Rapid HATU-Mediated Solution Phase siRNA Conjugation

被引：11

作者：

Aaronson, Jeffrey G. ^{[1
]}

Klein, Lee J. ^{[2
]}

Momose, Aaron A. ^{[1
]}

O'Brien, Ann M. ^{[2
]}

Shaw, Anthony W. ^{[1
]}

Tucker, Thomas J. ^{[1
]}

Yuan, Yu ^{[1
]}

Tellers, David M. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, West Point, PA 19486 USA

[2] Merck & Co Inc, Dept Pharmaceut Analyt Chem, Merck Res Labs, West Point, PA 19486 USA

来源：

BIOCONJUGATE CHEMISTRY | 2011年 / 22卷 / 08期

关键词：

COUPLING REAGENTS; PEPTIDE-SYNTHESIS; IN-VIVO; OLIGONUCLEOTIDE; DELIVERY; DNA; CHEMISTRY; LABELS; CELLS;

D O I：

10.1021/bc2001227

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Conditions for facile solution-phase amide conjugation of amine-modified siRNA with a diverse set of carboxylic acid partners using the coupling reagent HATU are described. These conditions eliminate the need for isolated activated esters and allow for rapid access to conjugates with a wide range of lipophilicity and functionality in good yield.

引用

页码：1723 / 1728

页数：6

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