Selective small-molecule EPAC activators

Biochem Soc Trans. 2019 Oct 31;47(5):1415-1427. doi: 10.1042/BST20190254.

Abstract

The cellular signalling enzymes, EPAC1 and EPAC2, have emerged as key intracellular sensors of the secondary messenger cyclic 3',5'-adenosine monophosphate (cyclic adenosine monophosphate) alongside protein kinase A. Interest has been galvanised in recent years thanks to the emergence of these species as potential targets for new cardiovascular disease therapies, including vascular inflammation and insulin resistance in vascular endothelial cells. We herein summarise the current state-of-the-art in small-molecule EPAC activity modulators, including cyclic nucleotides, sulphonylureas, and N-acylsulphonamides.

Keywords: cAMP; exchange proteins; signalling.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Guanine Nucleotide Exchange Factors / metabolism*
  • Humans
  • Ligands
  • Signal Transduction
  • Small Molecule Libraries / metabolism

Substances

  • Guanine Nucleotide Exchange Factors
  • Ligands
  • RAPGEF3 protein, human
  • RAPGEF4 protein, human
  • Small Molecule Libraries