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Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors.
Lucas SCC, Atkinson SJ, Chung CW, Davis R, Gordon L, Grandi P, Gray JJR, Grimes T, Phillipou A, Preston AG, Prinjha RK, Rioja I, Taylor S, Tomkinson NCO, Wall I, Watson RJ, Woolven J, Demont EH. Lucas SCC, et al. Among authors: rioja i. J Med Chem. 2021 Aug 12;64(15):10711-10741. doi: 10.1021/acs.jmedchem.1c00344. Epub 2021 Jul 14. J Med Chem. 2021. PMID: 34260229 Free article.
BET Inhibition Improves NASH and Liver Fibrosis.
Middleton SA, Rajpal N, Cutler L, Mander P, Rioja I, Prinjha RK, Rajpal D, Agarwal P, Kumar V. Middleton SA, et al. Among authors: rioja i. Sci Rep. 2018 Nov 22;8(1):17257. doi: 10.1038/s41598-018-35653-4. Sci Rep. 2018. PMID: 30467325 Free PMC article.
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Among authors: rioja i. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
Clegg MA, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Leveridge M, Lindon M, Liwicki GM, Michon AM, Molnar J, Rioja I, Soden PE, Theodoulou NH, Werner T, Tomkinson NCO, Prinjha RK, Humphreys PG. Clegg MA, et al. Among authors: rioja i. J Med Chem. 2020 Jun 11;63(11):5816-5840. doi: 10.1021/acs.jmedchem.0c00075. Epub 2020 May 29. J Med Chem. 2020. PMID: 32410449 Free article.
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.
Preston A, Atkinson S, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Gray JRJ, Jones EJ, Lindon M, Michon AM, Mitchell DJ, Prinjha RK, Rianjongdee F, Rioja I, Seal J, Taylor S, Wall I, Watson RJ, Woolven J, Demont EH. Preston A, et al. Among authors: rioja i. J Med Chem. 2020 Sep 10;63(17):9070-9092. doi: 10.1021/acs.jmedchem.0c00605. Epub 2020 Aug 20. J Med Chem. 2020. PMID: 32691591
56 results