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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
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: rioja i. 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.
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.
Targeting Histone Deacetylases in Myeloid Cells Inhibits Their Maturation and Inflammatory Function With Limited Effects on Atherosclerosis.
Luque-Martin R, Van den Bossche J, Furze RC, Neele AE, van der Velden S, Gijbels MJJ, van Roomen CPPA, Bernard SG, de Jonge WJ, Rioja I, Prinjha RK, Lewis HD, Mander PK, de Winther MPJ. Luque-Martin R, et al. Among authors: rioja i. Front Pharmacol. 2019 Oct 29;10:1242. doi: 10.3389/fphar.2019.01242. eCollection 2019. Front Pharmacol. 2019. PMID: 31736752 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.
56 results