Compound C inhibits hypoxic activation of HIF-1 independent of AMPK

FEBS Lett. 2007 Dec 11;581(29):5727-31. doi: 10.1016/j.febslet.2007.11.038. Epub 2007 Nov 26.

Abstract

The key transcription factor that regulates the cellular responses to hypoxia is hypoxia inducible factor-1 (HIF-1). The signaling mechanisms that regulate the hypoxic activation of HIF-1 are not fully understood. Our objective here was to test whether AMP-activated kinase (AMPK) was an upstream regulator of HIF-1. Our results show that AMPK is not required for the hypoxic activation of HIF-1. Interestingly, the AMPK inhibitor, Compound C, inhibits the hypoxic activation of HIF-1 independent of AMPK. Furthermore, we demonstrate that Compound C functions as a repressor of HIF-1 by inhibiting respiration and suppressing mitochondrial generated ROS.

Publication types

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

MeSH terms

  • AMP-Activated Protein Kinases
  • Cell Hypoxia
  • Hypoxia-Inducible Factor 1 / antagonists & inhibitors
  • Hypoxia-Inducible Factor 1 / metabolism*
  • Mitochondria / metabolism
  • Multienzyme Complexes / metabolism*
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Serine-Threonine Kinases / metabolism*
  • Pyrazoles / pharmacology*
  • Pyrimidines / pharmacology*
  • Reactive Oxygen Species / metabolism

Substances

  • Hypoxia-Inducible Factor 1
  • Multienzyme Complexes
  • Protein Kinase Inhibitors
  • Pyrazoles
  • Pyrimidines
  • Reactive Oxygen Species
  • dorsomorphin
  • Protein Serine-Threonine Kinases
  • AMP-Activated Protein Kinases