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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: lai a. 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 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: lai a. 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: lai a. Nature. 2018 Jun;558(7710):E1. doi: 10.1038/s41586-018-0111-5. Nature. 2018. PMID: 29769713
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: lai a. 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 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: lai a. 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.
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: lai a. 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.
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: lai c, lai a. 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.
The HPK1 Inhibitor A-745 Verifies the Potential of Modulating T Cell Kinase Signaling for Immunotherapy.
Malchow S, Korepanova A, Panchal SC, McClure RA, Longenecker KL, Qiu W, Zhao H, Cheng M, Guo J, Klinge KL, Trusk P, Pratt SD, Li T, Kurnick MD, Duan L, Shoemaker AR, Gopalakrishnan SM, Warder SE, Shotwell JB, Lai A, Sun C, Osuma AT, Pappano WN. Malchow S, et al. Among authors: lai a. ACS Chem Biol. 2022 Mar 18;17(3):556-566. doi: 10.1021/acschembio.1c00819. Epub 2022 Feb 21. ACS Chem Biol. 2022. PMID: 35188729
1,940 results