| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1368591 | Bioorganic & Medicinal Chemistry Letters | 2016 | 4 Pages |
Abstract
A convenient method for the synthesis of several triantennary GalNAc clusters based on a nitromethanetrispropionic acid core was developed. The synthetic approach involves pentafluorophenolic ester intermediates which can be used in a one-pot, seven reaction procedure to quickly prepare a variety of triantennary GalNAc conjugated ASOs. The GalNAc clusters were conjugated to the 5′-end of an antisense oligonucleotide and evaluated for activity in primary mouse hepatocytes where they showed ∼10-fold improvement in activity.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Michael T. Migawa, Thazha P. Prakash, Guillermo Vasquez, W. Brad Wan, Jinghua Yu, Garth A. Kinberger, Michael E. Østergaard, Eric E. Swayze, Punit P. Seth,