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Abstract
Small synthetic molecules that can specifically inhibit translation and/or transcription
have shown great promise as potential antisense/antigene drugs. Peptide nucleic acid
(PNA), an oligonucleotide mimic, has a non-charged achiral polyamide backbone to which
the nucleobases are attached. PNA oligomers are extremely stable in biological fluids
and they specifically hybridise to DNA or RNA in a complementary manner, forming very
strong heteroduplexes. Some of the mRNAs have yet undetermined and possibly long half-lives,
successful down regulation of gene expression by antisense oligonucleotides (ON) requires
that the antisense agent is long lived. PNA fulfils this requirement better than phosphodiester
or phosphorothioate ONs. PNA can inhibit transcription and translation of respective
genes by tight binding to DNA or mRNA. First in vitro experiments to specifically
down regulate protein expression by PNA have been followed by successful antisense
and antigene application of PNA oligomers in vivo. This review discusses the principles
of the in vitro and in vivo use of PNA oligonucleotides.