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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: cockerill m. 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: cockerill m. Haematologica. 2021 Jul 1;106(7):1979-1987. doi: 10.3324/haematol.2020.248658. Haematologica. 2021. PMID: 32586904 Free PMC article.
Discovery and Optimization of Allosteric Inhibitors of Mutant Isocitrate Dehydrogenase 1 (R132H IDH1) Displaying Activity in Human Acute Myeloid Leukemia Cells.
Jones S, Ahmet J, Ayton K, Ball M, Cockerill M, Fairweather E, Hamilton N, Harper P, Hitchin J, Jordan A, Levy C, Lopez R, McKenzie E, Packer M, Plant D, Simpson I, Simpson P, Sinclair I, Somervaille TC, Small H, Spencer GJ, Thomson G, Tonge M, Waddell I, Walsh J, Waszkowycz B, Wigglesworth M, Wiseman DH, Ogilvie D. Jones S, et al. Among authors: cockerill m. J Med Chem. 2016 Dec 22;59(24):11120-11137. doi: 10.1021/acs.jmedchem.6b01320. Epub 2016 Dec 5. J Med Chem. 2016. PMID: 28002956
Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244).
Dry JR, Pavey S, Pratilas CA, Harbron C, Runswick S, Hodgson D, Chresta C, McCormack R, Byrne N, Cockerill M, Graham A, Beran G, Cassidy A, Haggerty C, Brown H, Ellison G, Dering J, Taylor BS, Stark M, Bonazzi V, Ravishankar S, Packer L, Xing F, Solit DB, Finn RS, Rosen N, Hayward NK, French T, Smith PD. Dry JR, et al. Among authors: cockerill m. Cancer Res. 2010 Mar 15;70(6):2264-73. doi: 10.1158/0008-5472.CAN-09-1577. Epub 2010 Mar 9. Cancer Res. 2010. PMID: 20215513 Free PMC article.
AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models.
Davies BR, Logie A, McKay JS, Martin P, Steele S, Jenkins R, Cockerill M, Cartlidge S, Smith PD. Davies BR, et al. Among authors: cockerill m. Mol Cancer Ther. 2007 Aug;6(8):2209-19. doi: 10.1158/1535-7163.MCT-07-0231. Mol Cancer Ther. 2007. PMID: 17699718
Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis.
Kettle JG, Ballard P, Bardelle C, Cockerill M, Colclough N, Critchlow SE, Debreczeni J, Fairley G, Fillery S, Graham MA, Goodwin L, Guichard S, Hudson K, Ward RA, Whittaker D. Kettle JG, et al. Among authors: cockerill m. J Med Chem. 2015 Mar 26;58(6):2834-44. doi: 10.1021/acs.jmedchem.5b00098. Epub 2015 Mar 12. J Med Chem. 2015. PMID: 25738750
Factors determining the optimal body site and method for obtaining punch biopsies of human skin as a tissue in which to assess pharmacodynamic and pharmacokinetic endpoints in drug development studies.
Camidge DR, Davies MJ, Laud PJ, Marshall AL, Cockerill M, Smith PD, Hughes AM. Camidge DR, et al. Among authors: cockerill m. Cancer Chemother Pharmacol. 2006 Jan;57(1):52-8. doi: 10.1007/s00280-005-0024-5. Epub 2005 Nov 5. Cancer Chemother Pharmacol. 2006. PMID: 16032432
Identification of DYRK1B as a substrate of ERK1/2 and characterisation of the kinase activity of DYRK1B mutants from cancer and metabolic syndrome.
Ashford AL, Dunkley TP, Cockerill M, Rowlinson RA, Baak LM, Gallo R, Balmanno K, Goodwin LM, Ward RA, Lochhead PA, Guichard S, Hudson K, Cook SJ. Ashford AL, et al. Among authors: cockerill m. Cell Mol Life Sci. 2016 Feb;73(4):883-900. doi: 10.1007/s00018-015-2032-x. Epub 2015 Sep 7. Cell Mol Life Sci. 2016. PMID: 26346493 Free PMC article.
Working on the assembly line.
Gibbs RA, Cockerill M. Gibbs RA, et al. Among authors: cockerill m. Trends Biochem Sci. 1995 Apr;20(4):162-3. doi: 10.1016/s0968-0004(00)88995-1. Trends Biochem Sci. 1995. PMID: 7770918 No abstract available.
36 results