| Literature DB >> 27025342 |
Michael T Migawa1, Thazha P Prakash2, Guillermo Vasquez2, W Brad Wan2, Jinghua Yu2, Garth A Kinberger2, Michael E Østergaard2, Eric E Swayze2, Punit P Seth2.
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.Entities:
Keywords: Conjugate; GalNAc; Nucleic acid; Synthesis
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Year: 2016 PMID： 27025342 DOI： 10.1016/j.bmcl.2016.03.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823