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Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: zhu s. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20. Bioorg Med Chem Lett. 2015. PMID: 26497283
Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd. Gerritz SW, et al. Among authors: zhu s. J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2. J Med Chem. 2012. PMID: 23030502
Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.
Sheriff S, Beno BR, Zhai W, Kostich WA, McDonnell PA, Kish K, Goldfarb V, Gao M, Kiefer SE, Yanchunas J, Huang Y, Shi S, Zhu S, Dzierba C, Bronson J, Macor JE, Appiah KK, Westphal RS, O'Connell J, Gerritz SW. Sheriff S, et al. Among authors: zhu s. J Med Chem. 2011 Oct 13;54(19):6548-62. doi: 10.1021/jm2003766. Epub 2011 Sep 20. J Med Chem. 2011. PMID: 21882820
Inhibition of influenza virus replication via small molecules that induce the formation of higher-order nucleoprotein oligomers.
Gerritz SW, Cianci C, Kim S, Pearce BC, Deminie C, Discotto L, McAuliffe B, Minassian BF, Shi S, Zhu S, Zhai W, Pendri A, Li G, Poss MA, Edavettal S, McDonnell PA, Lewis HA, Maskos K, Mörtl M, Kiefersauer R, Steinbacher S, Baldwin ET, Metzler W, Bryson J, Healy MD, Philip T, Zoeckler M, Schartman R, Sinz M, Leyva-Grado VH, Hoffmann HH, Langley DR, Meanwell NA, Krystal M. Gerritz SW, et al. Among authors: zhu s. Proc Natl Acad Sci U S A. 2011 Sep 13;108(37):15366-71. doi: 10.1073/pnas.1107906108. Epub 2011 Sep 6. Proc Natl Acad Sci U S A. 2011. PMID: 21896751 Free PMC article.
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