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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: werner t. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.
A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation.
Bergamini G, Bell K, Shimamura S, Werner T, Cansfield A, Müller K, Perrin J, Rau C, Ellard K, Hopf C, Doce C, Leggate D, Mangano R, Mathieson T, O'Mahony A, Plavec I, Rharbaoui F, Reinhard F, Savitski MM, Ramsden N, Hirsch E, Drewes G, Rausch O, Bantscheff M, Neubauer G. Bergamini G, et al. Among authors: werner t. Nat Chem Biol. 2012 Apr 29;8(6):576-82. doi: 10.1038/nchembio.957. Nat Chem Biol. 2012. PMID: 22544264
High-resolution enabled TMT 8-plexing.
Werner T, Becher I, Sweetman G, Doce C, Savitski MM, Bantscheff M. Werner T, et al. Anal Chem. 2012 Aug 21;84(16):7188-94. doi: 10.1021/ac301553x. Epub 2012 Aug 8. Anal Chem. 2012. PMID: 22881393
The commonly used PI3-kinase probe LY294002 is an inhibitor of BET bromodomains.
Dittmann A, Werner T, Chung CW, Savitski MM, Fälth Savitski M, Grandi P, Hopf C, Lindon M, Neubauer G, Prinjha RK, Bantscheff M, Drewes G. Dittmann A, et al. Among authors: werner t. ACS Chem Biol. 2014 Feb 21;9(2):495-502. doi: 10.1021/cb400789e. Epub 2013 Dec 10. ACS Chem Biol. 2014. PMID: 24533473
Tracking cancer drugs in living cells by thermal profiling of the proteome.
Savitski MM, Reinhard FB, Franken H, Werner T, Savitski MF, Eberhard D, Martinez Molina D, Jafari R, Dovega RB, Klaeger S, Kuster B, Nordlund P, Bantscheff M, Drewes G. Savitski MM, et al. Among authors: werner t. Science. 2014 Oct 3;346(6205):1255784. doi: 10.1126/science.1255784. Epub 2014 Oct 2. Science. 2014. PMID: 25278616
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.
Chen P, Chaikuad A, Bamborough P, Bantscheff M, Bountra C, Chung CW, Fedorov O, Grandi P, Jung D, Lesniak R, Lindon M, Müller S, Philpott M, Prinjha R, Rogers C, Selenski C, Tallant C, Werner T, Willson TM, Knapp S, Drewry DH. Chen P, et al. Among authors: werner t. J Med Chem. 2016 Feb 25;59(4):1410-24. doi: 10.1021/acs.jmedchem.5b00209. Epub 2015 Apr 6. J Med Chem. 2016. PMID: 25799074 Free PMC article.
Structure-Based Optimization of Naphthyridones into Potent ATAD2 Bromodomain Inhibitors.
Bamborough P, Chung CW, Furze RC, Grandi P, Michon AM, Sheppard RJ, Barnett H, Diallo H, Dixon DP, Douault C, Jones EJ, Karamshi B, Mitchell DJ, Prinjha RK, Rau C, Watson RJ, Werner T, Demont EH. Bamborough P, et al. Among authors: werner t. J Med Chem. 2015 Aug 13;58(15):6151-78. doi: 10.1021/acs.jmedchem.5b00773. Epub 2015 Jul 31. J Med Chem. 2015. PMID: 26230603
829 results