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High-throughput evaluation of relative cell permeability between peptoids and peptides

Title
High-throughput evaluation of relative cell permeability between peptoids and peptides
Authors
Tan N.C.Yu P.Kwon Y.-U.Kodadek T.
Ewha Authors
권용억
SCOPUS Author ID
권용억scopus
Issue Date
2008
Journal Title
Bioorganic and Medicinal Chemistry
ISSN
0968-0896JCR Link
Citation
vol. 16, no. 11, pp. 5853 - 5861
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
Peptides are limited in their use as drugs due to low cell permeability and vulnerability to proteases. In contrast, peptoids are immune to enzymatic degradation and some peptoids have been shown to be relatively cell permeable. In order to facilitate future design of peptoid libraries for screening experiments, it would be useful to have a high-throughput method to estimate the cell permeability of peptoids containing different residues. In this paper, we report the strengths and limitations of a high-throughput cell-based permeability assay that registers the relative ability of steroid-conjugated peptides and peptoids to enter a cell. A comparative investigation of the physicochemical properties and side chain composition of peptoids and peptides is described to explain the observed higher cell permeability of peptoids over peptides. These data suggest that the conversion of the monomeric residues in peptides to an N-alkylglycine moiety in peptoids reduced the hydrogen-bonding potential of the molecules and is the main contributor to the observed permeability improvement. © 2008 Elsevier Ltd. All rights reserved.
DOI
10.1016/j.bmc.2008.04.074
Appears in Collections:
자연과학대학 > 화학·나노과학전공 > Journal papers
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