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Systematic screening of the cellular uptake of designed alpha-helix peptides.

Abstract：

:The cellular penetration (CP) activity of functional molecules has attracted significant attention as one of the most promising new approaches for drug delivery. In particular, cell-penetrating peptides (CPPs) have been studied extensively in cellular engineering. Because there have been few large-scale systematic studies to identify peptide sequences with optimal CP activity or that are suitable for further applications in cell engineering, such as cell-specific penetration and cell-selective culture, we screened and compared the cellular uptake (CU) activity of 54 systematically designed α-helical peptides in HeLa cells. Furthermore, the CU activity of 24 designed peptides was examined in four cell lines using a cell fingerprinting technique and statistical approaches. The CU activities in various cells depended on amino acid residues of peptide sequences as well as charge, α-helical content and hydrophobicity of the peptides. Notably, the mutation of a single residue significantly altered the CU ability of a peptide, highlighting the variability of cell uptake mechanisms. Moreover, these results demonstrated the feasibility of cell-selective culture by conducting cell-selective permeation and death in cultures containing two cell types. These studies may lead to further peptide library design and screening for new classes of CPPs with useful functions.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Usui K,Kikuchi T,Mie M,Kobatake E,Mihara H

doi

10.1016/j.bmc.2013.02.030

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

2560-7

issue

9

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(13)00163-6

journal_volume

21

pub_type

杂志文章

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