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Issue 15, 2012
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Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors

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Abstract

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.

Graphical abstract: Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors

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Article information


Submitted
18 Dec 2011
Accepted
31 Jan 2012
First published
01 Feb 2012

Org. Biomol. Chem., 2012,10, 2928-2933
Article type
Communication

Relaxation of the rigid backbone of an oligoamide-foldamer-based α-helix mimetic: identification of potent Bcl-xL inhibitors

J. L. Yap, X. Cao, K. Vanommeslaeghe, K. Jung, C. Peddaboina, P. T. Wilder, A. Nan, A. D. MacKerell, W. R. Smythe and S. Fletcher, Org. Biomol. Chem., 2012, 10, 2928
DOI: 10.1039/C2OB07125H

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