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Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.
Lauffer BE, Mintzer R, Fong R, Mukund S, Tam C, Zilberleyb I, Flicke B, Ritscher A, Fedorowicz G, Vallero R, Ortwine DF, Gunzner J, Modrusan Z, Neumann L, Koth CM, Lupardus PJ, Kaminker JS, Heise CE, Steiner P. Lauffer BE, et al. Among authors: lupardus pj. J Biol Chem. 2013 Sep 13;288(37):26926-43. doi: 10.1074/jbc.M113.490706. Epub 2013 Jul 29. J Biol Chem. 2013. PMID: 23897821 Free PMC article.
RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases.
Patel S, Webster JD, Varfolomeev E, Kwon YC, Cheng JH, Zhang J, Dugger DL, Wickliffe KE, Maltzman A, Sujatha-Bhaskar S, Bir Kohli P, Ramaswamy S, Deshmukh G, Liederer BM, Fong R, Hamilton G, Lupardus P, Caplazi P, Lee WP, van Lookeren Campagne M, Johnson A, McKenzie BS, Junttila MR, Newton K, Vucic D. Patel S, et al. Cell Death Differ. 2020 Jan;27(1):161-175. doi: 10.1038/s41418-019-0347-0. Epub 2019 May 17. Cell Death Differ. 2020. PMID: 31101885 Free PMC article.
Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.
Hamilton GL, Chen H, Deshmukh G, Eigenbrot C, Fong R, Johnson A, Kohli PB, Lupardus PJ, Liederer BM, Ramaswamy S, Wang H, Wang J, Xu Z, Zhu Y, Vucic D, Patel S. Hamilton GL, et al. Among authors: lupardus pj. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1497-1501. doi: 10.1016/j.bmcl.2019.04.014. Epub 2019 Apr 11. Bioorg Med Chem Lett. 2019. PMID: 31000154
Novel triazolo-pyrrolopyridines as inhibitors of Janus kinase 1.
Hurley CA, Blair WS, Bull RJ, Chang C, Crackett PH, Deshmukh G, Dyke HJ, Fong R, Ghilardi N, Gibbons P, Hewitt PR, Johnson A, Johnson T, Kenny JR, Kohli PB, Kulagowski JJ, Liimatta M, Lupardus PJ, Maxey RJ, Mendonca R, Narukulla R, Pulk R, Ubhayakar S, van Abbema A, Ward SI, Waszkowycz B, Zak M. Hurley CA, et al. Among authors: lupardus pj. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3592-8. doi: 10.1016/j.bmcl.2013.04.018. Epub 2013 Apr 17. Bioorg Med Chem Lett. 2013. PMID: 23642482
59 results