Identification of the ability of highly charged nanomolar inhibitors of protein kinases to cross plasma membranes and carry a protein into cells

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2117-20. doi: 10.1016/s0960-894x(02)00337-2.

Abstract

A fluorescently labeled adenosine-oligoarginine conjugate (ARC), nanomolar bisubstrate analogue-type inhibitor of basophilic protein kinases PKA and PKC, readily enters cells of different origin and localizes into cytoplasm and nucleus. Moreover, the biotinylated derivative of ARC is able to deliver avidin, a non-covalently attached protein cargo, into cells.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / analogs & derivatives*
  • Adenosine / chemistry*
  • Adenosine / metabolism*
  • Adenosine / pharmacology
  • Arginine / analogs & derivatives*
  • Arginine / chemistry
  • Arginine / metabolism*
  • Arginine / pharmacology
  • Avidin / metabolism*
  • Biotinylation
  • Cell Membrane / metabolism*
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / metabolism*
  • Enzyme Inhibitors / pharmacology
  • Fluorescent Dyes
  • Humans
  • Molecular Structure
  • Protein Kinase Inhibitors*
  • Protein Transport
  • Temperature
  • Tumor Cells, Cultured

Substances

  • Enzyme Inhibitors
  • Fluorescent Dyes
  • Protein Kinase Inhibitors
  • Avidin
  • Arginine
  • Adenosine