siRNA modified with 2'-deoxy-2'-C-methylpyrimidine nucleosides.

siRNA modified with 2'-deoxy-2'-C-methylpyrimidine nucleosides.
Chembiochem. 2018 Apr 14;:
Authors: Dellafiore M, Aviñó A, Alagia A, Montserrat JM, Iribarren AM, Eritja R
Abstract
(2'S)-2'-Deoxy-2'-C-methyluridine and (2'R)-2'-deoxy-2'-C-methyluridine were incorporated in the 3'-overhang region of the sense and antisense strands and in positions 2- and 5- of the seed region of siRNA duplexes directed against Renilla luciferase, while (2'S)-2'-deoxy-2'-C-methylcytidine was incorporated in the 6- position of the seed region of the same constructions. Dual luciferase reporter assay in transfected HeLa cells was used as model system to measure IC50 values of 24 different modified duplexes. The best results were obtained by the substitution of one thymidine of the antisense 3'-overhang region by (2'S) or (2'R)-2'-deoxy-2'-C-methyluridine reducing IC50 by half of the value observed for the natural control. Selectivity of the modified siRNA was measured, finding that modifications in positions 5- and 6- of the seed region had a positive effect on the ON/OFF activity.
PMID: 29656613 [PubMed - as supplied by publisher]

Source: Chembiochem - April 14, 2018 Category: Biochemistry Authors: Dellafiore M, Aviñó A, Alagia A, Montserrat JM, Iribarren AM, Eritja R Tags: Chembiochem Source Type: research