| 초록 |
Covalent conjugation of disparate peptide and oligonucleotide biomacromolecular species produces peptide-oligonucleotide conjugates (POCs) with great potential for use in diverse bioapplications. However, peptide-oligonucleotide conjugation methods are not well established, and the intracellular delivery efficacy of POCs is debatable. Here, we describe a simple method for the synthesis of POCs utilizing fragment conjugation to circumvent the incompatibilities in deprotection chemistries. When peptides are carefully designed to have a near-neutral charge state, a relatively hydrophobic polarity, receptor-targeting ligands and synthesis become highly efficient and straightforward. Also, POCs can easily be purified without tricky desalting process. The peptide design strategy, targeting ligands and relatively hydrophobic property enable the efficient cellular delivery of POCs. |
