Exchange protein directly activated by cAMP plays a critical role in bacterial invasion during fatal rickettsioses

Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19615-20. doi: 10.1073/pnas.1314400110. Epub 2013 Nov 11.

Abstract

Rickettsiae are responsible for some of the most devastating human infections. A high infectivity and severe illness after inhalation make some rickettsiae bioterrorism threats. We report that deletion of the exchange protein directly activated by cAMP (Epac) gene, Epac1, in mice protects them from an ordinarily lethal dose of rickettsiae. Inhibition of Epac1 suppresses bacterial adhesion and invasion. Most importantly, pharmacological inhibition of Epac1 in vivo using an Epac-specific small-molecule inhibitor, ESI-09, completely recapitulates the Epac1 knockout phenotype. ESI-09 treatment dramatically decreases the morbidity and mortality associated with fatal spotted fever rickettsiosis. Our results demonstrate that Epac1-mediated signaling represents a mechanism for host-pathogen interactions and that Epac1 is a potential target for the prevention and treatment of fatal rickettsioses.

Keywords: Epac inhibitor; cyclic AMP; prophylaxis; rickettsial infection; therapeutics.

Publication types

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

MeSH terms

  • Animals
  • Bacterial Adhesion / drug effects*
  • Bacterial Adhesion / physiology
  • Guanine Nucleotide Exchange Factors / antagonists & inhibitors*
  • Guanine Nucleotide Exchange Factors / metabolism
  • Host-Pathogen Interactions / physiology*
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Hydrazones / pharmacology*
  • Hydrazones / therapeutic use
  • Immunohistochemistry
  • Isoxazoles / pharmacology*
  • Isoxazoles / therapeutic use
  • Male
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Rickettsia Infections / drug therapy*
  • Rickettsia Infections / metabolism
  • Signal Transduction / physiology*

Substances

  • 3-(5-tert-butylisoxazol-3-yl)-2-((3-chlorophenyl)hydrazono)-3-oxopropionitrile
  • Epac protein, mouse
  • Guanine Nucleotide Exchange Factors
  • Hydrazones
  • Isoxazoles