Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 1, Pages 354-358Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.10.098
Keywords
CD4 mimic; HIV entry; Synergistic effect; CXCR4
Categories
Funding
- Mitsui Life Social Welfare Foundation
- Ministry of Education, Culture, Sports, Science, and Technology of Japan
- Japanese Ministry of Health, Labor, and Welfare
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A structure-activity relationship study was conducted of several CD4 mimicking small molecules which block the interaction between HIV-1 gp120 and CD4. These CD4 mimics induce a conformational change in gp120, exposing its co-receptor-binding site. This induces a highly synergistic interaction in the use in combination with a co-receptor CXCR4 antagonist and reveals a pronounced effect on the dynamic supramolecular mechanism of HIV-1 entry. (C) 2009 Elsevier Ltd. All rights reserved.
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