title: Novel cell penetrating peptides with multiple motifs composed of RGD and its analogs.
abstract: Cell penetrating peptides (CPPs) have been used to transport macromolecules into cells. Most CPPs have properties such as a strong polycationic charge, amphipathic basic, and hydrophobicity. In this study, we designed the peptides with multiple motifs composed of RGD and its analogs to induce integrin-mediated endocytosis as well as endosomal escape by forming an amphipathic helix in acidic endosomes. These peptides were proved less toxic to animal cells than those without acidic residues. Unexpectedly, peptide conjugated liposomes could penetrate into cells regardless of integrins. The replacement of all aspartic acids by glutamic acids did not prevent the peptide-mediated liposome uptake, and the higher basic and leucine contents enhanced the gene silencing activity of siRNA encapsulated in the liposomes. The peptide is considered to be a new type of CPP which can be used for drug delivery.
authors: Bionanotechnology Research Center, KRIBB, 125 Gwahak-ro, Yuseong-gu, Daejeon 305-806, Republic of Korea.
authors: Amir Abbas
authors: AA
authors: Mokhtarieh
authors: Semi
authors: S
authors: Kim
authors: Yunhee
authors: Y
authors: Lee
authors: Bong Hyun
authors: BH
authors: Chung
authors: Myung Kyu
authors: MK
authors: Lee
mesh_terms: D020816:Amino Acid Motifs; D000595:Amino Acid Sequence; D019943:Amino Acid Substitution; D000818:Animals; D001224:Aspartic Acid / Q000737:chemistry; D045744:Cell Line, Tumor; D057846:Cell-Penetrating Peptides / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D020868:Gene Silencing; D018698:Glutamic Acid / Q000737:chemistry; D006801:Humans; D008081:Liposomes; D051379:Mice; D008969:Molecular Sequence Data; D041681:NIH 3T3 Cells; D009842:Oligopeptides / Q000737:chemistry*; D034741:RNA, Small Interfering / Q000235:genetics / Q000378:metabolism*
chemical_list: D057846:Cell-Penetrating Peptides; D008081:Liposomes; D009842:Oligopeptides; D034741:RNA, Small Interfering; D001224:Aspartic Acid; D018698:Glutamic Acid; C047981:arginyl-glycyl-aspartic acid