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BETA
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation
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.
Published in Science (American Association for the Advancement of Science) (24.04.2020)
Published in Science (American Association for the Advancement of Science) (24.04.2020)
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Journal Article
Discovery of I‑BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition
Theodoulou, Natalie H, Bamborough, Paul, Bannister, Andrew J, Becher, Isabelle, Bit, Rino A, Che, Ka Hing, Chung, Chun-wa, Dittmann, Antje, Drewes, Gerard, Drewry, David H, Gordon, Laurie, Grandi, Paola, Leveridge, Melanie, Lindon, Matthew, Michon, Anne-Marie, Molnar, Judit, Robson, Samuel C, Tomkinson, Nicholas C. O, Kouzarides, Tony, Prinjha, Rab K, Humphreys, Philip G
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N‑Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype
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
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening
Wellaway, Christopher R, Amans, Dominique, Bamborough, Paul, Barnett, Heather, Bit, Rino A, Brown, Jack A, Carlson, Neil R, Chung, Chun-wa, Cooper, Anthony W. J, Craggs, Peter D, Davis, Robert P, Dean, Tony W, Evans, John P, Gordon, Laurie, Harada, Isobel L, Hirst, David J, Humphreys, Philip G, Jones, Katherine L, Lewis, Antonia J, Lindon, Matthew J, Lugo, Dave, Mahmood, Mahnoor, McCleary, Scott, Medeiros, Patricia, Mitchell, Darren J, O’Sullivan, Michael, Le Gall, Armelle, Patel, Vipulkumar K, Patten, Chris, Poole, Darren L, Shah, Rishi R, Smith, Jane E, Stafford, Kayleigh A. J, Thomas, Pamela J, Vimal, Mythily, Wall, Ian D, Watson, Robert J, Wellaway, Natalie, Yao, Gang, Prinjha, Rab K
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Journal Article
Design, Synthesis, and Characterization of I‑BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate
Humphreys, Philip G, Atkinson, Stephen J, Bamborough, Paul, Bit, Rino A, Chung, Chun-wa, Craggs, Peter D, Cutler, Leanne, Davis, Rob, Ferrie, Alan, Gong, GangLi, Gordon, Laurie J, Gray, Matthew, Harrison, Lee A, Hayhow, Thomas G, Haynes, Andrea, Henley, Nick, Hirst, David J, Holyer, Ian D, Lindon, Matthew J, Lovatt, Cerys, Lugo, David, McCleary, Scott, Molnar, Judit, Osmani, Qendresa, Patten, Chris, Preston, Alex, Rioja, Inmaculada, Seal, Jonathan T, Smithers, Nicholas, Sun, Fenglai, Tang, Dalin, Taylor, Simon, Theodoulou, Natalie H, Thomas, Clare, Watson, Robert J, Wellaway, Christopher R, Zhu, Linrong, Tomkinson, Nicholas C. O, Prinjha, Rab K
Published in Journal of medicinal chemistry (10.02.2022)
Published in Journal of medicinal chemistry (10.02.2022)
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Journal Article
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I‑BET787
Hirst, David J., Bamborough, Paul, Al-Mahdi, Niam, Angell, Davina C., Barnett, Heather A., Baxter, Andrew, Bit, Rino A., Brown, Jack A., Chung, Chun-wa, Craggs, Peter D., Davis, Robert P., Demont, Emmanuel H., Ferrie, Alan, Gordon, Laurie J., Harada, Isobel, Ho, Tim C. T., Holyer, Ian D., Hooper-Greenhill, Edward, Jones, Katherine L., Lindon, Matthew J., Lovatt, Cerys, Lugo, David, Maller, Claire, McGonagle, Grant, Messenger, Cassie, Mitchell, Darren J., Pascoe, David D., Patel, Vipulkumar K., Patten, Christopher, Poole, Darren L., Shah, Rishi R., Rioja, Inmaculada, Stafford, Kayleigh A. J., Tape, Daniel, Taylor, Simon, Theodoulou, Natalie H., Tomlinson, Laura, Wall, Ian D., Wellaway, Christopher R., White, Gemma, Prinjha, Rab K., Humphreys, Philip G.
Published in Journal of medicinal chemistry (27.06.2024)
Published in Journal of medicinal chemistry (27.06.2024)
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Journal Article
The Commonly Used PI3-Kinase Probe LY294002 Is an Inhibitor of BET Bromodomains
Dittmann, Antje, Werner, Thilo, Chung, Chun-Wa, Savitski, Mikhail M, Fälth Savitski, Maria, Grandi, Paola, Hopf, Carsten, Lindon, Matthew, Neubauer, Gitte, Prinjha, Rabinder K, Bantscheff, Marcus, Drewes, Gerard
Published in ACS chemical biology (21.02.2014)
Published in ACS chemical biology (21.02.2014)
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Journal Article
Epigenetic pathway targets for the treatment of disease: accelerating progress in the development of pharmacological tools: IUPHAR Review 11
Tough, David F, Lewis, Huw D, Rioja, Inmaculada, Lindon, Matthew J, Prinjha, Rab K
Published in British journal of pharmacology (01.11.2014)
Published in British journal of pharmacology (01.11.2014)
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Journal Article
BET bromodomain inhibition promotes neurogenesis while inhibiting gliogenesis in neural progenitor cells
Li, Jingjun, Ma, Jing, Meng, Guofeng, Lin, Hong, Wu, Sharon, Wang, Jamie, Luo, Jie, Xu, Xiaohong, Tough, David, Lindon, Matthew, Rioja, Inmaculada, Zhao, Jing, Mei, Hongkang, Prinjha, Rab, Zhong, Zhong
Published in Stem cell research (01.09.2016)
Published in Stem cell research (01.09.2016)
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Journal Article
A novel series of potent γ-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core
Lewis, Stephen J., Smith, Adrian L., Neduvelil, Joseph G., Stevenson, Graeme I., Lindon, Matthew J., Jones, A. Brian, Shearman, Mark S., Beher, Dirk, Clarke, Earl, Best, Jonathan D., Peachey, James E., Harrison, Timothy, Castro, J. Luis
Published in Bioorganic & medicinal chemistry letters (17.01.2005)
Published in Bioorganic & medicinal chemistry letters (17.01.2005)
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Journal Article
Oxazolidinones as novel human CCR8 antagonists
Jin, Jian, Wang, Yonghui, Wang, Feng, Kerns, Jeffery K., Vinader, Victoria M., Hancock, Ashley P., Lindon, Matthew J., Stevenson, Graeme I., Morrow, Dwight M., Rao, Parvathi, Nguyen, Cuc, Barrett, Victoria J., Browning, Chris, Hartmann, Guido, Andrew, David P., Sarau, Henry M., Foley, James J., Jurewicz, Anthony J., Fornwald, James A., Harker, Andy J., Moore, Michael L., Rivero, Ralph A., Belmonte, Kristen E., Connor, Helen E.
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
Published in Bioorganic & medicinal chemistry letters (15.03.2007)
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Journal Article
Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain
Law, Robert P, Atkinson, Stephen J, Bamborough, Paul, Chung, Chun-wa, Demont, Emmanuel H, Gordon, Laurie J, Lindon, Matthew, Prinjha, Rab K, Watson, Allan J. B, Hirst, David J
Published in Journal of medicinal chemistry (24.05.2018)
Published in Journal of medicinal chemistry (24.05.2018)
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Journal Article
Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B
Chen, Peiling, Chaikuad, Apirat, Bamborough, Paul, Bantscheff, Marcus, Bountra, Chas, Chung, Chun-wa, Fedorov, Oleg, Grandi, Paola, Jung, David, Lesniak, Robert, Lindon, Matthew, Müller, Susanne, Philpott, Martin, Prinjha, Rab, Rogers, Catherine, Selenski, Carolyn, Tallant, Cynthia, Werner, Thilo, Willson, Timothy M, Knapp, Stefan, Drewry, David H
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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Journal Article
The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor
Seal, Jonathan T, Atkinson, Stephen J, Aylott, Helen, Bamborough, Paul, Chung, Chun-wa, Copley, Royston C. B, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Harrison, Lee A, Hayhow, Thomas G, Lindon, Matthew, Messenger, Cassie, Michon, Anne-Marie, Mitchell, Darren, Preston, Alex, Prinjha, Rab K, Rioja, Inmaculada, Taylor, Simon, Wall, Ian D, Watson, Robert J, Woolven, James M, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins
Preston, Alex, Atkinson, Stephen, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Gray, James R. J, Jones, Emma J, Lindon, Matthew, Michon, Anne-Marie, Mitchell, Darren J, Prinjha, Rab K, Rianjongdee, Francesco, Rioja, Inmaculada, Seal, Jonathan, Taylor, Simon, Wall, Ian, Watson, Robert J, Woolven, James, Demont, Emmanuel H
Published in Journal of medicinal chemistry (10.09.2020)
Published in Journal of medicinal chemistry (10.09.2020)
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Journal Article
Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe
Humphreys, Philip G, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Gordon, Laurie, Grandi, Paola, Hayhow, Thomas G, Hussain, Jameed, Jones, Katherine L, Lindon, Matthew, Michon, Anne-Marie, Renaux, Jessica F, Suckling, Colin J, Tough, David F, Prinjha, Rab K
Published in Journal of medicinal chemistry (26.01.2017)
Published in Journal of medicinal chemistry (26.01.2017)
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Journal Article
Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains
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.
Published in Journal of medicinal chemistry (11.06.2020)
Published in Journal of medicinal chemistry (11.06.2020)
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Journal Article
Structure-based optimisation of orally active & reversible MetAP-2 inhibitors maintaining a tight ‘molecular budget’
Hirst, David J., Brandt, Martin, Bruton, Gordon, Christodoulou, Erica, Cutler, Leanne, Deeks, Nigel, Goodacre, Jonathan D., Jack, Torquil, Lindon, Matthew, Miah, Afjal, Page, Kevin, Parr, Nigel, Shukla, Lena, Sims, Martin, Thomas, Pamela, Thorpe, James, Holmes, Duncan S.
Published in Bioorganic & medicinal chemistry letters (01.11.2020)
Published in Bioorganic & medicinal chemistry letters (01.11.2020)
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Journal Article
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immuno-inflammation
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.
Published in Science (American Association for the Advancement of Science) (19.03.2020)
Published in Science (American Association for the Advancement of Science) (19.03.2020)
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Journal Article