Depth-Profiling the Nuclease Stability and the Gene Silencing Efficacy of Brush-Architectured Poly(ethylene glycol)-DNA Conjugates

J Am Chem Soc. 2017 Aug 9;139(31):10605-10608. doi: 10.1021/jacs.7b05064. Epub 2017 Jul 26.

Abstract

PEGylation of an oligonucleotide using a brush polymer can improve its biopharmaceutical characteristics, including enzymatic stability and biodistribution. Herein, we quantitatively explore the nuclease accessibility of the nucleic acid as a function of "depth" toward the backbone of the brush polymer. It is found that protein accessibility decreases as the nucleotide is located closer to the backbone. Thus, by moving the conjugation point from the terminus of the nucleic acid strand to an internal position, much smaller brushes can be used to achieve the same level of steric shielding. This finding also makes it possible to assess antisense gene regulation efficiency of these brush-DNA conjugates as a function of their nuclease stability.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Biological Assay
  • DNA / chemistry*
  • DNA / pharmacology*
  • Deoxyribonucleases / chemistry
  • Enzyme Stability
  • Gene Silencing / drug effects*
  • Nucleotides / chemistry*
  • Nucleotides / pharmacology
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacology*
  • Surface Properties

Substances

  • Nucleotides
  • Polyethylene Glycols
  • DNA
  • Deoxyribonucleases