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Table 2 Representative examples of His-rich peptides used in nanomedicine as endosomolytic agents.

From: Biological activities of histidine-rich peptides; merging biotechnology and nanomedicine

Type of construct

Tag sequence

Experimental model

# of His residues

References

pDNA/siRNA +peptide

CHK6HC

CH3K3H3C

CH6K3H6C

In vitro, HepG2, COS 7, and CHO cells, 10X more expression than w/o histidine

2-12

[44]

pDNA + peptide +lactosylated polylysine

H5WYG (23 aas; GLFHAIAHFIHGGWHGLIHGWYG)

In vitro, HepG2, B16 and Rb-1cells, 93-2150X more expression than control, with serum.

5

[45]

MS2 VLPs-peptide

 

In Hep3B cells mediate endosomal escape that doesn't occur without the peptide.

5

[46]

pDNA+ PEG-H5WYG

 

CHO cells; increase expression 2-5 fold.

5

[47]

Lipopeptide + pDNA

Lau/PalCK3H2

In vitro, COS 7 cells, similar results to PEI, lipofectamine

2

[48]

pDNA + peptide

LAH4 (26 aas; KKALLALALHHLAHLALHLALALKKA)

In vitro, human hepatocarcinoma cells, 10× more expression than lipofectamine.

4

[49]

Chitosan-CH + pDNA

Chitosan-CH

Chit. KH dendron

In vitro, HEK293 cells, increases expression up to 50-fold over chitosan alone.

1

[50]

Chit. 4 gen KH dendron + pDNA

 

Chitosan dendron improves escape over Chitosan-CH

1

[51]

pDNA + peptide

Tat-H10

C-H5-Tat-H5-C

In vitro, in U251, H4, T98G and C6 cell lines, up to 7000-fold improvement. In vivo, in rat intrastriatum injection.

10

[27]

FuGENE lipid+ peptide+ pDNA

 

In vitro in 5 different cell lines, significant improvement over pDNA+ peptide alone

10

[52]

CM-PLH+PbAE+pDNA

Polymer CM-PLH

In vitro, in HEK293 and B16-F10 cells, and in vivo, i.v. mice injection; higher transfection efficiency over PbAE alone

1

[53]

STR-CH2R4H2C +pDNA

STR-CH2R4H2C

In vitro, COS-7 cells, improves lipofectamine levels of expression.

2

[54]

(KHKHKHKHKK)6-FGF2 + pDNA

KHKHKHKHKK

In vitro, NIH 3T3, T-47D and COS-1 cells; expression is detected in 15-41% of cells, but not quantitated; no serum.

24

[55]

  1. Abbreviations: aas, amino acids; pDNA, plasmid DNA; PEI, poly (ethylene imine); aas, aminoacids; Lau, lauryl; Pal, palmytoil; chit. 4 gen, chitosan 4 generation; CM-PLH, carboxymethyl poly (L- histidine); PbAE, poly (β-amino ester); STR, staeroyl; FGF-2, fibroblast growth factor-2.