The conjugation of Aib-containing amphipathic helical peptide with cyclo(-Arg-Gly-Asp-d-Phe-Cys-) (cRGDfC) at the C-terminus of the helix peptide (PI) has been reported to be useful for constructing a carrier for targeted siRNA delivery into cells. In order to explore structure–activity relationships for the development of potential carriers for siRNA delivery, we synthesized conjugates of Aib-containing amphipathic helical peptide with cRGDfC at the N-terminus (PII) and both the N- and C-termini (PIII) of the helical peptide. Furthermore, to examine the influence of PI helical chain length on siRNA delivery, truncated peptides containing 16 (PIV), 12 (PV), and 8 (PVI) amino acid residues at the N-terminus of the helical chain were synthesized. PII and PIII, as well as PI, could deliver anti-luciferase siRNA into cells to induce the knockdown of luciferase stably expressed in cells. In contrast, all of the truncated peptides were unlikely to transport siRNA into cells.

据报道，含有Aib的两亲性螺旋肽在螺旋肽（PI）的C末端与环（-Arg-Gly-Asp- d -Phe -Cys- ）（cRGDfC）缀合。靶向siRNA进入细胞的载体。为了探索结构-活性之间的关系，以开发潜在的siRNA传递载体，我们在N末端（PII）和N末端和C末端（PIII）上合成了含Aib的两亲性螺旋肽与cRGDfC的结合物。螺旋肽。此外，为了检查PI螺旋链长度对siRNA传递的影响，截短的肽包含16（PIV），12（PV），并在螺旋链的N端合成了8个（PVI）氨基酸残基。PII和PIII以及PI可以将抗萤光素酶siRNA传递到细胞中，从而诱导在细胞中稳定表达的萤光素酶的敲低。相反，所有截短的肽都不太可能将siRNA转运到细胞中。