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Page 1
Targeting histone acetylation dynamics and oncogenic transcription by catalytic P300/CBP inhibition.
Hogg SJ, Motorna O, Cluse LA, Johanson TM, Coughlan HD, Raviram R, Myers RM, Costacurta M, Todorovski I, Pijpers L, Bjelosevic S, Williams T, Huskins SN, Kearney CJ, Devlin JR, Fan Z, Jabbari JS, Martin BP, Fareh M, Kelly MJ, Dupéré-Richer D, Sandow JJ, Feran B, Knight D, Khong T, Spencer A, Harrison SJ, Gregory G, Wickramasinghe VO, Webb AI, Taberlay PC, Bromberg KD, Lai A, Papenfuss AT, Smyth GK, Allan RS, Licht JD, Landau DA, Abdel-Wahab O, Shortt J, Vervoort SJ, Johnstone RW. Hogg SJ, et al. Among authors: bromberg kd. Mol Cell. 2021 May 20;81(10):2183-2200.e13. doi: 10.1016/j.molcel.2021.04.015. Mol Cell. 2021. PMID: 34019788 Free PMC article.
Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome.
Weinert BT, Narita T, Satpathy S, Srinivasan B, Hansen BK, Schölz C, Hamilton WB, Zucconi BE, Wang WW, Liu WR, Brickman JM, Kesicki EA, Lai A, Bromberg KD, Cole PA, Choudhary C. Weinert BT, et al. Among authors: bromberg kd. Cell. 2018 Jun 28;174(1):231-244.e12. doi: 10.1016/j.cell.2018.04.033. Epub 2018 May 24. Cell. 2018. PMID: 29804834 Free PMC article.
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor.
Mastracchio A, Lai C, Digiammarino E, Ready DB, Lasko LM, Bromberg KD, McClellan WJ, Montgomery D, Manaves V, Shaw B, Algire M, Patterson MJ, Sun CC, Rosenberg S, Lai A, Michaelides MR. Mastracchio A, et al. Among authors: bromberg kd. ACS Med Chem Lett. 2021 Apr 5;12(5):726-731. doi: 10.1021/acsmedchemlett.0c00654. eCollection 2021 May 13. ACS Med Chem Lett. 2021. PMID: 34055218 Free PMC article.
Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Van Drie JH, McElligott D, Kesicki E, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Lasko LM, et al. Among authors: bromberg kd. Nature. 2017 Oct 5;550(7674):128-132. doi: 10.1038/nature24028. Epub 2017 Sep 27. Nature. 2017. PMID: 28953875 Free PMC article.
Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases.
Ji Z, Clark RF, Bhat V, Matthew Hansen T, Lasko LM, Bromberg KD, Manaves V, Algire M, Martin R, Qiu W, Torrent M, Jakob CG, Liu H, Cole PA, Marmorstein R, Kesicki EA, Lai A, Michaelides MR. Ji Z, et al. Among authors: bromberg kd. Bioorg Med Chem Lett. 2021 May 1;39:127854. doi: 10.1016/j.bmcl.2021.127854. Epub 2021 Feb 23. Bioorg Med Chem Lett. 2021. PMID: 33631370 Free PMC article.
Discovery of Spiro Oxazolidinediones as Selective, Orally Bioavailable Inhibitors of p300/CBP Histone Acetyltransferases.
Michaelides MR, Kluge A, Patane M, Van Drie JH, Wang C, Hansen TM, Risi RM, Mantei R, Hertel C, Karukurichi K, Nesterov A, McElligott D, de Vries P, Langston JW, Cole PA, Marmorstein R, Liu H, Lasko L, Bromberg KD, Lai A, Kesicki EA. Michaelides MR, et al. Among authors: bromberg kd. ACS Med Chem Lett. 2017 Dec 13;9(1):28-33. doi: 10.1021/acsmedchemlett.7b00395. eCollection 2018 Jan 11. ACS Med Chem Lett. 2017. PMID: 29348807 Free PMC article.
Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours.
Lasko LM, Jakob CG, Edalji RP, Qiu W, Montgomery D, Digiammarino EL, Hansen TM, Risi RM, Frey R, Manaves V, Shaw B, Algire M, Hessler P, Lam LT, Uziel T, Faivre E, Ferguson D, Buchanan FG, Martin RL, Torrent M, Chiang GG, Karukurichi K, Langston JW, Weinert BT, Choudhary C, de Vries P, Kluge AF, Patane MA, Van Drie JH, Wang C, McElligott D, Kesicki EA, Marmorstein R, Sun C, Cole PA, Rosenberg SH, Michaelides MR, Lai A, Bromberg KD. Lasko LM, et al. Among authors: bromberg kd. Nature. 2018 Jun;558(7710):E1. doi: 10.1038/s41586-018-0111-5. Nature. 2018. PMID: 29769713
The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity.
Bromberg KD, Mitchell TR, Upadhyay AK, Jakob CG, Jhala MA, Comess KM, Lasko LM, Li C, Tuzon CT, Dai Y, Li F, Eram MS, Nuber A, Soni NB, Manaves V, Algire MA, Sweis RF, Torrent M, Schotta G, Sun C, Michaelides MR, Shoemaker AR, Arrowsmith CH, Brown PJ, Santhakumar V, Martin A, Rice JC, Chiang GG, Vedadi M, Barsyte-Lovejoy D, Pappano WN. Bromberg KD, et al. Nat Chem Biol. 2017 Mar;13(3):317-324. doi: 10.1038/nchembio.2282. Epub 2017 Jan 23. Nat Chem Biol. 2017. PMID: 28114273
Investigation of biaryl heterocycles as inhibitors of Wee1 kinase.
Mastracchio A, Lai C, Torrent M, Bromberg K, Buchanan FG, Ferguson D, Bontcheva V, Johnson EF, Lasko L, Maag D, Shoemaker AR, Penning TD. Mastracchio A, et al. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1481-1486. doi: 10.1016/j.bmcl.2019.04.017. Epub 2019 Apr 9. Bioorg Med Chem Lett. 2019. PMID: 31014911
24 results