The Discovery of I‑BET726 (GSK1324726A), a Potent Tetrahydroquinoline ApoA1 Up-Regulator and Selective BET Bromodomain Inhibitor von Gosmini, Romain, Nguyen, Van Loc, Toum, Jérôme, Simon, Christophe, Brusq, Jean-Marie G, Krysa, Gael, Mirguet, Olivier, Riou-Eymard, Alizon M, Boursier, Eric V, Trottet, Lionel, Bamborough, Paul, Clark, Hugh, Chung, Chun-wa, Cutler, Leanne, Demont, Emmanuel H, Kaur, Rejbinder, Lewis, Antonia J, Schilling, Mark B, Soden, Peter E, Taylor, Simon, Walker, Ann L, Walker, Matthew D, Prinjha, Rab K, Nicodème, Edwige

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Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression von Jones, Katherine L, Beaumont, Dominic M, Bernard, Sharon G, Bit, Rino A, Campbell, Simon P, Chung, Chun-Wa, Cutler, Leanne, Demont, Emmanuel H, Dennis, Kate, Gordon, Laurie, Gray, James R, Haase, Michael V, Lewis, Antonia J, McCleary, Scott, Mitchell, Darren J, Moore, Susanne M, Parr, Nigel, Robb, Olivia J, Smithers, Nicholas, Soden, Peter E, Suckling, Colin J, Taylor, Simon, Walker, Ann L, Watson, Robert J, Prinjha, Rab K

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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation von Gilan, Omer, Rioja, Inmaculada, Knezevic, Kathy, Bell, Matthew J, Yeung, Miriam M, Harker, Nicola R, Lam, Enid Y N, Chung, Chun-Wa, Bamborough, Paul, Petretich, Massimo, Urh, Marjeta, Atkinson, Stephen J, Bassil, Anna K, Roberts, Emma J, Vassiliadis, Dane, Burr, Marian L, Preston, Alex G S, Wellaway, Christopher, Werner, Thilo, Gray, James R, Michon, Anne-Marie, Gobbetti, Thomas, Kumar, Vinod, Soden, Peter E, Haynes, Andrea, Vappiani, Johanna, Tough, David F, Taylor, Simon, Dawson, Sarah-Jane, Bantscheff, Marcus, Lindon, Matthew, Drewes, Gerard, Demont, Emmanuel H, Daniels, Danette L, Grandi, Paola, Prinjha, Rab K, Dawson, Mark A

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The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes von Atkinson, Stephen J., Soden, Peter E., Angell, Davina C., Bantscheff, Marcus, Chung, Chun-wa, Giblin, Kathryn A., Smithers, Nicholas, Furze, Rebecca C., Gordon, Laurie, Drewes, Gerard, Rioja, Inmaculada, Witherington, Jason, Parr, Nigel J., Prinjha, Rab K.

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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia von Dawson, Mark A., Prinjha, Rab K., Dittmann, Antje, Giotopoulos, George, Bantscheff, Marcus, Chan, Wai-In, Robson, Samuel C., Chung, Chun-wa, Hopf, Carsten, Savitski, Mikhail M., Huthmacher, Carola, Gudgin, Emma, Lugo, Dave, Beinke, Soren, Chapman, Trevor D., Roberts, Emma J., Soden, Peter E., Auger, Kurt R., Mirguet, Olivier, Doehner, Konstanze, Delwel, Ruud, Burnett, Alan K., Jeffrey, Phillip, Drewes, Gerard, Lee, Kevin, Huntly, Brian J. P., Kouzarides, Tony

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Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N‑Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative P... von Wellaway, Christopher R, Bamborough, Paul, Bernard, Sharon G, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Demont, Emmanuel H, Evans, John P, Gordon, Laurie, Karamshi, Bhumika, Lewis, Antonia J, Lindon, Matthew J, Mitchell, Darren J, Rioja, Inmaculada, Soden, Peter E, Taylor, Simon, Watson, Robert J, Willis, Rob, Woolven, James M, Wyspiańska, Beata S, Kerr, William J, Prinjha, Rab K

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Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BR... von Clegg, Michael A, Bamborough, Paul, Chung, Chun-Wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Leveridge, Melanie, Lindon, Matthew, Liwicki, Gemma M, Michon, Anne-Marie, Molnar, Judit, Rioja, Inmaculada, Soden, Peter E, Theodoulou, Natalie H, Werner, Thilo, Tomkinson, Nicholas C O, Prinjha, Rab K, Humphreys, Philip G

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A randomized study of the safety and pharmacokinetics of GSK3358699, a mononuclear myeloid‐targeted bromodomain and extra‐terminal domain inhibitor von Brown, Jack A., Bal, Joanne, Simeoni, Monica, Williams, Peter, Mander, Palwinder K., Soden, Peter E., Daga, Shruti, Fahy, William A., Wong, Gabriel K., Bloomer, Jackie C., Erwig, Lars, Cui, Yi, Fernando, Disala, Carnaghan, Helen, Banham‐Hall, Edward J., Hopkins, Sarah, Davis, Bill G., Oliveira, Joao J. D., Prinjha, Rabinder K.

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Design and Characterization of 1,3-Dihydro‑2H‑benzo[d]azepin-2-ones as Rule-of‑5 Compliant Bivalent BET Inhibitors von Bamborough, Paul, Chung, Chun-wa, Goodwin, Nicole C., Mitchell, Darren J., Neipp, Christopher E., Phillipou, Alex, Preston, Alex, Prinjha, Rab K., Soden, Peter E., Watson, Robert J., Demont, Emmanuel H.

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Discovery of Potent, Isoform-Selective Inhibitors of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups and a N‑(2-Aminophenyl)benzamide Binding Unit von Marson, Charles M, Matthews, Christopher J, Yiannaki, Elena, Atkinson, Stephen J, Soden, Peter E, Shukla, Lena, Lamadema, Nermina, Thomas, N. Shaun B

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Design and Characterization of 1,3-Dihydro-2 H -benzo[ d ]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors von Bamborough, Paul, Chung, Chun-Wa, Goodwin, Nicole C, Mitchell, Darren J, Neipp, Christopher E, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Soden, Peter E, Watson, Robert J, Demont, Emmanuel H

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MAPK-activated Protein Kinase 2 Deficiency in Microglia Inhibits Pro-inflammatory Mediator Release and Resultant Neurotoxicity: RELEVANCE TO NEUROINFLAMMATION IN A TRANSGENIC MOUSE... von Culbert, Ainsley A, Skaper, Stephen D, Howlett, David R, Evans, Nicholas A, Facci, Laura, Soden, Peter E, Seymour, Zoe M, Guillot, Florence, Gaestel, Matthias, Richardson, Jill C

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Oligodendrocytes are a Novel Source of Amyloid Peptide Generation von Skaper, Stephen D., Evans, Nicholas A., Soden, Peter E., Rosin, Claudia, Facci, Laura, Richardson, Jill C.

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Design and Characterization of 1,3-Dihydro-2H-benzodazepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors von Bamborough, Paul, Chung, Chun-Wa, Goodwin, Nicole C, Mitchell, Darren J, Neipp, Christopher E, Phillipou, Alex, Preston, Alex, Prinjha, Rab K, Soden, Peter E, Watson, Robert J, Demont, Emmanuel H

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MAPK-activated Protein Kinase 2 Deficiency in Microglia Inhibits Pro-inflammatory Mediator Release and Resultant Neurotoxicity von Culbert, Ainsley A., Skaper, Stephen D., Howlett, David R., Evans, Nicholas A., Facci, Laura, Soden, Peter E., Seymour, Zoe M., Guillot, Florence, Gaestel, Matthias, Richardson, Jill C.

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Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation von Gilan, Omer, Rioja, Inmaculada, Knezevic, Kathy, Bell, Matthew J, Yeung, Miriam M., Harker, Nicola R, Lam, Enid Y.N., Chung, Chun-wa, Bamborough, Paul, Petretich, Massimo, Urh, Marjeta, Atkinson, Stephen J, Bassil, Anna K, Roberts, Emma J, Vassiliadis, Dane, Burr, Marian L., Preston, Alex G.S, Wellaway, Christopher, Werner, Thilo, Gray, James R, Michon, Anne-Marie, Gobbetti, Thomas, Kumar, Vinod, Soden, Peter E, Haynes, Andrea, Vappiani, Johanna, Tough, David F, Taylor, Simon, Dawson, Sarah-Jane, Bantscheff, Marcus, Lindon, Matthew, Drewes, Gerard, Demont, Emmanuel H, Daniels, Danette L., Grandi, Paola, Prinjha, Rab K, Dawson, Mark A.

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Aβ1–42 reduces synapse number and inhibits neurite outgrowth in primary cortical and hippocampal neurons: A quantitative analysis von Evans, Nicholas A., Facci, Laura, Owen, Davina E., Soden, Peter E., Burbidge, Stephen A., Prinjha, Rab K., Richardson, Jill C., Skaper, Stephen D.

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Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia von Dawson, Mark A, Prinjha, Rab K, Dittmann, Antje, Giotopoulos, George, Bantscheff, Marcus, Chan, Wai-In, Robson, Samuel C, Chung, Chun-wa, Hopf, Carsten, Savitski, Mikhail M, Huthmacher, Carola, Gudgin, Emma, Lugo, Dave, Beinke, Soren, Chapman, Trevor D, Roberts, Emma J, Soden, Peter E, Auger, Kurt R, Mirguet, Olivier, Doehner, Konstanze, Delwel, Ruud, Burnett, Alan K, Jeffrey, Phillip, Drewes, Gerard, Lee, Kevin, Huntly, Brian J.P, Kouzarides, Tony

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The structure based design of dual HDAC/BET inhibitors as novel epigenetic probesElectronic supplementary information (ESI) available. See DOI: 10.1039/c3md00285c von Atkinson, Stephen J, Soden, Peter E, Angell, Davina C, Bantscheff, Marcus, Chung, Chun-wa, Giblin, Kathryn A, Smithers, Nicholas, Furze, Rebecca C, Gordon, Laurie, Drewes, Gerard, Rioja, Inmaculada, Witherington, Jason, Parr, Nigel J, Prinjha, Rab K

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Abeta(1-42) reduces synapse number and inhibits neurite outgrowth in primary cortical and hippocampal neurons: a quantitative analysis von Evans, Nicholas A, Facci, Laura, Owen, Davina E, Soden, Peter E, Burbidge, Stephen A, Prinjha, Rab K, Richardson, Jill C, Skaper, Stephen D

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