Structure and functional roles of Epac2 (Rapgef4)

Gene. 2016 Jan 10;575(2 Pt 3):577-83. doi: 10.1016/j.gene.2015.09.029. Epub 2015 Sep 24.

Abstract

Epac (exchange protein activated by cyclic-AMP) 2 is a direct target of 3'-5'-cyclic adenosine monophosphate (cAMP) and is involved in cAMP-mediated signal transduction through activation of the Ras-like small GTPase Rap. Crystallographic analyses revealed that activation of Epac2 by cAMP is accompanied by dynamic structural changes. Epac2 is expressed mainly in brain, neuroendocrine and endocrine tissues, and is involved in diverse cellular functions in the tissues. In this review, we summarize the structure and function of Epac2. We also discuss the physiological and pathophysiological roles of Epac2, and the possibility of Epac2 as a therapeutic target.

Keywords: Epac2; Rap; cAMP.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Brain / metabolism
  • Cyclic AMP / metabolism*
  • Endocrine System / metabolism
  • Guanine Nucleotide Exchange Factors / chemistry*
  • Guanine Nucleotide Exchange Factors / metabolism*
  • Humans
  • Myocardium / metabolism
  • Protein Conformation
  • Signal Transduction
  • ras Proteins / metabolism

Substances

  • Guanine Nucleotide Exchange Factors
  • RAPGEF4 protein, human
  • Cyclic AMP
  • ras Proteins