 2013. PMID: 23295920 Free PMC article.
2-Aryl-2-hydroxyethylamine substituted 4-oxo-4,7-dihydrothieno[2,3-b]pyridines as broad-spectrum inhibitors of human herpesvirus polymerases.
Schnute ME, Anderson DJ, Brideau RJ, Ciske FL, Collier SA, Cudahy MM, Eggen M, Genin MJ, Hopkins TA, Judge TM, Kim EJ, Knechtel ML, Nair SK, Nieman JA, Oien NL, Scott A, Tanis SP, Vaillancourt VA, Wathen MW, Wieber JL. Schnute ME, et al. Among authors: nieman ja. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3349-53. doi: 10.1016/j.bmcl.2007.03.102. Epub 2007 Apr 5. Bioorg Med Chem Lett. 2007. PMID: 17434304
Peptidomimetic α-Acyloxymethylketone Warheads with Six-Membered Lactam P1 Glutamine Mimic: SARS-CoV-2 3CL Protease Inhibition, Coronavirus Antiviral Activity, and in Vitro Biological Stability.
Bai B, Belovodskiy A, Hena M, Kandadai AS, Joyce MA, Saffran HA, Shields JA, Khan MB, Arutyunova E, Lu J, Bajwa SK, Hockman D, Fischer C, Lamer T, Vuong W, van Belkum MJ, Gu Z, Lin F, Du Y, Xu J, Rahim M, Young HS, Vederas JC, Tyrrell DL, Lemieux MJ, Nieman JA. Bai B, et al. Among authors: nieman ja. J Med Chem. 2022 Feb 24;65(4):2905-2925. doi: 10.1021/acs.jmedchem.1c00616. Epub 2021 Jul 9. J Med Chem. 2022. PMID: 34242027
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, He M, Hogan RJ, Kozminski K, Li LY, Lockner JW, Lou J, Marra MT, Mitchell LJ Jr, Murray BW, Nieman JA, Noell S, Planken SP, Rowe T, Ryan K, Smith GJ 3rd, Solowiej JE, Steppan CM, Taggart B. Hoffman RL, et al. Among authors: nieman ja. J Med Chem. 2020 Nov 12;63(21):12725-12747. doi: 10.1021/acs.jmedchem.0c01063. Epub 2020 Oct 15. J Med Chem. 2020. PMID: 33054210
Improved SARS-CoV-2 Mpro inhibitors based on feline antiviral drug GC376: Structural enhancements, increased solubility, and micellar studies.
Vuong W, Fischer C, Khan MB, van Belkum MJ, Lamer T, Willoughby KD, Lu J, Arutyunova E, Joyce MA, Saffran HA, Shields JA, Young HS, Nieman JA, Tyrrell DL, Lemieux MJ, Vederas JC. Vuong W, et al. Among authors: nieman ja. Eur J Med Chem. 2021 Oct 15;222:113584. doi: 10.1016/j.ejmech.2021.113584. Epub 2021 May 30. Eur J Med Chem. 2021. PMID: 34118724 Free PMC article. Review.
HIV capsid is a tractable target for small molecule therapeutic intervention.
Blair WS, Pickford C, Irving SL, Brown DG, Anderson M, Bazin R, Cao J, Ciaramella G, Isaacson J, Jackson L, Hunt R, Kjerrstrom A, Nieman JA, Patick AK, Perros M, Scott AD, Whitby K, Wu H, Butler SL. Blair WS, et al. Among authors: nieman ja. PLoS Pathog. 2010 Dec 9;6(12):e1001220. doi: 10.1371/journal.ppat.1001220. PLoS Pathog. 2010. PMID: 21170360 Free PMC article.
27 results