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Development of Cell-type specific anti-HIV gp120 aptamers for siRNA delivery
Published on: June 23, 2011
Rapid HATU-mediated solution phase siRNA conjugation
Jeffrey G Aaronson1, Lee J Klein, Aaron A Momose
1Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., West Point, Pennsylvania 19486, United States. jeffrey_aaronson@merck.com
Bioconjugate Chemistry
|July 13, 2011
Abstract:
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.
