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27 results

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Page 1
Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor.
Thomson DW, Poeckel D, Zinn N, Rau C, Strohmer K, Wagner AJ, Graves AP, Perrin J, Bantscheff M, Duempelfeld B, Kasparcova V, Ramanjulu JM, Pesiridis GS, Muelbaier M, Bergamini G. Thomson DW, et al. Among authors: graves ap. ACS Med Chem Lett. 2019 Mar 11;10(5):780-785. doi: 10.1021/acsmedchemlett.9b00027. eCollection 2019 May 9. ACS Med Chem Lett. 2019. PMID: 31097999 Free PMC article.
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Verma SK, Tian X, LaFrance LV, Duquenne C, Suarez DP, Newlander KA, Romeril SP, Burgess JL, Grant SW, Brackley JA, Graves AP, Scherzer DA, Shu A, Thompson C, Ott HM, Aller GS, Machutta CA, Diaz E, Jiang Y, Johnson NW, Knight SD, Kruger RG, McCabe MT, Dhanak D, Tummino PJ, Creasy CL, Miller WH. Verma SK, et al. Among authors: graves ap. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13. ACS Med Chem Lett. 2012. PMID: 24900432 Free PMC article.
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors.
Su DS, Qu J, Schulz M, Blackledge CW, Yu H, Zeng J, Burgess J, Reif A, Stern M, Nagarajan R, Pappalardi MB, Wong K, Graves AP, Bonnette W, Wang L, Elkins P, Knapp-Reed B, Carson JD, McHugh C, Mohammad H, Kruger R, Luengo J, Heerding DA, Creasy CL. Su DS, et al. Among authors: graves ap. ACS Med Chem Lett. 2019 Dec 27;11(2):133-140. doi: 10.1021/acsmedchemlett.9b00493. eCollection 2020 Feb 13. ACS Med Chem Lett. 2019. PMID: 32071679 Free PMC article.
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: graves ap. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening.
Tian X, Suarez D, Thomson D, Li W, King EA, LaFrance L, Boehm J, Barton L, Di Marco C, Martyr C, Thalji R, Medina J, Knight S, Heerding D, Gao E, Nartey E, Cecconie T, Nixon C, Zhang G, Berrodin TJ, Phelps C, Patel A, Bai X, Lind K, Prabhu N, Messer J, Zhu Z, Shewchuk L, Reid R, Graves AP, McHugh C, Mangatt B. Tian X, et al. Among authors: graves ap. J Med Chem. 2022 Nov 10;65(21):14391-14408. doi: 10.1021/acs.jmedchem.2c00670. Epub 2022 Oct 27. J Med Chem. 2022. PMID: 36302181
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K).
Lawhorn BG, Philp J, Zhao Y, Louer C, Hammond M, Cheung M, Fries H, Graves AP, Shewchuk L, Wang L, Cottom JE, Qi H, Zhao H, Totoritis R, Zhang G, Schwartz B, Li H, Sweitzer S, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: graves ap. J Med Chem. 2015 Sep 24;58(18):7431-48. doi: 10.1021/acs.jmedchem.5b00931. Epub 2015 Sep 10. J Med Chem. 2015. PMID: 26355916
GSK114: A selective inhibitor for elucidating the biological role of TNNI3K.
Lawhorn BG, Philp J, Graves AP, Shewchuk L, Holt DA, Gatto GJ Jr, Kallander LS. Lawhorn BG, et al. Among authors: graves ap. Bioorg Med Chem Lett. 2016 Jul 15;26(14):3355-3358. doi: 10.1016/j.bmcl.2016.05.033. Epub 2016 May 14. Bioorg Med Chem Lett. 2016. PMID: 27246618
27 results