Chemical Biology of Lysine Demethylases

por Heightman, Tom D
Publicado 2011

Protein Degradation by In-Cell Self-Assembly of Proteolysis Targeting Chimeras

por Lebraud, Honorine, Wright, David J., Johnson, Christopher N., Heightman, Tom D.
Publicado 2016

Enabling synthesis in fragment-based drug discovery by reactivity mapping: photoredox-mediated cross-dehydrogenative heteroarylation of cyclic amines

por Grainger, Rachel, Heightman, Tom D., Ley, Steven V., Lima, Fabio, Johnson, Christopher N.
Publicado 2018

Fragment-based drug discovery: opportunities for organic synthesis

por St. Denis, Jeffrey D., Hall, Richard J., Murray, Christopher W., Heightman, Tom D., Rees, David C.
Publicado 2020

Quantitation of ERK1/2 inhibitor cellular target occupancies with a reversible slow off-rate probe

por Lebraud, Honorine, Surova, Olga, Courtin, Aurélie, O'Reilly, Marc, Valenzano, Chiara R., Nordlund, Pär, Heightman, Tom D.
Publicado 2018

High-Affinity Inhibitors of Human NAD(+)-Dependent 15-Hydroxyprostaglandin Dehydrogenase: Mechanisms of Inhibition and Structure-Activity Relationships

por Niesen, Frank H., Schultz, Lena, Jadhav, Ajit, Bhatia, Chitra, Guo, Kunde, Maloney, David J., Pilka, Ewa S., Wang, Minghua, Oppermann, Udo, Heightman, Tom D., Simeonov, Anton
Publicado 2010

Synthesis and Biological Evaluation of JAHAs: Ferrocene-Based Histone Deacetylase Inhibitors

por Spencer, John, Amin, Jahangir, Wang, Minghua, Packham, Graham, Alwi, Sharifah S. Syed, Tizzard, Graham J., Coles, Simon J., Paranal, Ronald M., Bradner, James E., Heightman, Tom D.
Publicado 2011

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

por 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.
Publicado 2011

Isoxazole‐Derived Amino Acids are Bromodomain‐Binding Acetyl‐Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3

por Sekirnik (née Measures), Angelina R., Hewings, David S., Theodoulou, Natalie H., Jursins, Lukass, Lewendon, Katie R., Jennings, Laura E., Rooney, Timothy P. C., Heightman, Tom D., Conway, Stuart J.
Publicado 2016

Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors

por King, Oliver N. F., Li, Xuan Shirley, Sakurai, Masaaki, Kawamura, Akane, Rose, Nathan R., Ng, Stanley S., Quinn, Amy M., Rai, Ganesha, Mott, Bryan T., Beswick, Paul, Klose, Robert J., Oppermann, Udo, Jadhav, Ajit, Heightman, Tom D., Maloney, David J., Schofield, Christopher J., Simeonov, Anton
Publicado 2010

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

por 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
Publicado 2014

Selective inhibition of BET bromodomains

por Filippakopoulos, Panagis, Qi, Jun, Picaud, Sarah, Shen, Yao, Smith, William B., Fedorov, Oleg, Morse, Elizabeth M., Keates, Tracey, Hickman, Tyler T., Felletar, Ildiko, Philpott, Martin, Munro, Shonagh, McKeown, Michael R., Wang, Yuchuan, Christie, Amanda L., West, Nathan, Cameron, Michael J., Schwartz, Brian, Heightman, Tom D., La Thangue, Nicholas, French, Christopher A., Wiest, Olaf, Kung, Andrew L., Knapp, Stefan, Bradner, James E.
Publicado 2010