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Page 1
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: prinjha r. 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.
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Chung CW, Coste H, White JH, Mirguet O, Wilde J, Gosmini RL, Delves C, Magny SM, Woodward R, Hughes SA, Boursier EV, Flynn H, Bouillot AM, Bamborough P, Brusq JM, Gellibert FJ, Jones EJ, Riou AM, Homes P, Martin SL, Uings IJ, Toum J, Clement CA, Boullay AB, Grimley RL, Blandel FM, Prinjha RK, Lee K, Kirilovsky J, Nicodeme E. Chung CW, et al. Among authors: prinjha rk. J Med Chem. 2011 Jun 9;54(11):3827-38. doi: 10.1021/jm200108t. Epub 2011 May 13. J Med Chem. 2011. PMID: 21568322
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: prinjha rk. Nature. 2011 Oct 2;478(7370):529-33. doi: 10.1038/nature10509. Nature. 2011. PMID: 21964340 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. 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
BET protein inhibition shows efficacy against JAK2V617F-driven neoplasms.
Wyspiańska BS, Bannister AJ, Barbieri I, Nangalia J, Godfrey A, Calero-Nieto FJ, Robson S, Rioja I, Li J, Wiese M, Cannizzaro E, Dawson MA, Huntly B, Prinjha RK, Green AR, Gottgens B, Kouzarides T. Wyspiańska BS, et al. Among authors: prinjha rk. Leukemia. 2014 Jan;28(1):88-97. doi: 10.1038/leu.2013.234. Epub 2013 Aug 9. Leukemia. 2014. PMID: 23929215
BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.
Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ. Wyce A, et al. Among authors: prinjha rk. PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013. PLoS One. 2013. PMID: 24009722 Free PMC article.
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: prinjha rk. Leukemia. 2014 Feb;28(2):311-20. doi: 10.1038/leu.2013.338. Epub 2013 Nov 13. Leukemia. 2014. PMID: 24220271 Free PMC article.
BRD4 short isoform interacts with RRP1B, SIPA1 and components of the LINC complex at the inner face of the nuclear membrane.
Alsarraj J, Faraji F, Geiger TR, Mattaini KR, Williams M, Wu J, Ha NH, Merlino T, Walker RC, Bosley AD, Xiao Z, Andresson T, Esposito D, Smithers N, Lugo D, Prinjha R, Day A, Crawford NP, Ozato K, Gardner K, Hunter KW. Alsarraj J, et al. Among authors: prinjha r. PLoS One. 2013 Nov 19;8(11):e80746. doi: 10.1371/journal.pone.0080746. eCollection 2013. PLoS One. 2013. PMID: 24260471 Free PMC article.
159 results