Anti-(Raf-1) RNA aptamers that inhibit Ras-induced Raf-1 activation

Eur J Biochem. 2002 Jan;269(2):697-704. doi: 10.1046/j.0014-2956.2001.02703.x.


RNA aptamers with affinity for the Ras-binding domain (RBD) of Raf-1 were isolated from a degenerate pool by in vitro selection. These aptamers efficiently inhibited the Ras interaction with the Raf-1 RBD, and also inhibited Ras-induced Raf-1 activation in a cell-free system. The RNA aptamer with the most potent inhibitory effect specifically inhibited the Ras-Raf-1 interaction and had no affinity for the RBD of the RGL protein, a homolog of the Ral GDP dissociation stimulator. Although the aptamer was capable of binding to the B-Raf RBD, the RNA did not inhibit the interaction between Ras and the B-Raf RBD. Enzymatic and chemical probing experiments indicated that the aptamer was folded into a pseudoknot structure, and some loop regions of the pseudoknot were located at the binding interface for the Raf-1 RBD.

MeSH terms

  • Base Sequence
  • Cell Line
  • Humans
  • Molecular Sequence Data
  • Nucleic Acid Conformation
  • Proto-Oncogene Proteins c-raf / antagonists & inhibitors
  • Proto-Oncogene Proteins c-raf / genetics
  • Proto-Oncogene Proteins c-raf / metabolism*
  • RNA / chemistry
  • RNA / pharmacology*
  • ras Proteins / metabolism*


  • RNA
  • Proto-Oncogene Proteins c-raf
  • ras Proteins