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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: zhang xp. 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
MEK inhibitors overcome resistance to BET inhibition across a number of solid and hematologic cancers.
Wyce A, Matteo JJ, Foley SW, Felitsky DJ, Rajapurkar SR, Zhang XP, Musso MC, Korenchuk S, Karpinich NO, Keenan KM, Stern M, Mathew LK, McHugh CF, McCabe MT, Tummino PJ, Kruger RG, Carpenter C, Barbash O. Wyce A, et al. Among authors: zhang xp. Oncogenesis. 2018 Apr 20;7(4):35. doi: 10.1038/s41389-018-0043-9. Oncogenesis. 2018. PMID: 29674704 Free PMC article.
GSK137, a potent small-molecule BCL6 inhibitor with in vivo activity, suppresses antibody responses in mice.
Pearce AC, Bamford MJ, Barber R, Bridges A, Convery MA, Demetriou C, Evans S, Gobbetti T, Hirst DJ, Holmes DS, Hutchinson JP, Jayne S, Lezina L, McCabe MT, Messenger C, Morley J, Musso MC, Scott-Stevens P, Manso AS, Schofield J, Slocombe T, Somers D, Walker AL, Wyce A, Zhang XP, Wagner SD. Pearce AC, et al. Among authors: zhang xp. J Biol Chem. 2021 Aug;297(2):100928. doi: 10.1016/j.jbc.2021.100928. Epub 2021 Jul 15. J Biol Chem. 2021. PMID: 34274316 Free PMC article.
Activation of the p53-MDM4 regulatory axis defines the anti-tumour response to PRMT5 inhibition through its role in regulating cellular splicing.
Gerhart SV, Kellner WA, Thompson C, Pappalardi MB, Zhang XP, Montes de Oca R, Penebre E, Duncan K, Boriack-Sjodin A, Le B, Majer C, McCabe MT, Carpenter C, Johnson N, Kruger RG, Barbash O. Gerhart SV, et al. Among authors: zhang xp. Sci Rep. 2018 Jun 26;8(1):9711. doi: 10.1038/s41598-018-28002-y. Sci Rep. 2018. PMID: 29946150 Free PMC article.
1,283 results