期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 8, 页码 2861-2865出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.062
关键词
HIV; gp41; Fusion inhibitors; alpha-Helix mimetics
资金
- National Institutes of Health [CA42056, GM87998, NS59403]
The evaluation of a comprehensive alpha-helix mimetic library for binding the gp41 NHR hydrophobic pocket recognizing an intramolecular CHR alpha-helix provided a detailed depiction of structural features required for binding and led to the discovery of small molecule inhibitors (K-i 0.6-1.3 mu M) that not only match or exceed the potency of those disclosed over the past decade, but that also exhibit effective activity in a cell-cell fusion assay (IC50 5-8 mu M). (C) 2012 Elsevier Ltd. All rights reserved.
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