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Recurrent mutations, including NPM1c, activate a BRD4-dependent core transcriptional program in acute myeloid leukemia.
Dawson MA, Gudgin EJ, Horton SJ, Giotopoulos G, Meduri E, Robson S, Cannizzaro E, Osaki H, Wiese M, Putwain S, Fong CY, Grove C, Craig J, Dittmann A, Lugo D, Jeffrey P, Drewes G, Lee K, Bullinger L, Prinjha RK, Kouzarides T, Vassiliou GS, Huntly BJ. Dawson MA, et al. Among authors: lee k. Leukemia. 2014 Feb;28(2):311-20. doi: 10.1038/leu.2013.338. Epub 2013 Nov 13. Leukemia. 2014. PMID: 24220271 Free PMC article.
Place your BETs: the therapeutic potential of bromodomains.
Prinjha RK, Witherington J, Lee K. Prinjha RK, et al. Among authors: lee k. Trends Pharmacol Sci. 2012 Mar;33(3):146-53. doi: 10.1016/j.tips.2011.12.002. Epub 2012 Jan 23. Trends Pharmacol Sci. 2012. PMID: 22277300 Review.
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
Dawson MA, Prinjha RK, Dittmann A, Giotopoulos G, Bantscheff M, Chan WI, Robson SC, Chung CW, Hopf C, Savitski MM, Huthmacher C, Gudgin E, Lugo D, Beinke S, Chapman TD, Roberts EJ, Soden PE, Auger KR, Mirguet O, Doehner K, Delwel R, Burnett AK, Jeffrey P, Drewes G, Lee K, Huntly BJ, Kouzarides T. Dawson MA, et al. Among authors: lee k. Nature. 2011 Oct 2;478(7370):529-33. doi: 10.1038/nature10509. Nature. 2011. PMID: 21964340 Free PMC article.
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy.
Picaud S, Fedorov O, Thanasopoulou A, Leonards K, Jones K, Meier J, Olzscha H, Monteiro O, Martin S, Philpott M, Tumber A, Filippakopoulos P, Yapp C, Wells C, Che KH, Bannister A, Robson S, Kumar U, Parr N, Lee K, Lugo D, Jeffrey P, Taylor S, Vecellio ML, Bountra C, Brennan PE, O'Mahony A, Velichko S, Müller S, Hay D, Daniels DL, Urh M, La Thangue NB, Kouzarides T, Prinjha R, Schwaller J, Knapp S. Picaud S, et al. Among authors: lee k. Cancer Res. 2015 Dec 1;75(23):5106-5119. doi: 10.1158/0008-5472.CAN-15-0236. Epub 2015 Nov 9. Cancer Res. 2015. PMID: 26552700 Free PMC article.
BET bromodomain inhibitors show anti-papillomavirus activity in vitro and block CRPV wart growth in vivo.
Morse MA, Balogh KK, Brendle SA, Campbell CA, Chen MX, Furze RC, Harada IL, Holyer ID, Kumar U, Lee K, Prinjha RK, Rüdiger M, Seal JT, Taylor S, Witherington J, Christensen ND. Morse MA, et al. Among authors: lee k. Antiviral Res. 2018 Jun;154:158-165. doi: 10.1016/j.antiviral.2018.03.012. Epub 2018 Apr 11. Antiviral Res. 2018. PMID: 29653131 Free PMC article.
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK. Seal J, et al. Among authors: lee k. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24. Bioorg Med Chem Lett. 2012. PMID: 22437115
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. Among authors: lee k. 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
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 1. 3-Amino-4-pyridine Carboxylate Derivatives.
Westaway SM, Preston AG, Barker MD, Brown F, Brown JA, Campbell M, Chung CW, Diallo H, Douault C, Drewes G, Eagle R, Gordon L, Haslam C, Hayhow TG, Humphreys PG, Joberty G, Katso R, Kruidenier L, Leveridge M, Liddle J, Mosley J, Muelbaier M, Randle R, Rioja I, Rueger A, Seal GA, Sheppard RJ, Singh O, Taylor J, Thomas P, Thomson D, Wilson DM, Lee K, Prinjha RK. Westaway SM, et al. Among authors: lee k. J Med Chem. 2016 Feb 25;59(4):1357-69. doi: 10.1021/acs.jmedchem.5b01537. Epub 2016 Jan 15. J Med Chem. 2016. PMID: 26771107
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