A novel branch-type PEGylation of aptamer therapeutics

Hyungu Kang; Jung Kyu Park; Young Bae Seu; Sei Kwang Hahn

doi:10.4028/0-87849-436-7.529

A novel branch-type PEGylation of aptamer therapeutics

Hyungu Kang, Jung Kyu Park, Young Bae Seu, Sei Kwang Hahn

School of Life Science and Biotechnology

Pohang University of Science and Technology

Research output: Contribution to journal › Article › peer-review

3 Scopus citations

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	https://doi.org/10.4028/0-87849-436-7.529
State	Published - 2007

Keywords

Anti-thrombin aptamer
Aptamer therapeutics
Branched oligo-nucleotide
Michael addition
PEGylation
Symmetric doubler phosphoramidite
Thrombus formation

Access to Document

10.4028/0-87849-436-7.529

Cite this

@article{c6d42a5453c347578f82e48df1698f77,

title = "A novel branch-type PEGylation of aptamer therapeutics",

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.",

keywords = "Anti-thrombin aptamer, Aptamer therapeutics, Branched oligo-nucleotide, Michael addition, PEGylation, Symmetric doubler phosphoramidite, Thrombus formation",

author = "Hyungu Kang and Park, {Jung Kyu} and Seu, {Young Bae} and Hahn, {Sei Kwang}",

year = "2007",

doi = "10.4028/0-87849-436-7.529",

language = "English",

volume = "342-343",

pages = "529--532",

journal = "Key Engineering Materials",

issn = "1013-9826",

publisher = "Trans Tech Publications Ltd.",

}

TY - JOUR

T1 - A novel branch-type PEGylation of aptamer therapeutics

AU - Kang, Hyungu

AU - Park, Jung Kyu

AU - Seu, Young Bae

AU - Hahn, Sei Kwang

PY - 2007

Y1 - 2007

N2 - 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.

AB - 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.

KW - Anti-thrombin aptamer

KW - Aptamer therapeutics

KW - Branched oligo-nucleotide

KW - Michael addition

KW - PEGylation

KW - Symmetric doubler phosphoramidite

KW - Thrombus formation

UR - http://www.scopus.com/inward/record.url?scp=34147118683&partnerID=8YFLogxK

U2 - 10.4028/0-87849-436-7.529

DO - 10.4028/0-87849-436-7.529

M3 - Article

AN - SCOPUS:34147118683

SN - 1013-9826

VL - 342-343

SP - 529

EP - 532

JO - Key Engineering Materials

JF - Key Engineering Materials

ER -

A novel branch-type PEGylation of aptamer therapeutics

Abstract

Keywords

Access to Document

Other files and links

Fingerprint

Cite this