SPOTing Acetyl-Lysine Dependent Interactions

by Picaud, Sarah, Filippakopoulos, Panagis
Published 2015

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

by Filippakopoulos, Panagis, Picaud, Sarah, Fedorov, Oleg, Keller, Marco, Wrobel, Matthias, Morgenstern, Olaf, Bracher, Franz, Knapp, Stefan
Published 2012

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding

by Kempen, Herman J, Bellus, Daniel, Fedorov, Oleg, Nicklisch, Silke, Filippakopoulos, Panagis, Picaud, Sarah, Knapp, Stefan
Published 2013

Structural basis of fumarate hydratase deficiency

by Picaud, Sarah, Kavanagh, Kathryn L., Yue, Wyatt W., Lee, Wen Hwa, Muller-Knapp, Susanne, Gileadi, Opher, Sacchettini, James, Oppermann, Udo
Published 2011

3,5-Dimethylisoxazoles Act As Acetyl-lysine-mimetic Bromodomain Ligands

by 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 2011

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

by Vidler, Lewis R., Filippakopoulos, Panagis, Fedorov, Oleg, Picaud, Sarah, Martin, Sarah, Tomsett, Michael, Woodward, Hannah, Brown, Nathan, Knapp, Stefan, Hoelder, Swen
Published 2013

9H-Purine Scaffold Reveals Induced-Fit Pocket Plasticity of the BRD9 Bromodomain

by Picaud, Sarah, Strocchia, Maria, Terracciano, Stefania, Lauro, Gianluigi, Mendez, Jacqui, Daniels, Danette L., Riccio, Raffaele, Bifulco, Giuseppe, Bruno, Ines, Filippakopoulos, Panagis
Published 2015

Histone Recognition and Large-Scale Structural Analysis of the Human Bromodomain Family

by 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 2012

Small-Molecule Inhibition of BRDT for Male Contraception

by Matzuk, Martin M., McKeown, Michael R., Filippakopoulos, Panagis, Li, Qinglei, Ma, Lang, Agno, Julio E., Lemieux, Madeleine E., Picaud, Sarah, Yu, Richard N., Qi, Jun, Knapp, Stefan, Bradner, James E.
Published 2012

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains

by Fedorov, Oleg, Lingard, Hannah, Wells, Chris, Monteiro, Octovia P., Picaud, Sarah, Keates, Tracy, Yapp, Clarence, Philpott, Martin, Martin, Sarah J., Felletar, Ildiko, Marsden, Brian D., Filippakopoulos, Panagis, Müller, Susanne, Knapp, Stefan, Brennan, Paul E.
Published 2013

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

by 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 2014

Multivalent Histone and DNA Engagement by a PHD/BRD/PWWP Triple Reader Cassette Recruits ZMYND8 to K14ac-Rich Chromatin

by Savitsky, Pavel, Krojer, Tobias, Fujisawa, Takao, Lambert, Jean-Philippe, Picaud, Sarah, Wang, Chen-Yi, Shanle, Erin K., Krajewski, Krzysztof, Friedrichsen, Hans, Kanapin, Alexander, Goding, Colin, Schapira, Matthieu, Samsonova, Anastasia, Strahl, Brian D., Gingras, Anne-Claude, Filippakopoulos, Panagis
Published 2016

Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory response

by Ghari, Fatemeh, Quirke, Anne-Marie, Munro, Shonagh, Kawalkowska, Joanna, Picaud, Sarah, McGouran, Joanna, Subramanian, Venkataraman, Muth, Aaron, Williams, Richard, Kessler, Benedikt, Thompson, Paul R., Fillipakopoulos, Panagis, Knapp, Stefan, Venables, Patrick J., La Thangue, Nicholas B.
Published 2016

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

by 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 2013

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

by 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 2012

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia

by Picaud, Sarah, Leonards, Katharina, Lambert, Jean-Philippe, Dovey, Oliver, Wells, Christopher, Fedorov, Oleg, Monteiro, Octovia, Fujisawa, Takao, Wang, Chen-Yi, Lingard, Hannah, Tallant, Cynthia, Nikbin, Nikzad, Guetzoyan, Lucie, Ingham, Richard, Ley, Steven V., Brennan, Paul, Muller, Susanne, Samsonova, Anastasia, Gingras, Anne-Claude, Schwaller, Juerg, Vassiliou, George, Knapp, Stefan, Filippakopoulos, Panagis
Published 2016

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

by Fedorov, Oleg, Castex, Josefina, Tallant, Cynthia, Owen, Dafydd R., Martin, Sarah, Aldeghi, Matteo, Monteiro, Octovia, Filippakopoulos, Panagis, Picaud, Sarah, Trzupek, John D., Gerstenberger, Brian S., Bountra, Chas, Willmann, Dominica, Wells, Christopher, Philpott, Martin, Rogers, Catherine, Biggin, Philip C., Brennan, Paul E., Bunnage, Mark E., Schüle, Roland, Günther, Thomas, Knapp, Stefan, Müller, Susanne
Published 2015

Discovery and Optimization of Small-Molecule Ligands for the CBP/p300 Bromodomains

by 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 2014

A Series of Potent CREBBP Bromodomain Ligands Reveals an Induced-Fit Pocket Stabilized by a Cation–π Interaction**

by Rooney, Timothy P C, Filippakopoulos, Panagis, Fedorov, Oleg, Picaud, Sarah, Cortopassi, Wilian A, Hay, Duncan A, Martin, Sarah, Tumber, Anthony, Rogers, Catherine M, Philpott, Martin, Wang, Minghua, Thompson, Amber L, Heightman, Tom D, Pryde, David C, Cook, Andrew, Paton, Robert S, Müller, Susanne, Knapp, Stefan, Brennan, Paul E, Conway, Stuart J
Published 2014