Chemical Biology of Lysine Demethylases

Por Heightman, Tom D
Publicado em 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 no ACS Cent Sci (2016)

Nonenzymatic biotinylation of histone H2A

Por Healy, Shannon, Heightman, Tom D, Hohmann, Laura, Schriemer, David, Gravel, Roy A
Publicado em 2009

Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates

Por Thalhammer, Armin, Mecinović, Jasmin, Loenarz, Christoph, Tumber, Anthony, Rose, Nathan R., Heightman, Tom D., Schofield, Christopher J.
Publicado no Org Biomol Chem (2010)

WHSC1 links transcription elongation to HIRA-mediated histone H3.3 deposition

Por Sarai, Naoyuki, Nimura, Keisuke, Tamura, Tomohiko, Kanno, Tomohiko, Patel, Mira C, Heightman, Tom D, Ura, Kiyoe, Ozato, Keiko
Publicado em 2013

BRD4 Coordinates Recruitment of Pause Release Factor P-TEFb and the Pausing Complex NELF/DSIF To Regulate Transcription Elongation of Interferon-Stimulated Genes

Por Patel, Mira C., Debrosse, Maxime, Smith, Matthew, Dey, Anup, Huynh, Walter, Sarai, Naoyuki, Heightman, Tom D., Tamura, Tomohiko, Ozato, Keiko
Publicado em 2013

Development of homogeneous luminescence assays for histone demethylase catalysis and binding

Por Kawamura, Akane, Tumber, Anthony, Rose, Nathan R., King, Oliver N. F., Daniel, Michelle, Oppermann, Udo, Heightman, Tom D., Schofield, Christopher
Publicado no Anal Biochem (2010)

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 em 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 em 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 em 2011

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

Por Ferguson, Fleur M., Fedorov, Oleg, Chaikuad, Apirat, Philpott, Martin, Muniz, Joao R. C., Felletar, Ildiko, von Delft, Frank, Heightman, Tom, Knapp, Stefan, Abell, Chris, Ciulli, Alessio
Publicado em 2013

Inhibition of Histone Demethylases by 4-Carboxy-2,2′-Bipyridyl Compounds

Por Chang, Kai-Hsuan, King, Oliver N.F., Tumber, Anthony, Woon, Esther C.Y., Heightman, Tom D., McDonough, Michael A., Schofield, Christopher J., Rose, Nathan R.
Publicado no ChemMedChem (2011)

A Selective Inhibitor and Probe of the Cellular Functions of Jumonji C Domain-Containing Histone Demethylases

Por Luo, Xuelai, Liu, Yongxiang, Kubicek, Stefan, Myllyharju, Johanna, Tumber, Anthony, Ng, Stanley, Che, Ka Hing, Podoll, Jessica, Heightman, Tom D., Oppermann, Udo, Schreiber, Stuart L., Wang, Xiang
Publicado em 2011

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

Por Hay, Duncan, Fedorov, Oleg, Filippakopoulos, Panagis, Martin, Sarah, Philpott, Martin, Picaud, Sarah, Hewings, David S., Uttakar, Sagar, Heightman, Tom D., Conway, Stuart J., Knapp, Stefan, Brennan, Paul E.
Publicado no Medchemcomm (2013)

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 no Angew Chem Int Ed Engl (2016)

BRD4 assists elongation of both coding and enhancer RNAs guided by histone acetylation

Por Kanno, Tomohiko, Kanno, Yuka, LeRoy, Gary, Campos, Eric, Sun, Hong-Wei, Brooks, Stephen R, Vahedi, Golnaz, Heightman, Tom D, Garcia, Benjamin A, Reinberg, Danny, Siebenlist, Ulrich, O’Shea, John J, Ozato, Keiko
Publicado no Nat Struct Mol Biol (2014)

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 em 2010

Fragment-Based Discovery of 6-Azaindazoles As Inhibitors of Bacterial DNA Ligase

Por Howard, Steven, Amin, Nader, Benowitz, Andrew B., Chiarparin, Elisabetta, Cui, Haifeng, Deng, Xiaodong, Heightman, Tom D., Holmes, David J., Hopkins, Anna, Huang, Jianzhong, Jin, Qi, Kreatsoulas, Constantine, Martin, Agnes C. L., Massey, Frances, McCloskey, Lynn, Mortenson, Paul N., Pathuri, Puja, Tisi, Dominic, Williams, Pamela A.
Publicado em 2013

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 no Angew Chem Int Ed Engl (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 em 2010