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Keywords:

  • anticancer agents;
  • ERK;
  • kinase inhibitors;
  • protein–protein interaction;
  • small molecules
Thumbnail image of graphical abstract

David and Goliath: Small-molecule inhibitors of the ERK signaling pathway (shown) and their potential as novel antitumor agents are discussed in detail within this Minireview. Specifically, the direct and indirect inhibition of ERK through ATP-competitive and non-ATP-competitive modes of action is highlighted.