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Acute Resistance to BET Inhibitors Remodels Compensatory Transcriptional Programs Via p300 Co-Activation Shah, Viral; Giotopoulos, George; Osaki, Hikari; Meyerhoefer, Markus; Meduri, Eshwar; Gallego-Crespo, Aaron; Behrendt, Malte Andreas; Saura-Panella, Maria; Schubert, Benedict; Yun, Haiyang; Horton, Sarah J.; Singh, Shuchi Agrawal; Haehnel, Patricia S.; Basheer, Faisal; Lugo, Dave; Kuehn, Michael; Guezguez, Borhane; Theobald, Matthias; Kindler, Thomas; Gallipoli, Paolo; Yeh, Paul; Dawson, Mark A.; Prinjha, Rab; Huntly, Brian J. P.; Sasca, Daniel Share Save
Integrated metabolic-transcriptomic network identifies immunometabolic modulations in human macrophages Chen, Hung-Jen; Sevin, Daniel C.; Griffith, Guillermo R.; Vappiani, Johanna; Booty, Lee M.; van Roomen, Cindy P. A. A.; Kuiper, Johan; den Dunnen, Jeroen; de Jonge, Wouter J.; Prinjha, Rab K.; Mander, Palwinder K.; Grandi, Paola; Wyspianska, Beata S.; de Winther, Menno P. J. Share Save
CBP/P300 Inhibition Impairs CD4+ T Cell Activation: Implications for Autoimmune Disorders Picavet, Lucas Wilhelmus; Samat, Anoushka A. K.; Calis, Jorg; Nijhuis, Lotte; Scholman, Rianne; Mokry, Michal; Tough, David F.; Prinjha, Rabinder K.; Vastert, Sebastiaan J.; van Loosdregt, Jorg Share Save
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. Share Save
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe Bradley, Erin; Fusani, Lucia; Chung, Chun-wa; Craggs, Peter D.; Demont, Emmanuel H.; Humphreys, Philip G.; Mitchell, Darren J.; Phillipou, Alex; Rioja, Inmaculada; Shah, Rishi R.; Wellaway, Christopher R.; Prinjha, Rab K.; Palmer, David S.; Kerr, William J.; Reid, Marc; Wall, Ian D.; Cookson, Rosa Share Save
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. Share Save
In silico enhancer mining reveals SNS-032 and EHMT2 inhibitors as therapeutic candidates in high-grade serous ovarian cancer Quintela, Marcos; James, David W.; Garcia, Jetzabel; Edwards, Kadie; Margarit, Lavinia; Das, Nagindra; Lutchman-Singh, Kerryn; Beynon, Amy L.; Rioja, Inmaculada; Prinjha, Rab K.; Harker, Nicola R.; Gonzalez, Deyarina; Steven Conlan, R.; Francis, Lewis W. Share Save
Bromodomain inhibitor i-BET858 triggers a unique transcriptional response coupled to enhanced DNA damage, cell cycle arrest and apoptosis in high-grade ovarian carcinoma cells Quintela, Marcos; James, David W.; Pociute, Agne; Powell, Lydia; Edwards, Kadie; Coombes, Zoe; Garcia, Jetzabel; Garton, Neil; Das, Nagindra; Lutchman-Singh, Kerryn; Margarit, Lavinia; Beynon, Amy L.; Rioja, Inmaculada; Prinjha, Rab K.; Harker, Nicola R.; Gonzalez, Deyarina; Conlan, R. Steven; Francis, Lewis W. Share Save
Drug-induced loss of imprinting revealed using bioluminescent reporters of Cdkn1c Dimond, Andrew; Van de Pette, Mathew; Taylor-Bateman, Victoria; Brown, Karen; Sardini, Alessandro; Whilding, Chad; Feytout, Amelie; Prinjha, Rab K.; Merkenschlager, Matthias; Fisher, Amanda G. Share Save
Endogenous bioluminescent reporters reveal a sustained increase in utrophin gene expression upon EZH2 and ERK1/2 inhibition Gleneadie, Hannah J. J.; Fernandez-Ruiz, Beatriz; Sardini, Alessandro; Van de Pette, Mathew; Dimond, Andrew; Prinjha, Rab K. K.; McGinty, James; French, Paul M. W.; Bagci, Hakan; Merkenschlager, Matthias; Fisher, Amanda G. G. Share Save
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 Share Save
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A BET Protein Inhibitor Targeting Mononuclear Myeloid Cells Affects Specific Inflammatory Mediators and Pathways in Crohn's Disease Elfiky, Ahmed M., I; Hageman, Ishtu L.; Becker, Marte A. J.; Verhoeff, Jan; Li Yim, Andrew Y. F.; Joustra, Vincent W.; Mulders, Lieven; Fung, Ivan; Rioja, Inmaculada; Prinjha, Rab K.; Smithers, Nicholas N.; Furze, Rebecca C.; Mander, Palwinder K.; Bell, Matthew J.; Buskens, Christianne J.; D'Haens, Geert R.; Wildenberg, Manon E.; de Jonge, Wouter J. Share Save
Cohesin couples transcriptional bursting probabilities of inducible enhancers and promoters Robles-Rebollo, Irene; Cuartero, Sergi; Canellas-Socias, Adria; Wells, Sarah; Karimi, Mohammad M.; Mereu, Elisabetta; Chivu, Alexandra G.; Heyn, Holger; Whilding, Chad; Dormann, Dirk; Marguerat, Samuel; Rioja, Inmaculada; Prinjha, Rab K.; Stumpf, Michael P. H.; Fisher, Amanda G.; Merkenschlager, Matthias Share Save
Bromodomain factor 5 is an essential regulator of transcription in Leishmania Jones, Nathaniel G.; Geoghegan, Vincent; Moore, Gareth; Carnielli, Juliana B. T.; Newling, Katherine; Calderon, Felix; Gabarro, Raquel; Martin, Julio; Prinjha, Rab K.; Rioja, Inmaculada; Wilkinson, Anthony J.; Mottram, Jeremy C. Share Save
Phase 1 and preclinical profiling of ESM-HDAC391, a myeloid-targeted histone deacetylase inhibitor, shows enhanced pharmacology and monocytopaenia Furze, Rebecca C.; Molnar, Judit; Parr, Nigel J.; Ahmad, Faiz; Henry, Yvette; Howe, David; Singh, Rajendra; Toal, Martin; Bassil, Anna K.; Bernard, Sharon G.; Davis, Robert P.; Gibson, Adele; Maller, N. Claire; Sharp, Catriona; Tough, David F.; Prinjha, Rab K.; Lewis, Huw D. Share Save
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Essential Bromodomain TcBDF2 as a Drug Target against Chagas Disease Pezza, Alejandro; Tavernelli, Luis E.; Alonso, Victoria L.; Perdomo, Virginia; Gabarro, Raquel; Prinjha, Rab; Rodriguez Araya, Elvio; Rioja, Inmaculada; Docampo, Roberto; Calderon, Felix; Martin, Julio; Serra, Esteban Share Save
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