Open access chemical probes for epigenetic targets

by Brown, Peter J, Müller, Susanne
Published 2015

Structure of the Catalytic Domain of EZH2 Reveals Conformational Plasticity in Cofactor and Substrate Binding Sites and Explains Oncogenic Mutations

by Wu, Hong, Zeng, Hong, Dong, Aiping, Li, Fengling, He, Hao, Senisterra, Guillermo, Seitova, Alma, Duan, Shili, Brown, Peter J., Vedadi, Masoud, Arrowsmith, Cheryl H., Schapira, Matthieu
Published 2013

SET9-Mediated Regulation of TGF-β Signaling Links Protein Methylation to Pulmonary Fibrosis

by Elkouris, Maximilianos, Kontaki, Haroula, Stavropoulos, Athanasios, Antonoglou, Anastasia, Nikolaou, Kostas C., Samiotaki, Martina, Szantai, Eszter, Saviolaki, Dimitra, Brown, Peter J., Sideras, Paschalis, Panayotou, George, Talianidis, Iannis
Published 2016

Discovery of a Selective, Substrate-Competitive Inhibitor of the Lysine Methyltransferase SETD8

by Ma, Anqi, Yu, Wenyu, Li, Fengling, Bleich, Rachel M., Herold, J. Martin, Butler, Kyle V., Norris, Jacqueline L., Korboukh, Victoria, Tripathy, Ashutosh, Janzen, William P., Arrowsmith, Cheryl H., Frye, Stephen V., Vedadi, Masoud, Brown, Peter J., Jin, Jian
Published 2014

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential t...

by Agarwal, Prasoon, Alzrigat, Mohammad, Párraga, Alba Atienza, Enroth, Stefan, Singh, Umashankar, Ungerstedt, Johanna, Österborg, Anders, Brown, Peter J., Ma, Anqi, Jin, Jian, Nilsson, Kenneth, Öberg, Fredrik, Kalushkova, Antonia, Jernberg-Wiklund, Helena
Published 2016

Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5

by Senisterra, Guillermo, Wu, Hong, Allali-Hassani, Abdellah, Wasney, Gregory A., Barsyte-Lovejoy, Dalia, Dombrovski, Ludmila, Dong, Aiping, Nguyen, Kong T., Smil, David, Bolshan, Yuri, Hajian, Taraneh, He, Hao, Seitova, Alma, Chau, Irene, Li, Fengling, Poda, Gennadiy, Couture, Jean-François, Brown, Peter J., Al-Awar, Rima, Schapira, Matthieu, Arrowsmith, Cheryl H., Vedadi, Masoud
Published 2012

Discovery of a chemical probe for the L3MBTL3 methyl-lysine reader domain

by James, Lindsey I., Barsyte-Lovejoy, Dalia, Zhong, Nan, Krichevsky, Liubov, Korboukh, Victoria K., Herold, Martin J., MacNevin, Christopher J., Norris, Jacqueline L., Sagum, Cari A., Tempel, Wolfram, Marcon, Edyta, Guo, Hongbo, Gao, Cen, Huang, Xi-Ping, Duan, Shili, Emili, Andrew, Greenblatt, Jack F., Kireev, Dmitri B., Jin, Jian, Janzen, William P., Brown, Peter J., Bedford, Mark T., Arrowsmith, Cheryl H., Frye, Stephen V.
Published 2013

Hemi-methylated DNA regulates DNA methylation inheritance through allosteric activation of H3 ubiquitylation by UHRF1

by Harrison, Joseph S, Cornett, Evan M, Goldfarb, Dennis, DaRosa, Paul A, Li, Zimeng M, Yan, Feng, Dickson, Bradley M, Guo, Angela H, Cantu, Daniel V, Kaustov, Lilia, Brown, Peter J, Arrowsmith, Cheryl H, Erie, Dorothy A, Major, Michael B, Klevit, Rachel E, Krajewski, Krzysztof, Kuhlman, Brian, Strahl, Brian D, Rothbart, Scott B
Published 2016

Discovery and Characterization of a Highly Potent and Selective Aminopyrazoline-Based in Vivo Probe (BAY-598) for the Protein Lysine Methyltransferase SMYD2

by Eggert, Erik, Hillig, Roman C., Koehr, Silke, Stöckigt, Detlef, Weiske, Jörg, Barak, Naomi, Mowat, Jeffrey, Brumby, Thomas, Christ, Clara D., ter Laak, Antonius, Lang, Tina, Fernandez-Montalvan, Amaury E., Badock, Volker, Weinmann, Hilmar, Hartung, Ingo V., Barsyte-Lovejoy, Dalia, Szewczyk, Magdalena, Kennedy, Steven, Li, Fengling, Vedadi, Masoud, Brown, Peter J., Santhakumar, Vijayaratnam, Arrowsmith, Cheryl H., Stellfeld, Timo, Stresemann, Carlo
Published 2016

A cellular chemical probe targeting the chromodomains of Polycomb Repressive Complex 1

by Stuckey, Jacob I, Dickson, Bradley M, Cheng, Nancy, Liu, Yanli, Norris, Jacqueline L, Cholensky, Stephanie H, Tempel, Wolfram, Qin, Su, Huber, Katherine G, Sagum, Cari, Black, Karynne, Li, Fengling, Huang, Xi-Ping, Roth, Bryan L, Baughman, Brandi M, Senisterra, Guillermo, Pattenden, Samantha G, Vedadi, Masoud, Brown, Peter J, Bedford, Mark T, Min, Jinrong, Arrowsmith, Cheryl H, James, Lindsey I, Frye, Stephen V
Published 2016

LLY-507, a Cell-active, Potent, and Selective Inhibitor of Protein-lysine Methyltransferase SMYD2*

by Nguyen, Hannah, Allali-Hassani, Abdellah, Antonysamy, Stephen, Chang, Shawn, Chen, Lisa Hong, Curtis, Carmen, Emtage, Spencer, Fan, Li, Gheyi, Tarun, Li, Fengling, Liu, Shichong, Martin, Joseph R., Mendel, David, Olsen, Jonathan B., Pelletier, Laura, Shatseva, Tatiana, Wu, Song, Zhang, Feiyu Fred, Arrowsmith, Cheryl H., Brown, Peter J., Campbell, Robert M., Garcia, Benjamin A., Barsyte-Lovejoy, Dalia, Mader, Mary, Vedadi, Masoud
Published 2015

Pharmacological targeting of the Wdr5-MLL interaction in C/EBPα N-terminal leukemia

by Grebien, Florian, Vedadi, Masoud, Getlik, Matthäus, Giambruno, Roberto, Grover, Amit, Avellino, Roberto, Skucha, Anna, Vittori, Sarah, Kuznetsova, Ekaterina, Smil, David, Barsyte-Lovejoy, Dalia, Li, Fengling, Poda, Gennadiy, Schapira, Matthieu, Wu, Hong, Dong, Aiping, Senisterra, Guillermo, Stukalov, Alexey, Huber, Kilian V. M., Schönegger, Andreas, Marcellus, Richard, Bilban, Martin, Bock, Christoph, Brown, Peter J., Zuber, Johannes, Bennett, Keiryn L., Al-awar, Rima, Delwel, Ruud, Nerlov, Claus, Arrowsmith, Cheryl H., Superti-Furga, Giulio
Published 2015