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Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J, Gordon L, Grandi P, Gray JRJ, Harrison LA, Kruger RG, Matteo JJ, McCabe MT, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A, Zhang XP, Demont EH. Seal JT, et al. Among authors: rioja i. J Med Chem. 2021 Aug 12;64(15):10772-10805. doi: 10.1021/acs.jmedchem.1c00365. Epub 2021 Jul 13. J Med Chem. 2021. PMID: 34255512
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.
Signaling function of PRC2 is essential for TCR-driven T cell responses.
Dobenecker MW, Park JS, Marcello J, McCabe MT, Gregory R, Knight SD, Rioja I, Bassil AK, Prinjha RK, Tarakhovsky A. Dobenecker MW, et al. Among authors: rioja i. J Exp Med. 2018 Apr 2;215(4):1101-1113. doi: 10.1084/jem.20170084. Epub 2018 Mar 9. J Exp Med. 2018. PMID: 29523590 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.
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