Saturday, September 17, 2016

Covalent inhibitors that target lysine side chains

Inhibition of Mcl-1 through covalent modification of a noncatalytic lysine side chain

Gizem Akçay, Matthew A Belmonte, Brian Aquila, Claudio Chuaqui, Alexander W Hird, Michelle L Lamb, Philip B Rawlins, Nancy Su, Sharon Tentarelli, Neil P Grimster & Qibin Su

Nature Chemical Biology (2016) doi:10.1038/nchembio.2174
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Discovery and Optimization of a WRN Helicase Inhibitor Series through Structure-Guided Drug Design from a Covalent Fragment Binding Insight

Momar Toure * ; Xin Cindy Yan; Yonghong Bai; Brian A. Sosa-Alvarado; Cen Gao; Theresa Baker; Erin Brophy; John R. Butler; Yuchen Yuan; Micha...