Membrane anchoring of a curvature-inducing peptide, EpN18, promotes membrane translocation of octaarginine

[Display omitted] EpN18 is a curvature-inducing peptide, which loosens lipid packing upon interaction with the cell membrane, and facilitates cell-membrane penetration by arginine-rich cell-penetrating peptides, including octaarginine (R8). In the present study, we conjugated the N-terminal of EpN18...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2021-07, Vol.43, p.128103-128103, Article 128103
Hauptverfasser: Kuroki, Kakeru, Sakai, Takayuki, Masuda, Toshihiro, Kawano, Kenichi, Futaki, Shiroh
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Sprache:eng
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Zusammenfassung:[Display omitted] EpN18 is a curvature-inducing peptide, which loosens lipid packing upon interaction with the cell membrane, and facilitates cell-membrane penetration by arginine-rich cell-penetrating peptides, including octaarginine (R8). In the present study, we conjugated the N-terminal of EpN18 with a pyrenebutyryl (pBu) moiety, which acts as an anchoring unit that increases membrane interactions. Enhanced lipid-packing loosening and cytosolic translocation of R8 were observed by the pBu anchoring of EpN18.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2021.128103