Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan.
Institute for Chemical Research, Kyoto University, Uji, Kyoto 611-0011, Japan.
Bioorg Med Chem Lett. 2021 Jul 1;43:128103. doi: 10.1016/j.bmcl.2021.128103. Epub 2021 May 10.
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.
EpN18 是一种诱导卷曲的肽,与细胞膜相互作用时会使脂质排列变松,并促进富含精氨酸的细胞穿透肽(包括八精氨酸(R8))穿透细胞膜。在本研究中,我们将 EpN18 的 N 端与一个 pyrenebutyryl(pBu)部分连接,该部分作为一个锚定单元,增加了与膜的相互作用。EpN18 的 pBu 锚定增强了 R8 的脂质排列变松和细胞质易位。