title: CD4 mimics targeting the mechanism of HIV entry.
abstract: 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.affiliation: Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.
authors.forename: Yuko
authors.initials: Y
authors.lastname: Yamada
authors.forename: Chihiro
authors.initials: C
authors.lastname: Ochiai
authors.forename: Kazuhisa
authors.initials: K
authors.lastname: Yoshimura
authors.forename: Tomohiro
authors.initials: T
authors.lastname: Tanaka
authors.forename: Nami
authors.initials: N
authors.lastname: Ohashi
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Narumi
authors.forename: Wataru
authors.initials: W
authors.lastname: Nomura
authors.forename: Shigeyoshi
authors.initials: S
authors.lastname: Harada
authors.forename: Shuzo
authors.initials: S
authors.lastname: Matsushita
authors.forename: Hirokazu
authors.initials: H
authors.lastname: Tamamura
mesh_terms: 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
chemical_list: D019380:Anti-HIV Agents; D015704:CD4 Antigens; D015699:HIV Envelope Protein gp120; D023581:HIV Fusion Inhibitors; D019718:Receptors, CXCR4