CD4 mimics targeting the mechanism of HIV entry

CD4 mimic small molecules interacting with a large cavity of HIV-1 gp120, which are targeted for the dynamic supramolecular mechanism of HIV entry, are reported. A structure–activity relationship study was conducted of several CD4 mimicking small molecules which block the interaction between HIV-1 g...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010, Vol.20 (1), p.354-358
Main Authors: Yamada, Yuko, Ochiai, Chihiro, Yoshimura, Kazuhisa, Tanaka, Tomohiro, Ohashi, Nami, Narumi, Tetsuo, Nomura, Wataru, Harada, Shigeyoshi, Matsushita, Shuzo, Tamamura, Hirokazu
Format: Article
Language:English
Subjects:
Anti-HIV Agents - chemical synthesis
Anti-HIV Agents - chemistry
Anti-HIV Agents - pharmacology
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiviral agents
Binding Sites
Biological and medical sciences
CD4 Antigens - chemistry
CD4 Antigens - metabolism
CD4 mimic
Cell Line
CXCR4
HIV entry
HIV Envelope Protein gp120 - chemistry
HIV Envelope Protein gp120 - metabolism
HIV Fusion Inhibitors - chemical synthesis
HIV Fusion Inhibitors - chemistry
HIV Fusion Inhibitors - pharmacology
Human immunodeficiency virus 1
Humans
Medical sciences
Pharmacology. Drug treatments
Receptors, CXCR4 - antagonists & inhibitors
Receptors, CXCR4 - metabolism
Structure-Activity Relationship
Synergistic effect
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Summary:CD4 mimic small molecules interacting with a large cavity of HIV-1 gp120, which are targeted for the dynamic supramolecular mechanism of HIV entry, are reported. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.10.098