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crc press - E-Lib FK UWKS

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Penetratins 33<br />

TABLE 2.3 (continued)<br />

Cargoes Internalized In Vitro and In Vivo<br />

with AntpHD-Derived Peptidic Vectors<br />

Type of cargo Length Vector Cargo effect Ref.<br />

PNA<br />

GalR1 21 mer Penetratin Down regulates Galanin receptor R1 in vivo 67<br />

Telomerase 13 mer Penetratin Inhibits telomerase in melanoma cells 65, 66<br />

Chemical drug<br />

Doxorubicin Penetratin Doxorubicin crosses BBB 78<br />

Cargo<br />

-SH<br />

Cargo -S-S- py<br />

Cargo<br />

NH2-<br />

Cargo<br />

-S-S-<br />

FIGURE 2.2 Two modes of coupling cargoes to Penetratin peptides: (1) linkage requiring<br />

disulfide bond formation. Cargo and vector are synthesized with a cysteine in which the thiol<br />

group is protected with a pyridinium group (py). The pyridinium on the cargo is removed<br />

either by dithiothreitol (DTT), in the case of oligonucleotides, or by tris-(2-carboxyethyl)<br />

phosphine hydrochloride (TCEP). (2) Chemical synthesis in tandem. The cargo (a peptide in<br />

this case) is synthesized in tandem with the vector. (3) Alternatively, fusion peptides (vector<br />

and cargo) can be ex<strong>press</strong>ed in E. Coli and purified.<br />

-S -<br />

NH2- Vector -COOH<br />

-S-S-<br />

Chemical synthesis and coupling via a disulfide bond<br />

Vector Cargo<br />

Chemical synthesis in tandem<br />

Vector Cargo<br />

Tandem synthesis in bacteria<br />

Vector<br />

py<br />

-COOH

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