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    J Med Chem. 2010 May 27;53(10):3919-26.

    Peptide nucleic acids conjugated to short basic peptides show improved pharmacokinetics and antisense activity in adipose tissue.

    Wancewicz EV, Maier MA, Siwkowski AM, Albertshofer K, Winger TM, Berdeja A, Gaus H, Vickers TA, Bennett CF, Monia BP, Griffey RH, Nulf CJ, Hu J, Corey DR, Swayze EE, Kinberger GA.

    Source

    Isis Pharmaceuticals, Inc., Carlsbad, California 92008, USA.

    Abstract

    A peptide nucleic acid (PNA) targeting a splice junction of the murine PTEN primary transcript was covalently conjugated to various basic peptides. When systemically administered to healthy mice, the conjugates displayed sequence-specific alteration of PTEN mRNA splicing as well as inhibition of full length PTEN protein expression. Correlating activity with drug concentration in various tissues indicated strong tissue-dependence, with highest levels of activity observed in adipose tissue. While the presence of a peptide carrier was found to be crucial for efficient delivery to tissue, little difference was observed between the various peptides evaluated. A second PNA-conjugate targeting the murine insulin receptor primary transcript showed a similar activity profile, suggesting that short basic peptides can generally be used to effectively deliver peptide nucleic acids to adipose tissue.

    PMID:
    20420385
    [PubMed - indexed for MEDLINE]
    PMCID: PMC3072269
    Free PMC Article

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