Binding Properties of the Conjugates of Oligo(2′‐O‐Methylribonucleotides) with Minor Groove Binders Targeted to Double Stranded DNA

Abstract

Design, synthesis, physico‐chemical and in vitro biological studies of new pyrimidine oligo(2′‐O‐methylribonucleotide) conjugates with oligocarboxamide minor groove binders (MGB) and benzoindoloquinoline intercalator (BIQ) are described. These conjugates formed stable triple helices with the target double‐stranded DNA and inhibited its in vitro transcription upon binding.

Keywords:

• Oligo(2′‐O‐methylribonucleotides)
• Conjugates
• Minor groove binders
• Triple helix
• Transcription inhibition

Acknowledgments

This work was supported by INTAS (project 2001–0638), CRDF (project NO‐008‐X1), Ministry of Foreign Affairs of France (project EGIDE N° 04542ND), Ministry of Education of Russian Federation (project E02.–2.0–30) and RAS (project No. 228 of the Sixth Competition of Young Scientists).