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Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe.
Humphreys PG, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Hayhow TG, Hussain J, Jones KL, Lindon M, Michon AM, Renaux JF, Suckling CJ, Tough DF, Prinjha RK. Humphreys PG, et al. Among authors: Tough DF. J Med Chem. 2017 Jan 26;60(2):695-709. doi: 10.1021/acs.jmedchem.6b01566. Epub 2017 Jan 9. J Med Chem. 2017. PMID: 28002667
Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.
Bassi ZI, Fillmore MC, Miah AH, Chapman TD, Maller C, Roberts EJ, Davis LC, Lewis DE, Galwey NW, Waddington KE, Parravicini V, Macmillan-Jones AL, Gongora C, Humphreys PG, Churcher I, Prinjha RK, Tough DF. Bassi ZI, et al. Among authors: Tough DF. ACS Chem Biol. 2018 Oct 19;13(10):2862-2867. doi: 10.1021/acschembio.8b00705. Epub 2018 Sep 18. ACS Chem Biol. 2018. PMID: 30200762
Bromodomain Proteins Contribute to Maintenance of Bloodstream Form Stage Identity in the African Trypanosome.
Schulz D, Mugnier MR, Paulsen EM, Kim HS, Chung CW, Tough DF, Rioja I, Prinjha RK, Papavasiliou FN, Debler EW. Schulz D, et al. Among authors: Tough DF. PLoS Biol. 2015 Dec 8;13(12):e1002316. doi: 10.1371/journal.pbio.1002316. eCollection 2015 Dec. PLoS Biol. 2015. PMID: 26646171 Free PMC article.
Epigenetic drug discovery: breaking through the immune barrier.
Tough DF, Tak PP, Tarakhovsky A, Prinjha RK. Tough DF, et al. Nat Rev Drug Discov. 2016 Dec;15(12):835-853. doi: 10.1038/nrd.2016.185. Epub 2016 Oct 21. Nat Rev Drug Discov. 2016. PMID: 27765940 Review.
Influenza's signature move.
Tough DF. Tough DF. Nat Immunol. 2018 Jun;19(6):518-520. doi: 10.1038/s41590-018-0115-1. Nat Immunol. 2018. PMID: 29777225 No abstract available.
BET Bromodomain Inhibitor iBET151 Impedes Human ILC2 Activation and Prevents Experimental Allergic Lung Inflammation.
Kerscher B, Barlow JL, Rana BM, Jolin HE, Gogoi M, Bartholomew MA, Jhamb D, Pandey A, Tough DF, van Oosterhout AJM, McKenzie ANJ. Kerscher B, et al. Among authors: Tough DF. Front Immunol. 2019 Apr 9;10:678. doi: 10.3389/fimmu.2019.00678. eCollection 2019. Front Immunol. 2019. PMID: 31024538 Free PMC article.
BET bromodomain inhibition reduces maturation and enhances tolerogenic properties of human and mouse dendritic cells.
Schilderink R, Bell M, Reginato E, Patten C, Rioja I, Hilbers FW, Kabala PA, Reedquist KA, Tough DF, Tak PP, Prinjha RK, de Jonge WJ. Schilderink R, et al. Among authors: Tough DF. Mol Immunol. 2016 Nov;79:66-76. doi: 10.1016/j.molimm.2016.09.010. Epub 2016 Oct 3. Mol Immunol. 2016. PMID: 27710838
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