CD4 mimics targeting the mechanism of HIV entry.
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.
Yamada
Yuko
Y
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
Ochiai
Chihiro
C
Yoshimura
Kazuhisa
K
Tanaka
Tomohiro
T
Ohashi
Nami
N
Narumi
Tetsuo
T
Nomura
Wataru
W
Harada
Shigeyoshi
S
Matsushita
Shuzo
S
Tamamura
Hirokazu
H
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001665:Binding Sites; D015704:CD4 Antigens / Q000737:chemistry* / Q000378:metabolism; D002460:Cell Line; D015699:HIV Envelope Protein gp120 / Q000737:chemistry* / Q000378:metabolism; D023581:HIV Fusion Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D019718:Receptors, CXCR4 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
D019380:Anti-HIV Agents; D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D023581:HIV Fusion Inhibitors; D019718:Receptors, CXCR4