Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer

Autor: Sharma, Shikhar, Chung, Chi-Yeh, Uryu, Sean, Petrovic, Jelena, Cao, Joan, Rickard, Amanda, Nady, Nataliya, Greasley, Samantha, Johnson, Eric, Brodsky, Oleg, Khan, Showkhin, Wang, Hui, Wang, Zhenxiong, Zhang, Yong, Tsaparikos, Konstantinos, Chen, Lei, Mazurek, Anthony, Lapek, John, Kung, Pei-Pei, Sutton, Scott, Richardson, Paul F., Greenwald, Eric C., Yamazaki, Shinji, Jones, Rhys, Maegley, Karen A., Bingham, Patrick, Lam, Hieu, Stupple, Alexandra E., Kamal, Aileen, Chueh, Anderly, Cuzzupe, Anthony, Morrow, Benjamin J., Ren, Bin, Carrasco-Pozo, Catalina, Tan, Chin Wee, Bhuva, Dharmesh D., Allan, Elizabeth, Surgenor, Elliot, Vaillant, François, Pehlivanoglu, Havva, Falk, Hendrik, Whittle, James R., Newman, Janet, Cursons, Joseph, Doherty, Judy P., White, Karen L., MacPherson, Laura, Devlin, Mark, Dennis, Matthew L., Hattarki, Meghan K., De Silva, Melanie, Camerino, Michelle A., Butler, Miriam S., Dolezal, Olan, Pilling, Patricia, Foitzik, Richard, Stupple, Paul A., Lagiakos, H. Rachel, Walker, Scott R., Hediyeh-Zadeh, Soroor, Nuttall, Stewart, Spall, Sukhdeep K., Charman, Susan A., Connor, Theresa, Peat, Thomas S., Avery, Vicky M., Bozikis, Ylva E., Yang, Yuqing, Zhang, Ming, Monahan, Brendon J., Voss, Anne K., Thomas, Tim, Street, Ian P., Dawson, Sarah-Jane, Dawson, Mark A., Lindeman, Geoffrey J., Davis, Melissa J., Visvader, Jane E., Paul, Thomas A.

Publikováno v: In Cell Chemical Biology 19 October 2023 30(10):1191-1210

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Fragment screening for a protein-protein interaction inhibitor to WDR5

Autor: Matthew L. Dennis, Benjamin J. Morrow, Olan Dolezal, Anthony N. Cuzzupe, Alexandra E. Stupple, Janet Newman, John Bentley, Meghan Hattarki, Stewart D. Nuttall, Richard C. Foitzik, Ian P. Street, Paul A. Stupple, Brendon J. Monahan, Thomas. S. Peat

Publikováno v: Structural Dynamics, Vol 6, Iss 6, Pp 064701-064701-20 (2019)

The WD40-repeat protein WDR5 scaffolds various epigenetic writers and is a critical component of the mammalian SET/MLL histone methyltransferase complex. Dysregulation of the MLL1 catalytic function is associated with mixed-lineage leukemia, and anta

Externí odkaz: https://doaj.org/article/33add36f17f6424bb9dc83aa50562a57

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Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors

Autor: Alexandra L. Garnham, Peter E. Czabotar, Andrew F. Wilks, Stefan P Glaser, Peter Hall, Scott Taylor, Mark A. Dawson, John Thomas Feutrill, Zhen Xu, Carl R. Walkley, Phillip P. Sharp, Kate E. Jarman, Tamas Hatfaludi, Helene Jousset, David J. Segal, Christopher J. Burns, Jean-Marc Garnier, David C.S. Huang, Dean Tyler, Anthony Nicholas Cuzzupe

Publikováno v: ACS Medicinal Chemistry Letters. 8:1298-1303

A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an acetyl-lysine mimetic heterocycle onto the diazepine framework. Herein we describe a straightforw

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f53a8629f367b983d223e262028099ee
https://doi.org/10.1021/acsmedchemlett.7b00389