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Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Bradley E, Fusani L, Chung CW, Craggs PD, Demont EH, Humphreys PG, Mitchell DJ, Phillipou A, Rioja I, Shah RR, Wellaway CR, Prinjha RK, Palmer DS, Kerr WJ, Reid M, Wall ID, Cookson R. Bradley E, et al. Among authors: prinjha rk. J Med Chem. 2023 Dec 14;66(23):15728-15749. doi: 10.1021/acs.jmedchem.3c00906. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967462 Free PMC article.
In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer.
Quintela M, James DW, Garcia J, Edwards K, Margarit L, Das N, Lutchman-Singh K, Beynon AL, Rioja I, Prinjha RK, Harker NR, Gonzalez D, Steven Conlan R, Francis LW. Quintela M, et al. Among authors: prinjha rk. Br J Cancer. 2023 Jul;129(1):163-174. doi: 10.1038/s41416-023-02274-2. Epub 2023 Apr 29. Br J Cancer. 2023. PMID: 37120667 Free PMC article.
Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells.
Quintela M, James DW, Pociute A, Powell L, Edwards K, Coombes Z, Garcia J, Garton N, Das N, Lutchman-Singh K, Margarit L, Beynon AL, Rioja I, Prinjha RK, Harker NR, Gonzalez D, Conlan RS, Francis LW. Quintela M, et al. Among authors: prinjha rk. Clin Epigenetics. 2023 Apr 15;15(1):63. doi: 10.1186/s13148-023-01477-x. Clin Epigenetics. 2023. PMID: 37060086 Free PMC article.
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Humphreys PG, Anderson NA, Bamborough P, Baxter A, Chung CW, Cookson R, Craggs PD, Dalton T, Fournier JCL, Gordon LJ, Gray HF, Gray MW, Gregory R, Hirst DJ, Jamieson C, Jones KL, Kessedjian H, Lugo D, McGonagle G, Patel VK, Patten C, Poole DL, Prinjha RK, Ramirez-Molina C, Rioja I, Seal G, Stafford KAJ, Shah RR, Tape D, Theodoulou NH, Tomlinson L, Ukuser S, Wall ID, Wellaway N, White G. Humphreys PG, et al. Among authors: prinjha rk. J Med Chem. 2022 Nov 24;65(22):15174-15207. doi: 10.1021/acs.jmedchem.2c01102. Epub 2022 Nov 15. J Med Chem. 2022. PMID: 36378954
N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells.
Nord JA, Wynia-Smith SL, Gehant AL, Jones Lipinski RA, Naatz A, Rioja I, Prinjha RK, Corbett JA, Smith BC. Nord JA, et al. Among authors: prinjha rk. Front Endocrinol (Lausanne). 2022 Sep 13;13:923925. doi: 10.3389/fendo.2022.923925. eCollection 2022. Front Endocrinol (Lausanne). 2022. PMID: 36176467 Free PMC article.
A BET Protein Inhibitor Targeting Mononuclear Myeloid Cells Affects Specific Inflammatory Mediators and Pathways in Crohn's Disease.
Elfiky AMI, Hageman IL, Becker MAJ, Verhoeff J, Li Yim AYF, Joustra VW, Mulders L, Fung I, Rioja I, Prinjha RK, Smithers NN, Furze RC, Mander PK, Bell MJ, Buskens CJ, D'Haens GR, Wildenberg ME, de Jonge WJ. Elfiky AMI, et al. Among authors: prinjha rk. Cells. 2022 Sep 12;11(18):2846. doi: 10.3390/cells11182846. Cells. 2022. PMID: 36139421 Free PMC article.
139 results