Ontology highlight
ABSTRACT:
SUBMITTER: Wan WB
PROVIDER: S-EPMC4267618 | biostudies-literature | 2014 Dec
REPOSITORIES: biostudies-literature
Wan W Brad WB Migawa Michael T MT Vasquez Guillermo G Murray Heather M HM Nichols Josh G JG Gaus Hans H Berdeja Andres A Lee Sam S Hart Christopher E CE Lima Walt F WF Swayze Eric E EE Seth Punit P PP
Nucleic acids research 20141114 22
Bicyclic oxazaphospholidine monomers were used to prepare a series of phosphorothioate (PS)-modified gapmer antisense oligonucleotides (ASOs) with control of the chirality of each of the PS linkages within the 10-base gap. The stereoselectivity was determined to be 98% for each coupling. The objective of this work was to study how PS chirality influences biophysical and biological properties of the ASO including binding affinity (Tm), nuclease stability, activity in vitro and in vivo, RNase H ac ...[more]