Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family
Filippakopoulos, Panagis, Picaud, Sarah, Mangos, Maria, Keates, Tracy, Lambert, Jean-Philippe, Barsyte-Lovejoy, Dalia, Felletar, Ildiko, Volkmer, Rudolf, Müller, Susanne, Pawson, Tony, Gingras, Anne-Claude, Arrowsmith, Cheryl H., Knapp, Stefan
Published in Cell (30.03.2012)
Published in Cell (30.03.2012)
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Journal Article
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
Picaud, Sarah, Wells, Christopher, Felletar, Ildiko, Brotherton, Deborah, Martin, Sarah, Savitsky, Pavel, Diez-Dacal, Beatriz, Philpott, Martin, Bountra, Chas, Lingard, Hannah, Fedorov, Oleg, Müller, Susanne, Brennan, Paul E., Knapp, Stefan, Filippakopoulos, Panagis
Published in Proceedings of the National Academy of Sciences - PNAS (03.12.2013)
Published in Proceedings of the National Academy of Sciences - PNAS (03.12.2013)
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Journal Article
A TFEB nuclear export signal integrates amino acid supply and glucose availability
Li, Linxin, Friedrichsen, Hans J, Andrews, Sarah, Picaud, Sarah, Volpon, Laurent, Ngeow, Kaochin, Berridge, Georgina, Fischer, Roman, Borden, Katherine L B, Filippakopoulos, Panagis, Goding, Colin R
Published in Nature communications (11.07.2018)
Published in Nature communications (11.07.2018)
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Journal Article
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology
Ciceri, Pietro, Müller, Susanne, O'Mahony, Alison, Fedorov, Oleg, Filippakopoulos, Panagis, Hunt, Jeremy P, Lasater, Elisabeth A, Pallares, Gabriel, Picaud, Sarah, Wells, Christopher, Martin, Sarah, Wodicka, Lisa M, Shah, Neil P, Treiber, Daniel K, Knapp, Stefan
Published in Nature chemical biology (01.04.2014)
Published in Nature chemical biology (01.04.2014)
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Journal Article
Interactome Rewiring Following Pharmacological Targeting of BET Bromodomains
Lambert, Jean-Philippe, Picaud, Sarah, Fujisawa, Takao, Hou, Huayun, Savitsky, Pavel, Uusküla-Reimand, Liis, Gupta, Gagan D., Abdouni, Hala, Lin, Zhen-Yuan, Tucholska, Monika, Knight, James D.R., Gonzalez-Badillo, Beatriz, St-Denis, Nicole, Newman, Joseph A., Stucki, Manuel, Pelletier, Laurence, Bandeira, Nuno, Wilson, Michael D., Filippakopoulos, Panagis, Gingras, Anne-Claude
Published in Molecular cell (07.02.2019)
Published in Molecular cell (07.02.2019)
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Journal Article
Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy
Picaud, Sarah, Fedorov, Oleg, Thanasopoulou, Angeliki, Leonards, Katharina, Jones, Katherine, Meier, Julia, Olzscha, Heidi, Monteiro, Octovia, Martin, Sarah, Philpott, Martin, Tumber, Anthony, Filippakopoulos, Panagis, Yapp, Clarence, Wells, Christopher, Che, Ka Hing, Bannister, Andrew, Robson, Samuel, Kumar, Umesh, Parr, Nigel, Lee, Kevin, Lugo, Dave, Jeffrey, Philip, Taylor, Simon, Vecellio, Matteo L, Bountra, Chas, Brennan, Paul E, O'Mahony, Alison, Velichko, Sharlene, Müller, Susanne, Hay, Duncan, Daniels, Danette L, Urh, Marjeta, La Thangue, Nicholas B, Kouzarides, Tony, Prinjha, Rab, Schwaller, Jürg, Knapp, Stefan
Published in Cancer research (Chicago, Ill.) (01.12.2015)
Published in Cancer research (Chicago, Ill.) (01.12.2015)
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Journal Article
3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands
Hewings, David S, Wang, Minghua, Philpott, Martin, Fedorov, Oleg, Uttarkar, Sagar, Filippakopoulos, Panagis, Picaud, Sarah, Vuppusetty, Chaitanya, Marsden, Brian, Knapp, Stefan, Conway, Stuart J, Heightman, Tom D
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Journal Article
Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains
Hay, Duncan A, Fedorov, Oleg, Martin, Sarah, Singleton, Dean C, Tallant, Cynthia, Wells, Christopher, Picaud, Sarah, Philpott, Martin, Monteiro, Octovia P, Rogers, Catherine M, Conway, Stuart J, Rooney, Timothy P. C, Tumber, Anthony, Yapp, Clarence, Filippakopoulos, Panagis, Bunnage, Mark E, Müller, Susanne, Knapp, Stefan, Schofield, Christopher J, Brennan, Paul E
Published in Journal of the American Chemical Society (02.07.2014)
Published in Journal of the American Chemical Society (02.07.2014)
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Journal Article
PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains
PICAUD, Sarah, DA COSTA, David, BRADNER, James E, TANIERE, Philippe, O'SULLIVAN, Brendan, MÜLLER, Susanne, SCHWALLER, Juerg, STANKOVIC, Tatjana, KNAPP, Stefan, THANASOPOULOU, Angeliki, FILIPPAKOPOULOS, Panagis, FISH, Paul V, PHILPOTT, Martin, FEDOROV, Oleg, BRENNAN, Paul, BUNNAGE, Mark E, OWEN, Dafydd R
Published in Cancer research (Chicago, Ill.) (01.06.2013)
Published in Cancer research (Chicago, Ill.) (01.06.2013)
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Journal Article
Development and preclinical validation of a novel covalent ubiquitin receptor Rpn13 degrader in multiple myeloma
Song, Yan, Park, Paul M C, Wu, Lei, Ray, Arghya, Picaud, Sarah, Li, Deyao, Wimalasena, Virangika K, Du, Ting, Filippakopoulos, Panagis, Anderson, Kenneth C, Qi, Jun, Chauhan, Dharminder
Published in Leukemia (01.11.2019)
Published in Leukemia (01.11.2019)
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Journal Article
Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening
Vidler, Lewis R, Filippakopoulos, Panagis, Fedorov, Oleg, Picaud, Sarah, Martin, Sarah, Tomsett, Michael, Woodward, Hannah, Brown, Nathan, Knapp, Stefan, Hoelder, Swen
Published in Journal of medicinal chemistry (24.10.2013)
Published in Journal of medicinal chemistry (24.10.2013)
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Journal Article
Acetylation reprograms MITF target selectivity and residence time
Louphrasitthiphol, Pakavarin, Loffreda, Alessia, Pogenberg, Vivian, Picaud, Sarah, Schepsky, Alexander, Friedrichsen, Hans, Zeng, Zhiqiang, Lashgari, Anahita, Thomas, Benjamin, Patton, E Elizabeth, Wilmanns, Matthias, Filippakopoulos, Panagis, Lambert, Jean-Philippe, Steingrímsson, Eiríkur, Mazza, Davide, Goding, Colin R
Published in Nature communications (28.09.2023)
Published in Nature communications (28.09.2023)
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Journal Article
Identification of a Chemical Probe for Bromo and Extra C‑Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit
Fish, Paul V, Filippakopoulos, Panagis, Bish, Gerwyn, Brennan, Paul E, Bunnage, Mark E, Cook, Andrew S, Federov, Oleg, Gerstenberger, Brian S, Jones, Hannah, Knapp, Stefan, Marsden, Brian, Nocka, Karl, Owen, Dafydd R, Philpott, Martin, Picaud, Sarah, Primiano, Michael J, Ralph, Michael J, Sciammetta, Nunzio, Trzupek, John D
Published in Journal of medicinal chemistry (26.11.2012)
Published in Journal of medicinal chemistry (26.11.2012)
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Journal Article
MOB1 Mediated Phospho-recognition in the Core Mammalian Hippo Pathway
Couzens, Amber L., Xiong, Shawn, Knight, James D.R., Mao, Daniel Y., Guettler, Sebastian, Picaud, Sarah, Kurinov, Igor, Filippakopoulos, Panagis, Sicheri, Frank, Gingras, Anne-Claude
Published in Molecular & cellular proteomics (01.06.2017)
Published in Molecular & cellular proteomics (01.06.2017)
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Journal Article
Nut Directs p300-Dependent, Genome-Wide H4 Hyperacetylation in Male Germ Cells
Shiota, Hitoshi, Barral, Sophie, Buchou, Thierry, Tan, Minjia, Couté, Yohann, Charbonnier, Guillaume, Reynoird, Nicolas, Boussouar, Fayçal, Gérard, Matthieu, Zhu, Mingrui, Bargier, Lisa, Puthier, Denis, Chuffart, Florent, Bourova-Flin, Ekaterina, Picaud, Sarah, Filippakopoulos, Panagis, Goudarzi, Afsaneh, Ibrahim, Ziad, Panne, Daniel, Rousseaux, Sophie, Zhao, Yingming, Khochbin, Saadi
Published in Cell reports (Cambridge) (25.09.2018)
Published in Cell reports (Cambridge) (25.09.2018)
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Journal Article
Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands
Hewings, David S, Fedorov, Oleg, Filippakopoulos, Panagis, Martin, Sarah, Picaud, Sarah, Tumber, Anthony, Wells, Christopher, Olcina, Monica M, Freeman, Katherine, Gill, Andrew, Ritchie, Alison J, Sheppard, David W, Russell, Angela J, Hammond, Ester M, Knapp, Stefan, Brennan, Paul E, Conway, Stuart J
Published in Journal of medicinal chemistry (25.04.2013)
Published in Journal of medicinal chemistry (25.04.2013)
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Journal Article
Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit
Gerstenberger, Brian S, Trzupek, John D, Tallant, Cynthia, Fedorov, Oleg, Filippakopoulos, Panagis, Brennan, Paul E, Fedele, Vita, Martin, Sarah, Picaud, Sarah, Rogers, Catherine, Parikh, Mihir, Taylor, Alexandria, Samas, Brian, O’Mahony, Alison, Berg, Ellen, Pallares, Gabriel, Torrey, Adam D, Treiber, Daniel K, Samardjiev, Ivan J, Nasipak, Brian T, Padilla-Benavides, Teresita, Wu, Qiong, Imbalzano, Anthony N, Nickerson, Jeffrey A, Bunnage, Mark E, Müller, Susanne, Knapp, Stefan, Owen, Dafydd R
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
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Journal Article
9H‑Purine Scaffold Reveals Induced-Fit Pocket Plasticity of the BRD9 Bromodomain
Picaud, Sarah, Strocchia, Maria, Terracciano, Stefania, Lauro, Gianluigi, Mendez, Jacqui, Daniels, Danette L, Riccio, Raffaele, Bifulco, Giuseppe, Bruno, Ines, Filippakopoulos, Panagis
Published in Journal of medicinal chemistry (26.03.2015)
Published in Journal of medicinal chemistry (26.03.2015)
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Journal Article
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain
Brand, Michael, Clayton, James, Moroglu, Mustafa, Schiedel, Matthias, Picaud, Sarah, Bluck, Joseph P, Skwarska, Anna, Bolland, Hannah, Chan, Anthony K. N, Laurin, Corentine M. C, Scorah, Amy R, See, Larissa, Rooney, Timothy P. C, Andrews, Katrina H, Fedorov, Oleg, Perell, Gabriella, Kalra, Prakriti, Vinh, Kayla B, Cortopassi, Wilian A, Heitel, Pascal, Christensen, Kirsten E, Cooper, Richard I, Paton, Robert S, Pomerantz, William C. K, Biggin, Philip C, Hammond, Ester M, Filippakopoulos, Panagis, Conway, Stuart J
Published in Journal of medicinal chemistry (22.07.2021)
Published in Journal of medicinal chemistry (22.07.2021)
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Journal Article
A Tail-Based Mechanism Drives Nucleosome Demethylation by the LSD2/NPAC Multimeric Complex
Marabelli, Chiara, Marrocco, Biagina, Pilotto, Simona, Chittori, Sagar, Picaud, Sarah, Marchese, Sara, Ciossani, Giuseppe, Forneris, Federico, Filippakopoulos, Panagis, Schoehn, Guy, Rhodes, Daniela, Subramaniam, Sriram, Mattevi, Andrea
Published in Cell reports (Cambridge) (09.04.2019)
Published in Cell reports (Cambridge) (09.04.2019)
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Journal Article