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Page 1
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: kruger rg. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
In vitro and in vivo induction of fetal hemoglobin with a reversible and selective DNMT1 inhibitor.
Gilmartin AG, Groy A, Gore ER, Atkins C, Long ER, Montoute MN, Wu Z, Halsey W, McNulty DE, Ennulat D, Rueda L, Pappalardi M, Kruger RG, McCabe MT, Raoof A, Butlin R, Stowell A, Cockerill M, Waddell I, Ogilvie D, Luengo J, Jordan A, Benowitz AB. Gilmartin AG, et al. Among authors: kruger rg. Haematologica. 2021 Jul 1;106(7):1979-1987. doi: 10.3324/haematol.2020.248658. Haematologica. 2021. PMID: 32586904 Free PMC article.
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.
McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL. McCabe MT, et al. Among authors: kruger rg. Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10. Nature. 2012. PMID: 23051747
A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.
Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT. Ott HM, et al. Among authors: kruger rg. Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24. Mol Cancer Ther. 2014. PMID: 25253781
A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.
Mohammad HP, Smitheman KN, Kamat CD, Soong D, Federowicz KE, Van Aller GS, Schneck JL, Carson JD, Liu Y, Butticello M, Bonnette WG, Gorman SA, Degenhardt Y, Bai Y, McCabe MT, Pappalardi MB, Kasparec J, Tian X, McNulty KC, Rouse M, McDevitt P, Ho T, Crouthamel M, Hart TK, Concha NO, McHugh CF, Miller WH, Dhanak D, Tummino PJ, Carpenter CL, Johnson NW, Hann CL, Kruger RG. Mohammad HP, et al. Among authors: kruger rg. Cancer Cell. 2015 Jul 13;28(1):57-69. doi: 10.1016/j.ccell.2015.06.002. Cancer Cell. 2015. PMID: 26175415 Free article.
Antitumor activity of LSD1 inhibitors in lung cancer.
Mohammad HP, Kruger RG. Mohammad HP, et al. Among authors: kruger rg. Mol Cell Oncol. 2016 Jan 6;3(2):e1117700. doi: 10.1080/23723556.2015.1117700. eCollection 2016 Mar. Mol Cell Oncol. 2016. PMID: 27308632 Free PMC article.
Targeting Histone Methylation in Cancer.
McCabe MT, Mohammad HP, Barbash O, Kruger RG. McCabe MT, et al. Among authors: kruger rg. Cancer J. 2017 Sep/Oct;23(5):292-301. doi: 10.1097/PPO.0000000000000283. Cancer J. 2017. PMID: 28926430 Review.
Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-trans retinoic acid in acute myeloid leukemia across subtypes.
Smitheman KN, Severson TM, Rajapurkar SR, McCabe MT, Karpinich N, Foley J, Pappalardi MB, Hughes A, Halsey W, Thomas E, Traini C, Federowicz KE, Laraio J, Mobegi F, Ferron-Brady G, Prinjha RK, Carpenter CL, Kruger RG, Wessels L, Mohammad HP. Smitheman KN, et al. Among authors: kruger rg. Haematologica. 2019 Jun;104(6):1156-1167. doi: 10.3324/haematol.2018.199190. Epub 2018 Dec 4. Haematologica. 2019. PMID: 30514804 Free PMC article.
Inhibiting Type I Arginine Methyltransferase Activity Promotes T Cell-Mediated Antitumor Immune Responses.
Fedoriw A, Shi L, O'Brien S, Smitheman KN, Wang Y, Hou J, Sherk C, Rajapurkar S, Laraio J, Williams LJ, Xu C, Han G, Feng Q, Bedford MT, Wang L, Barbash O, Kruger RG, Hwu P, Mohammad HP, Peng W. Fedoriw A, et al. Among authors: kruger rg. Cancer Immunol Res. 2022 Apr 1;10(4):420-436. doi: 10.1158/2326-6066.CIR-21-0614. Cancer Immunol Res. 2022. PMID: 35181787 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. 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.
56 results