Design of a Novel HIV-1 Fusion Inhibitor That Displays a Minimal Interface for Binding Affinity

详细信息    查看全文

• 作者：Shinya Oishi ; Saori Ito ; Hiroki Nishikawa ; Kentaro Watanabe ; Michinori Tanaka ; Hiroaki Ohno ; Kazuki Izumi ; Yasuko Sakagami ; Eiichi Kodama ; Masao Matsuoka ; Nobutaka Fujii
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：February 14, 2008
• 年：2008
• 卷：51
• 期：3
• 页码：388 - 391
• 全文大小：440K
• 年卷期：v.51,no.3(February 14, 2008)
• ISSN：1520-4804

文摘

Reported herein are the design, biological activities, and biophysical properties of a novel HIV-1 membrane fusion inhibitor. α-Helix-inducible X-EE-XX-KK motifs were applied to design an enfuvirtide analogue 2 that exhibited highly potent anti-HIV activity against wild-type HIV-1, enfuvirtide-resistant HIV-1 strains, and an HIV-2 strain in vitro. Indispensable residues for bioactivity of enfuvirtide, including the residues interacting with the N-terminal heptad repeat and the C-terminal hydrophobic residues, were identified.