The angiotensin type 1 receptor activates extracellular signal-regulated kinases 1 and 2 by G protein-dependent and -independent pathways in cardiac myocytes and langendorff-perfused hearts

Basic Clin Pharmacol Toxicol. 2007 May;100(5):289-95. doi: 10.1111/j.1742-7843.2007.00063.x.

Abstract

The angiotensin II (AngII) type 1 receptor (AT(1)R) has been shown to activate extracellular signal-regulated kinases 1 and 2 (ERK1/2) through G proteins or G protein-independently through beta-arrestin2 in cellular expression systems. As activation mechanisms may greatly influence the biological effects of ERK1/2 activity, differential activation of the AT(1)R in its native cellular context could have important biological and pharmacological implications. To examine if AT(1)R activates ERK1/2 by G protein-independent mechanisms in the heart, we used the [Sar(1), Ile(4), Ile(8)]-AngII ([SII] AngII) analogue in native preparations of cardiac myocytes and beating hearts. We found that [SII] AngII does not activate G(q)-coupling, yet stimulates the beta-arrestin2-dependent ERK1/2. The G(q)-activated pool of ERK1/2 rapidly translocates to the nucleus, while the beta-arrestin2-scaffolded pool remains in the cytosol. Similar biased agonism was achieved in Langendorff-perfused hearts, where both agonists elicit ERK1/2 phosphorylation, but [SII] AngII induces neither inotropic nor chronotropic effects.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-Sarcosine-8-Isoleucine Angiotensin II / pharmacology
  • Angiotensin II / pharmacology
  • Animals
  • Animals, Newborn
  • Arrestins / metabolism
  • Cell Nucleus / enzymology
  • Cells, Cultured
  • Coronary Circulation / drug effects
  • Cytosol / metabolism
  • GTP-Binding Proteins / metabolism*
  • Heart Rate / drug effects
  • Heart Ventricles / drug effects
  • Heart Ventricles / metabolism
  • Male
  • Mitogen-Activated Protein Kinase 1 / biosynthesis*
  • Mitogen-Activated Protein Kinase 3 / biosynthesis*
  • Muscle Contraction / drug effects
  • Myocardium / enzymology*
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / enzymology*
  • Perfusion
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Receptor, Angiotensin, Type 1 / metabolism*
  • beta-Arrestins

Substances

  • Arrestins
  • Receptor, Angiotensin, Type 1
  • beta-Arrestins
  • Angiotensin II
  • 1-Sarcosine-8-Isoleucine Angiotensin II
  • Mitogen-Activated Protein Kinase 1
  • Mitogen-Activated Protein Kinase 3
  • GTP-Binding Proteins