Identification in human airways smooth muscle cells of the prostanoid receptor and signalling pathway through which PGE2 inhibits the release of GM-CSF

Br J Pharmacol. 2004 Apr;141(7):1141-50. doi: 10.1038/sj.bjp.0705716. Epub 2004 Mar 15.

Abstract

1. The prostanoid receptor(s) on human airways smooth muscle (HASM) cells that mediates the inhibitory effect of PGE(2) on interleukin (IL)-1 beta-induced granulocyte/macrophage colony-stimulating factor (GM-CSF) release has been classified. 2. IL-1 beta evoked the release of GM-CSF from HASM cells, which was suppressed by PGE(2), 16,16-dimethyl PGE(2) (nonselective), misoprostol (EP(2)/EP(3)-selective), ONO-AE1-259 and butaprost (both EP(2)-selective) with pIC(50) values of 8.61, 7.13, 5.64, 8.79 and 5.43, respectively. EP-receptor agonists that have selectivity for the EP(1)-(17-phenyl-omega-trinor PGE(2)) and EP(3)-receptor (sulprostone) subtypes as well as cicaprost (IP-selective), PGD(2), PGF(2 alpha) and U-46619 (TP-selective) were poorly active or inactive at concentrations up to 10 microM. 3. AH 6809, a drug that can be used to selectively block EP(2)-receptors in HASM cells, antagonised the inhibitory effect of PGE(2), 16,16-dimethyl PGE(2) and ONO-AE1-259 with apparent pA(2) values of 5.85, 6.09 and 6.1 respectively. In contrast, the EP(4)-receptor antagonists, AH 23848B and L-161,982, failed to displace to the right the concentration-response curves that described the inhibition of GM-CSF release evoked by PGE(2) and ONO-AE1-259. 4. Inhibition of GM-CSF release by PGE(2) and 8-Br-cAMP was abolished in cells infected with an adenovirus vector encoding an inhibitor protein of cAMP-dependent protein kinase (PKA) but not by H-89, a purported small molecule inhibitor of PKA. 5. We conclude that prostanoid receptors of the EP(2)-subtype mediate the inhibitory effect of PGE(2) on GM-CSF release from HASM cells by recruiting a PKA-dependent pathway. In addition, the data illustrate that caution should be exercised when using H-89 in studies designed to assess the role of PKA in biological processes.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid / pharmacology
  • 8-Bromo Cyclic Adenosine Monophosphate / pharmacology
  • Adenoviridae / genetics
  • Adenoviridae / metabolism
  • Adolescent
  • Adult
  • Aged
  • Alprostadil / analogs & derivatives*
  • Alprostadil / pharmacology
  • Cell Survival
  • Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors
  • Cyclic AMP-Dependent Protein Kinases / drug effects
  • Cyclic AMP-Dependent Protein Kinases / genetics
  • Dinoprostone / analogs & derivatives*
  • Dinoprostone / pharmacology
  • Enzyme Inhibitors / pharmacology
  • Female
  • Gene Expression / drug effects
  • Genetic Vectors / genetics
  • Granulocyte Colony-Stimulating Factor / antagonists & inhibitors
  • Granulocyte-Macrophage Colony-Stimulating Factor / antagonists & inhibitors
  • Granulocyte-Macrophage Colony-Stimulating Factor / metabolism*
  • Humans
  • Indomethacin / pharmacology
  • Interleukin-1 / antagonists & inhibitors
  • Interleukin-1 / pharmacology
  • Isoquinolines / pharmacology
  • Male
  • Middle Aged
  • Misoprostol / pharmacology
  • Myocytes, Smooth Muscle / drug effects*
  • Myocytes, Smooth Muscle / metabolism
  • Prostaglandins E, Synthetic / chemistry
  • Prostaglandins E, Synthetic / metabolism
  • Prostaglandins E, Synthetic / pharmacology*
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Receptors, Prostaglandin E / antagonists & inhibitors
  • Receptors, Prostaglandin E / classification*
  • Receptors, Prostaglandin E / drug effects*
  • Receptors, Prostaglandin E / physiology
  • Receptors, Prostaglandin E, EP2 Subtype
  • Receptors, Prostaglandin E, EP4 Subtype
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*
  • Sulfonamides / pharmacology
  • Trachea / cytology
  • Xanthones / pharmacology

Substances

  • 9-deoxy-9-chloro-15-deoxy-16-hydroxy-17,17-trimethylene-19,20-didehydroprostaglandin E2
  • Enzyme Inhibitors
  • Interleukin-1
  • Isoquinolines
  • PTGER2 protein, human
  • PTGER4 protein, human
  • Prostaglandins E, Synthetic
  • Protein Isoforms
  • Receptors, Prostaglandin E
  • Receptors, Prostaglandin E, EP2 Subtype
  • Receptors, Prostaglandin E, EP4 Subtype
  • Sulfonamides
  • Xanthones
  • Misoprostol
  • Granulocyte Colony-Stimulating Factor
  • 8-Bromo Cyclic Adenosine Monophosphate
  • 6-isopropoxy-9-oxoxanthene-2-carboxylic acid
  • 15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
  • Granulocyte-Macrophage Colony-Stimulating Factor
  • Cyclic AMP-Dependent Protein Kinases
  • Alprostadil
  • butaprost
  • Dinoprostone
  • N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide
  • Indomethacin