siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides

(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, whereas (2'...

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Detalles Bibliográficos
Publicado: 2018
Materias:
Deoxymethylpyrimidine bases
Nucleosides
SiRNA
Stability
Structure-activity relationships
Acceso en línea:https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14394227_v_n_p_Dellafiore
http://hdl.handle.net/20.500.12110/paper_14394227_v_n_p_Dellafiore
Aporte de:
Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA) de Universidad de Buenos Aires
id paper:paper_14394227_v_n_p_Dellafiore
record_format dspace
spelling paper:paper_14394227_v_n_p_Dellafiore2023-06-08T16:15:58Z siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides Deoxymethylpyrimidine bases Nucleosides SiRNA Stability Structure-activity relationships (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, whereas (2'S)-2'-deoxy-2'-C-methylcytidine was incorporated in the 6-position of the seed region of the same constructions. A dual luciferase reporter assay in transfected HeLa cells was used as a model system to measure the IC 50 values of 24 different modified duplexes. The best results were obtained by the substitution of one thymidine unit in the antisense 3'-overhang region by (2'S)- or (2'R)-2'-deoxy-2'-C-methyluridine, reducing IC 50 to half of the value observed for the natural control. The selectivity of the modified siRNA was measured, it being found that modifications in positions 5 and 6 of the seed region had a positive effect on the ON/OFF activity. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. 2018 https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14394227_v_n_p_Dellafiore http://hdl.handle.net/20.500.12110/paper_14394227_v_n_p_Dellafiore
institution Universidad de Buenos Aires
institution_str I-28
repository_str R-134
collection Biblioteca Digital - Facultad de Ciencias Exactas y Naturales (UBA)
topic Deoxymethylpyrimidine bases
Nucleosides
SiRNA
Stability
Structure-activity relationships
spellingShingle Deoxymethylpyrimidine bases
Nucleosides
SiRNA
Stability
Structure-activity relationships
siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
topic_facet Deoxymethylpyrimidine bases
Nucleosides
SiRNA
Stability
Structure-activity relationships
description (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, whereas (2'S)-2'-deoxy-2'-C-methylcytidine was incorporated in the 6-position of the seed region of the same constructions. A dual luciferase reporter assay in transfected HeLa cells was used as a model system to measure the IC 50 values of 24 different modified duplexes. The best results were obtained by the substitution of one thymidine unit in the antisense 3'-overhang region by (2'S)- or (2'R)-2'-deoxy-2'-C-methyluridine, reducing IC 50 to half of the value observed for the natural control. The selectivity of the modified siRNA was measured, it being found that modifications in positions 5 and 6 of the seed region had a positive effect on the ON/OFF activity. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
title siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
title_short siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
title_full siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
title_fullStr siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
title_full_unstemmed siRNA Modified with 2'-Deoxy-2'-C-methylpyrimidine Nucleosides
title_sort sirna modified with 2'-deoxy-2'-c-methylpyrimidine nucleosides
publishDate 2018
url https://bibliotecadigital.exactas.uba.ar/collection/paper/document/paper_14394227_v_n_p_Dellafiore
http://hdl.handle.net/20.500.12110/paper_14394227_v_n_p_Dellafiore
_version_ 1768543530077126656

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