1373319-39-1Relevant articles and documents
Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: Identification of potent Bcl-xL inhibitors
Yap, Jeremy L.,Cao, Xiaobo,Vanommeslaeghe, Kenno,Jung, Kwan-Young,Peddaboina, Chander,Wilder, Paul T.,Nan, Anjan,MacKerell, Alexander D.,Smythe, W. Roy,Fletcher, Steven
, p. 2928 - 2933 (2012/05/07)
By conducting a structure-activity relationship study of the backbone of a series of oligoamide-foldamer-based α-helix mimetics of the Bak BH3 helix, we have identified especially potent inhibitors of Bcl-xL. The most potent compound has a Ki value of 94 nM in vitro, and single-digit micromolar IC50 values against the proliferation of several Bcl-xL-overexpressing cancer cell lines. The Royal Society of Chemistry 2012.