Nucleic Acids Research · 1994 · 55 citations · 26 references
Life SciencesMedicinal ChemistryMolecular BiologyEnzymologyMolecular PharmacologySignal TransductionEnzyme InhibitionLigand BindingNucleic Acid Drug DesignOligonucleotide ChemistryReceptor Tyrosine Kinase SignalingTyrosine Kinase InhibitorsAptamer ChemistryBcr-abl InhibitorsChemical Modification Of OligonucleotidesOligonucleotide Backbone ModificationsOligonucleotide TherapeuticsProtein Kinase InhibitorsTherapeutic Tyrosine Kinase InhibitorsTyrosine Kinase Inhibition
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 microM. 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.
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Selection of single-stranded DNA molecules that bind and inhibit human thrombin
Louis C. Bock, Linda C. Griffin, John Latham et al. · Nature · 1992 · 2.5K citations
Steven K. Hanks, Anne Marie Quinn · Methods in enzymology on CD-ROM/Methods in enzymology · 1991 · 1.2K citations