Author/Authors :
Hiroki Nishikawa، نويسنده , , Shinya Oishi، نويسنده , , Mizuno Fujita، نويسنده , , Kentaro Watanabe، نويسنده , , Rei Tokiwa، نويسنده , , Hiroaki Ohno، نويسنده , , Eiichi Kodama، نويسنده , , Kazuki Izumi، نويسنده , , Keiko Kajiwara، نويسنده , , Takeshi Naitoh، نويسنده , , Masao Matsuoka، نويسنده , , Akira Otaka، نويسنده , , Nobutaka Fujii*، نويسنده ,
Abstract :
Emergence of multi-drug resistant HIV-1 is a serious problem for AIDS treatment. Recently, the virus-cell membrane fusion process has been identified as a promising target for the development of novel drugs against these resistant variants. In this study, we identified a 29-residue peptide fusion inhibitor, SC29EK, which shows activity comparable to the previously reported inhibitor SC35EK. Some residues in SC29EK not required for interaction with virus gp41 heptad repeat 1 (HR1) were replaced with a non-proteinogenic amino acid, 2-aminoisobutyric acid (Aib), to stabilize the α-helix structure and to provide resistance to peptidases.
Keywords :
HIV-1 , Fusion inhibitor , ?-Helix , Heptad repeat
