Journal
ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 15, Pages 2928-2933Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob07125h
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Funding
- University of Maryland School of Pharmacy
- University of Maryland Computer-Aided Drug Design Center
- American Association of Colleges of Pharmacy (AACP) New Pharmacy Faculty
- NSF [CHE-0823198]
- Center for Biomolecular Therapeutics
- University of Maryland School of Medicine
- Institute for Bioscience and Biotechnology Research
- Division Of Chemistry [0823198] Funding Source: National Science Foundation
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By conducting a structure-activity relationship study of the backbone of a series of oligoamide-foldamer-based alpha-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 IC50 values against the proliferation of several Bcl-x(L)-overexpressing cancer cell lines.
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