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Page 1
Click chemistry enables preclinical evaluation of targeted epigenetic therapies.
Tyler DS, Vappiani J, Cañeque T, Lam EYN, Ward A, Gilan O, Chan YC, Hienzsch A, Rutkowska A, Werner T, Wagner AJ, Lugo D, Gregory R, Ramirez Molina C, Garton N, Wellaway CR, Jackson S, MacPherson L, Figueiredo M, Stolzenburg S, Bell CC, House C, Dawson SJ, Hawkins ED, Drewes G, Prinjha RK, Rodriguez R, Grandi P, Dawson MA. Tyler DS, et al. Among authors: garton n. Science. 2017 Jun 30;356(6345):1397-1401. doi: 10.1126/science.aal2066. Epub 2017 Jun 15. Science. 2017. PMID: 28619718 Free PMC article.
Autism-like syndrome is induced by pharmacological suppression of BET proteins in young mice.
Sullivan JM, Badimon A, Schaefer U, Ayata P, Gray J, Chung CW, von Schimmelmann M, Zhang F, Garton N, Smithers N, Lewis H, Tarakhovsky A, Prinjha RK, Schaefer A. Sullivan JM, et al. Among authors: garton n. J Exp Med. 2015 Oct 19;212(11):1771-81. doi: 10.1084/jem.20151271. Epub 2015 Sep 21. J Exp Med. 2015. PMID: 26392221 Free PMC article.
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Drewes G, Eagle R, Garton N, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Pemberton M, Rioja I, Seal GA, Shipley T, Singh O, Suckling CJ, Taylor J, Thomas P, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: garton n. J Med Chem. 2016 Feb 25;59(4):1370-87. doi: 10.1021/acs.jmedchem.5b01538. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771203
Interrogating the Druggability of the 2-Oxoglutarate-Dependent Dioxygenase Target Class by Chemical Proteomics.
Joberty G, Boesche M, Brown JA, Eberhard D, Garton NS, Humphreys PG, Mathieson T, Muelbaier M, Ramsden NG, Reader V, Rueger A, Sheppard RJ, Westaway SM, Bantscheff M, Lee K, Wilson DM, Prinjha RK, Drewes G. Joberty G, et al. ACS Chem Biol. 2016 Jul 15;11(7):2002-10. doi: 10.1021/acschembio.6b00080. Epub 2016 May 19. ACS Chem Biol. 2016. PMID: 27197014
Functional interdependence of BRD4 and DOT1L in MLL leukemia.
Gilan O, Lam EY, Becher I, Lugo D, Cannizzaro E, Joberty G, Ward A, Wiese M, Fong CY, Ftouni S, Tyler D, Stanley K, MacPherson L, Weng CF, Chan YC, Ghisi M, Smil D, Carpenter C, Brown P, Garton N, Blewitt ME, Bannister AJ, Kouzarides T, Huntly BJ, Johnstone RW, Drewes G, Dawson SJ, Arrowsmith CH, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Among authors: garton n. Nat Struct Mol Biol. 2016 Jul;23(7):673-81. doi: 10.1038/nsmb.3249. Epub 2016 Jun 13. Nat Struct Mol Biol. 2016. PMID: 27294782
Optimisation of a novel series of potent and orally bioavailable azanaphthyridine SYK inhibitors.
Garton NS, Barker MD, Davis RP, Douault C, Hooper-Greenhill E, Jones E, Lewis HD, Liddle J, Lugo D, McCleary S, Preston AGS, Ramirez-Molina C, Neu M, Shipley TJ, Somers DO, Watson RJ, Wilson DM. Garton NS, et al. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4606-4612. doi: 10.1016/j.bmcl.2016.08.070. Epub 2016 Aug 23. Bioorg Med Chem Lett. 2016. PMID: 27578246
Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells.
Quintela M, James DW, Pociute A, Powell L, Edwards K, Coombes Z, Garcia J, Garton N, Das N, Lutchman-Singh K, Margarit L, Beynon AL, Rioja I, Prinjha RK, Harker NR, Gonzalez D, Conlan RS, Francis LW. Quintela M, et al. Among authors: garton n. Clin Epigenetics. 2023 Apr 15;15(1):63. doi: 10.1186/s13148-023-01477-x. Clin Epigenetics. 2023. PMID: 37060086 Free PMC article.
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor.
Liddle J, Atkinson FL, Barker MD, Carter PS, Curtis NR, Davis RP, Douault C, Dickson MC, Elwes D, Garton NS, Gray M, Hayhow TG, Hobbs CI, Jones E, Leach S, Leavens K, Lewis HD, McCleary S, Neu M, Patel VK, Preston AG, Ramirez-Molina C, Shipley TJ, Skone PA, Smithers N, Somers DO, Walker AL, Watson RJ, Weingarten GG. Liddle J, et al. Among authors: garton ns. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6188-94. doi: 10.1016/j.bmcl.2011.07.082. Epub 2011 Aug 12. Bioorg Med Chem Lett. 2011. PMID: 21903390
Orally active C-6 heteroaryl- and heterocyclyl-substituted imidazo[1,2-a]pyridine acid pump antagonists (APAs).
Bailey N, Bamford MJ, Brissy D, Brookfield J, Demont E, Elliott R, Garton N, Farre-Gutierrez I, Hayhow T, Hutley G, Naylor A, Panchal TA, Seow HX, Spalding D, Takle AK. Bailey N, et al. Among authors: garton n. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3602-6. doi: 10.1016/j.bmcl.2009.04.127. Epub 2009 May 3. Bioorg Med Chem Lett. 2009. PMID: 19467868
43 results