β2-Adrenoceptor agonist-induced RGS2 expression is a genomic mechanism of bronchoprotection that is enhanced by glucocorticoids

Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19713-8. doi: 10.1073/pnas.1110226108. Epub 2011 Nov 11.

Abstract

In asthma and chronic obstructive pulmonary disease, activation of G(q)-protein-coupled receptors causes bronchoconstriction. In each case, the management of moderate-to-severe disease uses inhaled corticosteroid (glucocorticoid)/long-acting β(2)-adrenoceptor agonist (LABA) combination therapies, which are more efficacious than either monotherapy alone. In primary human airway smooth muscle cells, glucocorticoid/LABA combinations synergistically induce the expression of regulator of G-protein signaling 2 (RGS2), a GTPase-activating protein that attenuates G(q) signaling. Functionally, RGS2 reduced intracellular free calcium flux elicited by histamine, methacholine, leukotrienes, and other spasmogens. Furthermore, protection against spasmogen-increased intracellular free calcium, following treatment for 6 h with LABA plus corticosteroid, was dependent on RGS2. Finally, Rgs2-deficient mice revealed enhanced bronchoconstriction to spasmogens and an absence of LABA-induced bronchoprotection. These data identify RGS2 gene expression as a genomic mechanism of bronchoprotection that is induced by glucocorticoids plus LABAs in human airway smooth muscle and provide a rational explanation for the clinical efficacy of inhaled corticosteroid (glucocorticoid)/LABA combinations in obstructive airways diseases.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic beta-2 Receptor Agonists / pharmacology*
  • Albuterol / analogs & derivatives
  • Albuterol / pharmacology
  • Animals
  • Blotting, Western
  • Bronchoconstriction / drug effects*
  • Bronchoconstriction / genetics
  • Bronchoconstriction / physiology
  • Budesonide / pharmacology
  • Calcium / metabolism
  • Cell Line
  • Cells, Cultured
  • Dexamethasone / pharmacology
  • Drug Synergism
  • Ethanolamines / pharmacology
  • Formoterol Fumarate
  • Gene Expression / drug effects
  • Glucocorticoids / pharmacology*
  • Humans
  • Lung / cytology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Muscle, Smooth / cytology
  • Muscle, Smooth / drug effects
  • Muscle, Smooth / physiology
  • Myocytes, Smooth Muscle / drug effects
  • Myocytes, Smooth Muscle / metabolism
  • RGS Proteins / genetics*
  • RGS Proteins / metabolism
  • RNA Interference
  • Reverse Transcriptase Polymerase Chain Reaction
  • Salmeterol Xinafoate

Substances

  • Adrenergic beta-2 Receptor Agonists
  • Ethanolamines
  • Glucocorticoids
  • RGS Proteins
  • RGS2 protein, human
  • Rgs2 protein, mouse
  • Budesonide
  • Salmeterol Xinafoate
  • Dexamethasone
  • Albuterol
  • Calcium
  • Formoterol Fumarate