未登录 BET Isoform Selectivity through Diverse Linkers for Bivalent Inhibitors: GSK785, a BRD2/4-Selective Bivalent BET Inhibitor Rianjongdee, Francesco; Atkinson, Stephen J.; Bamborough, Paul; Barnett, Heather A.; Friston, Kallie; Grandi, Paola; Neipp, Christopher E.; Petretich, Massimo; Phillipou, Alex; Preston, Alex G. S.; Prinjha, Rab K.; Tomkinson, Nicholas C. O.; Demont, Emmanuel H. 分享 收藏
Identification of novel bromodomain inhibitors of Trypanosoma cruzi bromodomain factor 2 (TcBDF2) using a fluorescence polarization-based high-throughput assay Tavernelli, Luis E.; Alonso, Victoria L.; Pena, Imanol; Araya, Elvio Rodriguez; Manarin, Romina; Cantizani, Juan; Martin, Julio; Salamanca, Juan; Bamborough, Paul; Calderon, Felix; Gabarro, Raquel; Serra, Esteban 分享 收藏
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. 分享 收藏
Design and Characterization of 1,3-Dihydro-2H-benzo[d]azepin-2-ones as Rule-of-5 Compliant Bivalent BET Inhibitors Bamborough, Paul; Chung, Chun-wa; Goodwin, Nicole C. C.; Mitchell, Darren J. J.; Neipp, Christopher E. E.; Phillipou, Alex; Preston, Alex; Prinjha, Rab K. K.; Soden, Peter E. E.; Watson, Robert J. J.; Demont, Emmanuel H. H. 分享 收藏
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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 分享 收藏
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. 分享 收藏
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism Wellaway, Christopher R.; Baldwin, Ian R.; Bamborough, Paul; Barker, Daniel; Bartholomew, Michelle A.; Chung, Chun-wa; Dumpelfeld, Birgit; Evans, John P.; Fazakerley, Neal J.; Homes, Paul; Keeling, Steven P.; Lewell, Xiao Q.; McNab, Finlay W.; Morley, Joanne; Needham, Deborah; Neu, Margarete; van Oosterhout, Antoon J. M.; Pal, Anshu; Reinhard, Friedrich B. M.; Rianjongdee, Francesco; Robertson, Craig M.; Rowland, Paul; Shah, Rishi R.; Sherriff, Emma B.; Sloan, Lisa A.; Teague, Simon; Thomas, Daniel A.; Wellaway, Natalie; Wojno-Picon, Justyna; Woolven, James M.; Coe, Diane M. 分享 收藏
Expanding Bromodomain Targeting into Neglected Parasitic Diseases Tallant, Cynthia; Bamborough, Paul; Chung, Chun-wa; Gamo, Francisco Javier; Kirkpatrick, Robert; Larminie, Chris; Martin, Julio; Prinjha, Rab; Rioja, Inmaculada; Simola, Daniel F.; Gabarro, Raquel; Calderon, Felix 分享 收藏
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. 分享 收藏
Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors Seal, Jonathan T.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-Wa; Foley, James; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Kruger, Ryan G.; Matteo, Jeanne J.; McCabe, Michael T.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alex; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Taylor, Simon; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Wyce, Anastasia; Zhang, Xi-Ping; Demont, Emmanuel H. 分享 收藏
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors Aylott, Helen E.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Hayhow, Thomas G.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alexander; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Seal, Jonathan T.; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Demont, Emmanuel H. 分享 收藏
A Photoaffinity-Based Fragment-Screening Platform for Efficient Identification of Protein Ligands Grant, Emma K.; Fallon, David J.; Hann, Michael M.; Fantom, Ken G. M.; Quinn, Chad; Zappacosta, Francesca; Annan, Roland S.; Chung, Chun-wa; Bamborough, Paul; Dixon, David P.; Stacey, Peter; House, David; Patel, Vipulkumar K.; Tomkinson, Nicholas C. O.; Bush, Jacob T. 分享 收藏
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.; Wyspianska, Beata S.; Kerr, William J.; Prinjha, Rab K. 分享 收藏
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. 分享 收藏
GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins Watson, Robert J.; Bamborough, Paul; Barnett, Heather; Chung, Chun-wa; Davis, Rob; Gordon, Laurie; Grandi, Paola; Petretich, Massimo; Phillipou, Alex; Prinjha, Rab K.; Rioja, Inmaculada; Soden, Peter; Werner, Thilo; Demont, Emmanuel H. 分享 收藏
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. 分享 收藏
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family Preston, Alex; Atkinson, Stephen J.; Bamborough, Paul; Chung, Chun-wa; Gordon, Laurie J.; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Lewis, Antonia J.; Lugo, David; Messenger, Cassie; Michon, Anne-Marie; Mitchell, Darren J.; Prinjha, Rab K.; Rioja, Inmaculada; Seal, Jon; Taylor, Simon; Thesmar, Pierre; Wall, Ian D.; Watson, J.; Woolven, James M.; Demont, Emmanuel H. 分享 收藏
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. 分享 收藏
CDK12 inhibition reduces abnormalities in cells from patients with myotonic dystrophy and in a mouse model Ketley, Ami; Wojciechowska, Marzena; Ghidelli-Disse, Sonja; Bamborough, Paul; Ghosh, Tushar K.; Morato, Marta Lopez; Sedehizadeh, Saam; Malik, Naveed Altaf; Tang, Zhenzhi; Powalowska, Paulina; Tanner, Matthew; Billeter-Clark, Rudolf; Trueman, Rebecca C.; Geiszler, Philippine C.; Agostini, Alessandra; Othman, Othman; Bosche, Markus; Bantscheff, Marcus; Rudiger, Martin; Mossakowska, Danuta E.; Drewry, David H.; Zuercher, William J.; Thornton, Charles A.; Drewes, Gerard; Uings, Iain; Hayes, Christopher J.; Brook, J. David 分享 收藏
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