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Page 1
BRD4 methylation by the methyltransferase SETD6 regulates selective transcription to control mRNA translation.
Vershinin Z, Feldman M, Werner T, Weil LE, Kublanovsky M, Abaev-Schneiderman E, Sklarz M, Lam EYN, Alasad K, Picaud S, Rotblat B, McAdam RA, Chalifa-Caspi V, Bantscheff M, Chapman T, Lewis HD, Filippakopoulos P, Dawson MA, Grandi P, Prinjha RK, Levy D. Vershinin Z, et al. Among authors: prinjha rk. Sci Adv. 2021 May 26;7(22):eabf5374. doi: 10.1126/sciadv.abf5374. Print 2021 May. Sci Adv. 2021. PMID: 34039605 Free PMC article.
Lysine methylation of the NF-κB subunit RelA by SETD6 couples activity of the histone methyltransferase GLP at chromatin to tonic repression of NF-κB signaling.
Levy D, Kuo AJ, Chang Y, Schaefer U, Kitson C, Cheung P, Espejo A, Zee BM, Liu CL, Tangsombatvisit S, Tennen RI, Kuo AY, Tanjing S, Cheung R, Chua KF, Utz PJ, Shi X, Prinjha RK, Lee K, Garcia BA, Bedford MT, Tarakhovsky A, Cheng X, Gozani O. Levy D, et al. Among authors: prinjha rk. Nat Immunol. 2011 Jan;12(1):29-36. doi: 10.1038/ni.1968. Epub 2010 Dec 5. Nat Immunol. 2011. PMID: 21131967 Free PMC article.
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.
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.
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Chen P, et al. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. J Med Chem. 2016. PMID: 25799074 Free PMC article.
Brd4 bridges the transcriptional regulators, Aire and P-TEFb, to promote elongation of peripheral-tissue antigen transcripts in thymic stromal cells.
Yoshida H, Bansal K, Schaefer U, Chapman T, Rioja I, Proekt I, Anderson MS, Prinjha RK, Tarakhovsky A, Benoist C, Mathis D. Yoshida H, et al. Among authors: prinjha rk. Proc Natl Acad Sci U S A. 2015 Aug 11;112(32):E4448-57. doi: 10.1073/pnas.1512081112. Epub 2015 Jul 27. Proc Natl Acad Sci U S A. 2015. PMID: 26216992 Free PMC article.
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH. Bamborough P, et al. Among authors: prinjha rk. J Med Chem. 2015 Aug 13;58(15):6151-78. doi: 10.1021/acs.jmedchem.5b00773. Epub 2015 Jul 31. J Med Chem. 2015. PMID: 26230603
BET inhibitor resistance emerges from leukaemia stem cells.
Fong CY, Gilan O, Lam EY, Rubin AF, Ftouni S, Tyler D, Stanley K, Sinha D, Yeh P, Morison J, Giotopoulos G, Lugo D, Jeffrey P, Lee SC, Carpenter C, Gregory R, Ramsay RG, Lane SW, Abdel-Wahab O, Kouzarides T, Johnstone RW, Dawson SJ, Huntly BJ, Prinjha RK, Papenfuss AT, Dawson MA. Fong CY, et al. Among authors: prinjha rk. Nature. 2015 Sep 24;525(7570):538-42. doi: 10.1038/nature14888. Epub 2015 Sep 14. Nature. 2015. PMID: 26367796 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. 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.
153 results