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Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia.
Pappalardi MB, Keenan K, Cockerill M, Kellner WA, Stowell A, Sherk C, Wong K, Pathuri S, Briand J, Steidel M, Chapman P, Groy A, Wiseman AK, McHugh CF, Campobasso N, Graves AP, Fairweather E, Werner T, Raoof A, Butlin RJ, Rueda L, Horton JR, Fosbenner DT, Zhang C, Handler JL, Muliaditan M, Mebrahtu M, Jaworski JP, McNulty DE, Burt C, Eberl HC, Taylor AN, Ho T, Merrihew S, Foley SW, Rutkowska A, Li M, Romeril SP, Goldberg K, Zhang X, Kershaw CS, Bantscheff M, Jurewicz AJ, Minthorn E, Grandi P, Patel M, Benowitz AB, Mohammad HP, Gilmartin AG, Prinjha RK, Ogilvie D, Carpenter C, Heerding D, Baylin SB, Jones PA, Cheng X, King BW, Luengo JI, Jordan AM, Waddell I, Kruger RG, McCabe MT. Pappalardi MB, et al. Among authors: eberl hc. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Design of amidobenzimidazole STING receptor agonists with systemic activity.
Ramanjulu JM, Pesiridis GS, Yang J, Concha N, Singhaus R, Zhang SY, Tran JL, Moore P, Lehmann S, Eberl HC, Muelbaier M, Schneck JL, Clemens J, Adam M, Mehlmann J, Romano J, Morales A, Kang J, Leister L, Graybill TL, Charnley AK, Ye G, Nevins N, Behnia K, Wolf AI, Kasparcova V, Nurse K, Wang L, Puhl AC, Li Y, Klein M, Hopson CB, Guss J, Bantscheff M, Bergamini G, Reilly MA, Lian Y, Duffy KJ, Adams J, Foley KP, Gough PJ, Marquis RW, Smothers J, Hoos A, Bertin J. Ramanjulu JM, et al. Among authors: eberl hc. Nature. 2018 Dec;564(7736):439-443. doi: 10.1038/s41586-018-0705-y. Epub 2018 Nov 7. Nature. 2018. PMID: 30405246
A hit deconstruction approach for the discovery of fetal hemoglobin inducers.
Benowitz AB, Eberl HC, Erickson-Miller CL, Gilmartin AG, Gore ER, Montoute MN, Wu Z. Benowitz AB, et al. Among authors: eberl hc. Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3676-3680. doi: 10.1016/j.bmcl.2018.10.032. Epub 2018 Oct 22. Bioorg Med Chem Lett. 2018. PMID: 30554630
Identifying drug targets in tissues and whole blood with thermal-shift profiling.
Perrin J, Werner T, Kurzawa N, Rutkowska A, Childs DD, Kalxdorf M, Poeckel D, Stonehouse E, Strohmer K, Heller B, Thomson DW, Krause J, Becher I, Eberl HC, Vappiani J, Sevin DC, Rau CE, Franken H, Huber W, Faelth-Savitski M, Savitski MM, Bantscheff M, Bergamini G. Perrin J, et al. Among authors: eberl hc. Nat Biotechnol. 2020 Mar;38(3):303-308. doi: 10.1038/s41587-019-0388-4. Epub 2020 Jan 20. Nat Biotechnol. 2020. PMID: 31959954
29 results