title: Identification of a peptide sequence that improves transport of macromolecules across the intestinal mucosal barrier targeting goblet cells.
abstract: In this study, we demonstrated that the CSKSSDYQC-peptide ligand which was identified from a random phage-peptide library through an in vivo phage display technique with rats could prominently improve the transport efficiency of macromolecules, such as large filamentous phage particles (M13 bacteriophage), across the intestinal mucosal barrier. Synthetic CSKSSDYQC-peptide ligands significantly inhibited the binding of phage P1 encoding CSKSSDYQC-peptide ligands to the intestinal mucosal tissue and immunohistochemical analysis showed that the CSKSSDYQC-peptide ligands could be transported across the intestinal mucosal barrier via goblet cells as their specific gateway. Thus, we inferred that CSKSSDYQC-peptide ligand might have a specific receptor on the goblet cells and transported from intestinal lumen to systemic circulation by transcytosis mechanism. These results suggest that CSKSSDYQC-ligand could be a promising tool for development of an efficient oral delivery system for macromolecular therapeutics in the carrier-drug conjugate strategy.
authors.affiliation: School of Agricultural Biotechnology, Seoul National University, San 56-1, Sillimdong, Gwanakgu, Seoul 151-921, South Korea.
authors.forename: Sang Kee
authors.initials: SK
authors.lastname: Kang
authors.forename: Jung Hee
authors.initials: JH
authors.lastname: Woo
authors.forename: Min Kook
authors.initials: MK
authors.lastname: Kim
authors.forename: Sang Soo
authors.initials: SS
authors.lastname: Woo
authors.forename: Jin Hyuk
authors.initials: JH
authors.lastname: Choi
authors.forename: Hong Gu
authors.initials: HG
authors.lastname: Lee
authors.forename: Nam Kyung
authors.initials: NK
authors.lastname: Lee
authors.forename: Yun Jaie
authors.initials: YJ
authors.lastname: Choi
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D017104:Bacteriophage M13 / Q000235:genetics / Q000378:metabolism / Q000502:physiology; D017101:Bacteriophage P1 / Q000235:genetics / Q000378:metabolism / Q000502:physiology; D001692:Biological Transport; D020397:Goblet Cells / Q000166:cytology / Q000378:metabolism*; D007150:Immunohistochemistry; D007413:Intestinal Mucosa / Q000166:cytology / Q000378:metabolism* / Q000821:virology; D007421:Intestine, Small / Q000166:cytology / Q000378:metabolism / Q000821:virology; D008297:Male; D008856:Microscopy, Fluorescence; D008962:Models, Theoretical; D019151:Peptide Library; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D011485:Protein Binding; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D019151:Peptide Library; D010455:Peptides