Biologically Active Antisense Phosphorothioate Oligodeoxyribonucleotides: Synthesis, Characterization, and Studies of 3′‐Terminal Phosphorothioate Monoester Analogues

Abstract

Multiple phosphorothioate oligonucleotides containing a 3′‐terminal negative charge were synthesized and characterized. Influence of the added negative charge on activation of duplexes by RNase H was investigated. No additional help in recruitment of RNase H was observed.

^†In honor and celebration of the 70th birthday of Professor Leroy B. Townsend.

Keywords:

• Antisense phosphorothioate oligonucleotides
• 3′‐TPT
• RNase H activation

Notes

^†In honor and celebration of the 70th birthday of Professor Leroy B. Townsend.

^aMultiple second‐generation phosphorothioate oligonucleotides are in various stages of evaluation targeted against TNFα, VLA4, C‐raf, PTB1B, ApoB 100, etc for a variety of diseases such as cancer, asthma, arthritis, multiple sclerosis, etc.