title: Identification of minimal sequence for HIV-1 fusion inhibitors.
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 alpha-helix structure and to provide resistance to peptidases.
authors.affiliation: Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
authors.forename: Hiroki
authors.initials: H
authors.lastname: Nishikawa
authors.forename: Shinya
authors.initials: S
authors.lastname: Oishi
authors.forename: Mizuno
authors.initials: M
authors.lastname: Fujita
authors.forename: Kentaro
authors.initials: K
authors.lastname: Watanabe
authors.forename: Rei
authors.initials: R
authors.lastname: Tokiwa
authors.forename: Hiroaki
authors.initials: H
authors.lastname: Ohno
authors.forename: Eiichi
authors.initials: E
authors.lastname: Kodama
authors.forename: Kazuki
authors.initials: K
authors.lastname: Izumi
authors.forename: Keiko
authors.initials: K
authors.lastname: Kajiwara
authors.forename: Takeshi
authors.initials: T
authors.lastname: Naitoh
authors.forename: Masao
authors.initials: M
authors.lastname: Matsuoka
authors.forename: Akira
authors.initials: A
authors.lastname: Otaka
authors.forename: Nobutaka
authors.initials: N
authors.lastname: Fujii
mesh_terms: D000595:Amino Acid Sequence; D002460:Cell Line; D002942:Circular Dichroism; D023581:HIV Fusion Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008969:Molecular Sequence Data; D011489:Protein Denaturation
chemical_list: D023581:HIV Fusion Inhibitors