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Page 1
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: gilmartin ag. 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
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. Haematologica. 2021 Jul 1;106(7):1979-1987. doi: 10.3324/haematol.2020.248658. Haematologica. 2021. PMID: 32586904 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: gilmartin ag. Nat Cancer. 2021 Oct;2(10):1002-1017. Epub 2021 Sep 27. Nat Cancer. 2021. PMID: 34790902 Free PMC article.
Discovery of a Highly Potent and Selective MEK Inhibitor: GSK1120212 (JTP-74057 DMSO Solvate).
Abe H, Kikuchi S, Hayakawa K, Iida T, Nagahashi N, Maeda K, Sakamoto J, Matsumoto N, Miura T, Matsumura K, Seki N, Inaba T, Kawasaki H, Yamaguchi T, Kakefuda R, Nanayama T, Kurachi H, Hori Y, Yoshida T, Kakegawa J, Watanabe Y, Gilmartin AG, Richter MC, Moss KG, Laquerre SG. Abe H, et al. Among authors: gilmartin ag. ACS Med Chem Lett. 2011 Feb 28;2(4):320-4. doi: 10.1021/ml200004g. eCollection 2011 Apr 14. ACS Med Chem Lett. 2011. PMID: 24900312 Free PMC article.
GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition.
Gilmartin AG, Bleam MR, Groy A, Moss KG, Minthorn EA, Kulkarni SG, Rominger CM, Erskine S, Fisher KE, Yang J, Zappacosta F, Annan R, Sutton D, Laquerre SG. Gilmartin AG, et al. Clin Cancer Res. 2011 Mar 1;17(5):989-1000. doi: 10.1158/1078-0432.CCR-10-2200. Epub 2011 Jan 18. Clin Cancer Res. 2011. PMID: 21245089
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction.
Gilmartin AG, Faitg TH, Richter M, Groy A, Seefeld MA, Darcy MG, Peng X, Federowicz K, Yang J, Zhang SY, Minthorn E, Jaworski JP, Schaber M, Martens S, McNulty DE, Sinnamon RH, Zhang H, Kirkpatrick RB, Nevins N, Cui G, Pietrak B, Diaz E, Jones A, Brandt M, Schwartz B, Heerding DA, Kumar R. Gilmartin AG, et al. Nat Chem Biol. 2014 Mar;10(3):181-7. doi: 10.1038/nchembio.1427. Epub 2014 Jan 5. Nat Chem Biol. 2014. PMID: 24390428
Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability.
Degenhardt Y, Greshock J, Laquerre S, Gilmartin AG, Jing J, Richter M, Zhang X, Bleam M, Halsey W, Hughes A, Moy C, Liu-Sullivan N, Powers S, Bachman K, Jackson J, Weber B, Wooster R. Degenhardt Y, et al. Among authors: gilmartin ag. Mol Cancer Ther. 2010 Jul;9(7):2079-89. doi: 10.1158/1535-7163.MCT-10-0095. Epub 2010 Jun 22. Mol Cancer Ther. 2010. PMID: 20571075
WIP1 phosphatase as a potential therapeutic target in neuroblastoma.
Richter M, Dayaram T, Gilmartin AG, Ganji G, Pemmasani SK, Van Der Key H, Shohet JM, Donehower LA, Kumar R. Richter M, et al. Among authors: gilmartin ag. PLoS One. 2015 Feb 6;10(2):e0115635. doi: 10.1371/journal.pone.0115635. eCollection 2015. PLoS One. 2015. PMID: 25658463 Free PMC article.
17 results