Document Detail


CD4 mimics targeting the mechanism of HIV entry.
MedLine Citation:
PMID:  19926478     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Yuko Yamada; Chihiro Ochiai; Kazuhisa Yoshimura; Tomohiro Tanaka; Nami Ohashi; Tetsuo Narumi; Wataru Nomura; Shigeyoshi Harada; Shuzo Matsushita; Hirokazu Tamamura
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-11-04
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Jan 
Date Detail:
Created Date:  2010-02-03     Completed Date:  2010-05-06     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  354-8     Citation Subset:  IM    
Copyright Information:
Copyright 2009 Elsevier Ltd. All rights reserved.
Affiliation:
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
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MeSH Terms
Descriptor/Qualifier:
Anti-HIV Agents / chemical synthesis,  chemistry*,  pharmacology
Antigens, CD4 / chemistry*,  metabolism
Binding Sites
Cell Line
HIV Envelope Protein gp120 / chemistry*,  metabolism
HIV Fusion Inhibitors / chemical synthesis,  chemistry*,  pharmacology
Humans
Receptors, CXCR4 / antagonists & inhibitors,  metabolism
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Anti-HIV Agents; 0/Antigens, CD4; 0/HIV Envelope Protein gp120; 0/HIV Fusion Inhibitors; 0/Receptors, CXCR4

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