Aptameric inhibition of p210bcr-abl tyrosine kinase autophosphorylation by oligodeoxynucleotides of defined sequence and backbone structure

Raymond Bergan, Yvette Connell, Brigid Fahmy, Edward Kyle, Len Neckers

Research output: Contribution to journalArticle

55 Citations (Scopus)

Abstract

Protein tyrosine kinases play key roles in cellular physiology. Specific inhibitors of these enzymes are important laboratory tools and may prove to be novel therapeutic agents. In this report we describe a new class of tyrosine kinase inhibitor, synthetic oligodeoxynucleotides (ODNs). An ODN is described which specifically inhibits p210bcr-abl tyrosine kinase autophosphorylation in vitro with a Ki of 0.5 μM. Inhibition is non-competitive with respect to ATP. The effects upon inhibitory activity of ODN structure modifications are described. The inhibition described is not mediated by classical antisense mechanisms and represents an example of the recently recognized aptameric properties of ODNs.

Original languageEnglish (US)
Pages (from-to)2150-2154
Number of pages5
JournalNucleic Acids Research
Volume22
Issue number11
StatePublished - Jun 11 1994
Externally publishedYes

Fingerprint

Oligodeoxyribonucleotides
Backbone
Protein-Tyrosine Kinases
Inhibitor
Protein Kinase
Physiology
Enzymes
Enzyme inhibition
Adenosinetriphosphate
Enzyme Inhibitors
Adenosine Triphosphate
Proteins
Class
Protein
Therapeutics

ASJC Scopus subject areas

  • Genetics
  • Statistics, Probability and Uncertainty
  • Applied Mathematics
  • Health, Toxicology and Mutagenesis
  • Toxicology
  • Genetics(clinical)

Cite this

Aptameric inhibition of p210bcr-abl tyrosine kinase autophosphorylation by oligodeoxynucleotides of defined sequence and backbone structure. / Bergan, Raymond; Connell, Yvette; Fahmy, Brigid; Kyle, Edward; Neckers, Len.

In: Nucleic Acids Research, Vol. 22, No. 11, 11.06.1994, p. 2150-2154.

Research output: Contribution to journalArticle

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