5625050 Modified oligonucleotides and intermediates useful in nucleic acid therapeutics

1997 ◽  
Vol 15 (3-4) ◽  
pp. 685
Author(s):  
Jayesh A. Kulkarni ◽  
Dominik Witzigmann ◽  
Sarah B. Thomson ◽  
Sam Chen ◽  
Blair R. Leavitt ◽  
...  

Small Methods ◽  
2021 ◽  
Vol 5 (9) ◽  
pp. 2170044
Author(s):  
Chiara Rinoldi ◽  
Seyed Shahrooz Zargarian ◽  
Pawel Nakielski ◽  
Xiaoran Li ◽  
Anna Liguori ◽  
...  

Small Methods ◽  
2021 ◽  
pp. 2100402
Author(s):  
Chiara Rinoldi ◽  
Seyed Shahrooz Zargarian ◽  
Pawel Nakielski ◽  
Xiaoran Li ◽  
Anna Liguori ◽  
...  

2020 ◽  
Vol 18 (46) ◽  
pp. 9461-9472
Author(s):  
Shinji Kumagai ◽  
Hiroaki Sawamoto ◽  
Tomo Takegawa-Araki ◽  
Yuuki Arai ◽  
Shuhei Yamakoshi ◽  
...  

Facile synthesis of GuNA (guanidine-bridged nucleic acid) phosphoramidites bearing thymine, adenine, guanine, and 5-methylcytosine nucleobases and a robust method for the preparation of GuNA-modified oligonucleotides are described.


2021 ◽  
Vol 17 ◽  
pp. 622-629
Author(s):  
Naohiro Horie ◽  
Takao Yamaguchi ◽  
Shinji Kumagai ◽  
Satoshi Obika

Chemical modifications have been extensively used for therapeutic oligonucleotides because they strongly enhance the stability against nucleases, binding affinity to the targets, and efficacy. We previously reported that oligonucleotides modified with an N-methylguanidine-bridged nucleic acid (GuNA[Me]) bearing the thymine (T) nucleobase show excellent biophysical properties for applications in antisense technology. In this paper, we describe the synthesis of GuNA[Me] phosphoramidites bearing other typical nucleobases including adenine (A), guanine (G), and 5-methylcytosine (mC). The phosphoramidites were successfully incorporated into oligonucleotides following the method previously developed for the GuNA[Me]-T-modified oligonucleotides. The binding affinity of the oligonucleotides modified with GuNA[Me]-A, -G, or -mC toward the complementary single-stranded DNAs or RNAs was systematically evaluated. All of the GuNA[Me]-modified oligonucleotides were found to have a strong affinity for RNAs. These data indicate that GuNA[Me] could be a useful modification for therapeutic antisense oligonucleotides.


2018 ◽  
Vol 15 (3) ◽  
pp. 1142-1149
Author(s):  
Elisa Zagato ◽  
Lotte Vermeulen ◽  
Heleen Dewitte ◽  
Griet Van Imschoot ◽  
Roosmarijn E. Vandenbroucke ◽  
...  

2020 ◽  
Vol 153 ◽  
pp. 105461
Author(s):  
Miguel Pereira-Silva ◽  
Ivana Jarak ◽  
Ana Cláudia Santos ◽  
Francisco Veiga ◽  
Ana Figueiras

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