Literature DB >> 21744777

Rapid HATU-mediated solution phase siRNA conjugation.

Jeffrey G Aaronson1, Lee J Klein, Aaron A Momose, Ann M O'Brien, Anthony W Shaw, Thomas J Tucker, Yu Yuan, David M Tellers.   

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.

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Year:  2011        PMID： 21744777     DOI： 10.1021/bc2001227

Source DB:  PubMed          Journal:  Bioconjug Chem        ISSN： 1043-1802            Impact factor:   4.774


  2 in total

1.  Control of phosphorothioate stereochemistry substantially increases the efficacy of antisense oligonucleotides.

Authors:  Naoki Iwamoto; David C D Butler; Nenad Svrzikapa; Susovan Mohapatra; Ivan Zlatev; Dinah W Y Sah; Stephany M Standley; Genliang Lu; Luciano H Apponi; Maria Frank-Kamenetsky; Jason Jingxin Zhang; Chandra Vargeese; Gregory L Verdine
Journal:  Nat Biotechnol       Date:  2017-08-21       Impact factor: 54.908

2.  Molecular umbrella conjugate for the ocular delivery of siRNA.

Authors:  Vaclav Janout; Lauren L Cline; Bradley P Feuston; Lee Klein; Ann O'Brien; Tom Tucker; Yu Yuan; Lynn A O'Neill-Davis; Robert L Peiffer; Sandhya S Nerurkar; Vasant Jadhav; David M Tellers; Steven L Regen
Journal:  Bioconjug Chem       Date:  2014-01-23       Impact factor: 4.774
  2 in total

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