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Xentry, a new class of cell-penetrating peptide uniquely equipped for delivery of drugs.

ABSTRACT: Here we describe an entirely new class of cell-penetrating peptide (CPP) represented by the short peptide Xentry (LCLRPVG) derived from an N-terminal region of the X-protein of the hepatitis B virus. Xentry permeates adherent cells using syndecan-4 as a portal for entry, and is uniquely restricted from entering syndecan-deficient, non-adherent cells, such as resting blood cells. Intravenous injection of Xentry alone or conjugated to ?-galactosidase led to its delivery to most tissues in mice, except circulating blood cells. There was a predilection for uptake by epithelia. Anti-B-raf antibodies and siRNAs linked to Xentry were capable of killing B-raf-dependent melanoma cells. Xentry represents a new class of CPP with properties that are potentially advantageous for life science and therapeutic applications.

SUBMITTER: Montrose K

PROVIDER: S-EPMC3627194 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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Xentry, a new class of cell-penetrating peptide uniquely equipped for delivery of drugs.

Montrose Kristopher K Yang Yi Y Sun Xueying X Wiles Siouxsie S Krissansen Geoffrey W GW

Scientific reports 20130101

Here we describe an entirely new class of cell-penetrating peptide (CPP) represented by the short peptide Xentry (LCLRPVG) derived from an N-terminal region of the X-protein of the hepatitis B virus. Xentry permeates adherent cells using syndecan-4 as a portal for entry, and is uniquely restricted from entering syndecan-deficient, non-adherent cells, such as resting blood cells. Intravenous injection of Xentry alone or conjugated to β-galactosidase led to its delivery to most tissues in mice, ex ...[more]

PMID: 23588666

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