Abstract
We have developed a novel protocol to prepare a branch-type PEGylation for a long acting formulation of aptamer therapeutics. A symmetric doubler phosphoramidite and the following amine modified phosphoramidite synthon were introduced to the final sequence of anti-thrombin aptamer, as a model for various aptamer therapeutics. The conventional linear PEGylation reagents were conjugated to the terminal amine groups of oligonucleotide to prepare the branch-type PEGylated anti-thrombin DNA aptamer. The PEGylated aptamer exhibited the improved bioactivity to retard the occlusive thrombus formation in vitro.
| Original language | English |
|---|---|
| Pages (from-to) | 529-532 |
| Number of pages | 4 |
| Journal | Key Engineering Materials |
| Volume | 342-343 |
| DOIs | |
| State | Published - 2007 |
Keywords
- Anti-thrombin aptamer
- Aptamer therapeutics
- Branched oligo-nucleotide
- Michael addition
- PEGylation
- Symmetric doubler phosphoramidite
- Thrombus formation
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