Monofunctionally trans-Diammine Platinum(II)-Modified Peptide Nucleic Acid Oligomers: A New Generation of Potential Antisense Drugs
✍ Scribed by Kathrin S. Schmidt; Marc Boudvillain; Annie Schwartz; Gijs A. van der Marel; Jacques H. van Boom; Jan Reedijk; Bernhard Lippert
- Publisher
- John Wiley and Sons
- Year
- 2002
- Tongue
- English
- Weight
- 121 KB
- Volume
- 8
- Category
- Article
- ISSN
- 0947-6539
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✦ Synopsis
A solid-phase approach is described that provides facile access to monofunctionally trans-PtII-modified PNA oligomers of arbitrary sequence for potential use both in antigene and antisense strategies. The approach includes the synthesis of a platinated building block 1 and its subsequent incorporation into three different PNA oligomers 5-7 by solid-phase synthesis. In a model cross-linking reaction one of the latter is found to recognize sequence-specifically a target oligonucleotide 8 and to cross-link to it. The resulting structure is the trans-PtII-cross-linked PNA/DNA duplex 9 as revealed by mass spectrometry in combination with a Maxam-Gilbert sequencing experiment.