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

Sulfinyl Aziridines as Stereoselective Covalent Destabilizing Degraders of the Oncogenic Transcription Factor MYC

H. T. Rosen ,  K. Li ,  C. E. Stieger ,  E. L. Li ,  B. Currier ,  S. M. Brittain ,  F. J. Garcia ,  D. C. Beard ,  M. D. Jones ,  S. Haenni...