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β-Glucocerebrosidase Modulators Promote Dimerization of β-Glucocerebrosidase and Reveal an Allosteric Binding Site.
Zheng J, Chen L, Skinner OS, Ysselstein D, Remis J, Lansbury P, Skerlj R, Mrosek M, Heunisch U, Krapp S, Charrow J, Schwake M, Kelleher NL, Silverman RB, Krainc D. Zheng J, et al. Among authors: skerlj r. J Am Chem Soc. 2018 May 9;140(18):5914-5924. doi: 10.1021/jacs.7b13003. Epub 2018 Apr 30. J Am Chem Soc. 2018. PMID: 29676907 Free PMC article.
A randomized single and multiple ascending dose study in healthy volunteers of LTI-291, a centrally penetrant glucocerebrosidase activator.
den Heijer JM, Kruithof AC, van Amerongen G, de Kam ML, Thijssen E, Grievink HW, Moerland M, Walker M, Been K, Skerlj R, Justman C, Dudgeon L, Lansbury P, Cullen VC, Hilt DC, Groeneveld GJ. den Heijer JM, et al. Among authors: skerlj r. Br J Clin Pharmacol. 2021 Sep;87(9):3561-3573. doi: 10.1111/bcp.14772. Epub 2021 Mar 2. Br J Clin Pharmacol. 2021. PMID: 33576113 Free PMC article.
Lead Optimization of Benzoxazolone Carboxamides as Orally Bioavailable and CNS Penetrant Acid Ceramidase Inhibitors.
Di Martino S, Tardia P, Cilibrasi V, Caputo S, Mazzonna M, Russo D, Penna I, Realini N, Margaroli N, Migliore M, Pizzirani D, Ottonello G, Bertozzi SM, Armirotti A, Nguyen D, Sun Y, Bongarzone ER, Lansbury P, Liu M, Skerlj R, Scarpelli R. Di Martino S, et al. Among authors: skerlj r. J Med Chem. 2020 Apr 9;63(7):3634-3664. doi: 10.1021/acs.jmedchem.9b02004. Epub 2020 Mar 26. J Med Chem. 2020. PMID: 32176488 Free PMC article.
Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.
Caputo S, Di Martino S, Cilibrasi V, Tardia P, Mazzonna M, Russo D, Penna I, Summa M, Bertozzi SM, Realini N, Margaroli N, Migliore M, Ottonello G, Liu M, Lansbury P, Armirotti A, Bertorelli R, Ray SS, Skerlj R, Scarpelli R. Caputo S, et al. Among authors: skerlj r. J Med Chem. 2020 Dec 24;63(24):15821-15851. doi: 10.1021/acs.jmedchem.0c01561. Epub 2020 Dec 8. J Med Chem. 2020. PMID: 33290061 Free PMC article.
Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, Langille J, Di Fluri M, Bogucki D, Yang W, Li T, Wang L, Nan S, Baird I, Metz M, Darkes M, Labrecque J, Lau G, Fricker S, Huskens D, Schols D. Skerlj R, et al. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2450-5. doi: 10.1016/j.bmcl.2011.02.058. Epub 2011 Feb 23. Bioorg Med Chem Lett. 2011. PMID: 21398122
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Langille J, Harwig C, Veale D, Yang W, Li T, Zhu Y, Bey M, Baird I, Sartori M, Metz M, Mosi R, Nelson K, Bodart V, Wong R, Fricker S, Mac Farland R, Huskens D, Schols D. Skerlj R, et al. Bioorg Med Chem Lett. 2011 Dec 1;21(23):6950-4. doi: 10.1016/j.bmcl.2011.09.133. Epub 2011 Oct 8. Bioorg Med Chem Lett. 2011. PMID: 22033460
Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Skerlj R, Bridger G, McEachern E, Harwig C, Smith C, Wilson T, Veale D, Yee H, Crawford J, Skupinska K, Wauthy R, Yang W, Zhu Y, Bogucki D, Di Fluri M, Langille J, Huskens D, De Clercq E, Schols D. Skerlj R, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):262-6. doi: 10.1016/j.bmcl.2010.11.023. Epub 2010 Nov 6. Bioorg Med Chem Lett. 2011. PMID: 21109432
47 results