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)
Get full text
Journal Article
Clinical progress and pharmacology of small molecule bromodomain inhibitors
Theodoulou, Natalie H, Tomkinson, Nicholas CO, Prinjha, Rab K, Humphreys, Philip G
Published in Current opinion in chemical biology (01.08.2016)
Published in Current opinion in chemical biology (01.08.2016)
Get full text
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)
Get full text
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)
Get full text
Journal Article
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I‑BET432
Humphreys, Philip G., Anderson, Niall A., Bamborough, Paul, Baxter, Andrew, Chung, Chun-wa, Cookson, Rosa, Craggs, Peter D., Dalton, Toryn, Fournier, Julie C. L., Gordon, Laurie J., Gray, Heather F., Gray, Matthew W., Gregory, Richard, Hirst, David J., Jamieson, Craig, Jones, Katherine L., Kessedjian, Hripsimee, Lugo, David, McGonagle, Grant, Patel, Vipulkumar K., Patten, Christopher, Poole, Darren L., Prinjha, Rab K., Ramirez-Molina, Cesar, Rioja, Inmaculada, Seal, Gail, Stafford, Kayleigh A. J., Shah, Rishi R., Tape, Daniel, Theodoulou, Natalie H., Tomlinson, Laura, Ukuser, Sabri, Wall, Ian D., Wellaway, Natalie, White, Gemma
Published in Journal of medicinal chemistry (24.11.2022)
Published in Journal of medicinal chemistry (24.11.2022)
Get full text
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)
Get full text
Journal Article
Progress in the Development of non-BET Bromodomain Chemical Probes
Theodoulou, Natalie H., Tomkinson, Nicholas C. O., Prinjha, Rab K., Humphreys, Philip G.
Published in ChemMedChem (04.03.2016)
Published in ChemMedChem (04.03.2016)
Get full text
Journal Article
Alkene anti-Dihydroxylation with Malonoyl Peroxides
Alamillo-Ferrer, Carla, Davidson, Stuart C, Rawling, Michael J, Theodoulou, Natalie H, Campbell, Matthew, Humphreys, Philip G, Kennedy, Alan R, Tomkinson, Nicholas C. O
Published in Organic letters (16.10.2015)
Published in Organic letters (16.10.2015)
Get full text
Journal Article
Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3
Sekirnik (née Measures), Angelina R., Hewings, David S., Theodoulou, Natalie H., Jursins, Lukass, Lewendon, Katie R., Jennings, Laura E., Rooney, Timothy P. C., Heightman, Tom D., Conway, Stuart J.
Published in Angewandte Chemie (International ed.) (11.07.2016)
Published in Angewandte Chemie (International ed.) (11.07.2016)
Get full text
Journal Article
Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors
Clegg, Michael A, Theodoulou, Natalie H, Bamborough, Paul, Chung, Chun-wa, Craggs, Peter D, Demont, Emmanuel H, Gordon, Laurie J, Liwicki, Gemma M, Phillipou, Alex, Tomkinson, Nicholas C. O, Prinjha, Rab K, Humphreys, Philip G
Published in ACS medicinal chemistry letters (12.08.2021)
Published in ACS medicinal chemistry letters (12.08.2021)
Get full text
Journal Article
Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3
Sekirnik (née Measures), Angelina R., Hewings, David S., Theodoulou, Natalie H., Jursins, Lukass, Lewendon, Katie R., Jennings, Laura E., Rooney, Timothy P. C., Heightman, Tom D., Conway, Stuart J.
Published in Angewandte Chemie (11.07.2016)
Published in Angewandte Chemie (11.07.2016)
Get full text
Journal Article
ChemInform Abstract: Alkene anti‐Dihydroxylation with Malonoyl Peroxides
Alamillo‐Ferrer, Carla, Davidson, Stuart C., Rawling, Michael J., Theodoulou, Natalie H., Campbell, Matthew, Humphreys, Philip G., Kennedy, Alan R., Tomkinson, Nicholas C. O.
Published in ChemInform (01.02.2016)
Published in ChemInform (01.02.2016)
Get full text
Journal Article