- Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.
Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors.
Organic & biomolecular chemistry (2012-03-08)
Jeremy L Yap, Xiaobo Cao, Kenno Vanommeslaeghe, Kwan-Young Jung, Chander Peddaboina, Paul T Wilder, Anjan Nan, Alexander D MacKerell, W Roy Smythe, Steven Fletcher
PMID22395339
摘要
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-x(L). The most potent compound has a K(i) value of 94 nM in vitro, and single-digit micromolar IC(50) values against the proliferation of several Bcl-x(L)-overexpressing cancer cell lines.
材料