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Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
Synthesis and evaluation of the functional oligonucleotides-PEG conjugates
Ali Md Monsur1, Fumi Nagatsugi, Motoi Oishi
1Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.
Nucleic Acids Symposium Series (2004)
|December 8, 2006
Summary
Researchers developed novel antisense agents by conjugating PEG to 2-amino-6-vinylpurine derivatives. These modified oligonucleotides show promise for targeted in vitro and in vivo gene silencing applications.
Area of Science:
- Medicinal Chemistry
- Oligonucleotide Therapeutics
- Bioconjugation Chemistry
Background:
- Previous work showed 2-amino-6-vinylpurine derivatives effectively cross-link with cytidine.
- Antisense agents require efficient delivery and stability for therapeutic applications.
Purpose of the Study:
- To synthesize polyethylene glycol (PEG) conjugates of 2-amino-6-vinylpurine derivatives for use as antisense agents.
- To evaluate the potential of these conjugates for in vitro and in vivo applications.
Main Methods:
- Synthesis of an oligonucleotide (ODN) containing a 2-amino-6-vinylpurine nucleoside analog targeting cytidine.
- Modification of the vinyl group to phenylsulfide derivatives.
- Functionalization of the 3' terminal amino group with a thiopropionyl moiety.
- Conjugation of the modified ODN to an acid-responsive PEG (PEG2).
Main Results:
- Successful synthesis of the ODN-PEG conjugate.
- Achieved good isolated yields (55-62%) for the conjugation reaction.
- The synthesized conjugate is designed for targeted delivery and potential therapeutic use.
Conclusions:
- The synthesized 2-amino-6-vinylpurine-PEG conjugates represent a promising platform for developing advanced antisense agents.
- These modified oligonucleotides offer potential for targeted gene silencing in both in vitro and in vivo settings.
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