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Research ArticleArticle

Cyclic AMP and Protein Kinase A Stimulate Cdc42: Role of A2 Adenosine Receptors in Human Mast Cells

Igor Feoktistov, Anna E. Goldstein and Italo Biaggioni
Molecular Pharmacology November 2000, 58 (5) 903-910; DOI: https://doi.org/10.1124/mol.58.5.903
Igor Feoktistov
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Anna E. Goldstein
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Italo Biaggioni
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Abstract

The functional activity of Cdc42 is known to be regulated by proteins that control its GDP/GTP-bound state. However, there is still limited information on how Cdc42 is controlled by G-protein-coupled receptors. Adenosine receptors belong to the G-protein-coupled receptor family of cell surface receptors. Human HMC-1 mast cells express the high-affinity A2A and the low-affinity A2B subtypes of adenosine receptors known to increase intracellular cAMP levels. We found that both subtypes of A2 adenosine receptors activate Cdc42 in HMC-1 cells. Furthermore, stimulation of adenylate cyclase with forskolin, or loading of HMC-1 with the cell-permeable cAMP analog 8-Br-cAMP, activated Cdc42. Stimulation of Cdc42 by cAMP was also observed in CHO-K1 and COS-7 cells. Protein kinase A (PKA)-mediated phosphorylation is likely involved in cAMP-dependent Cdc42 activation, because transient expression of the PKA catalytic subunit in COS-7 cells activated Cdc42. Inhibition of protein phosphatases 1 and 2A with calyculin A potentiated the effects of 5′-N-ethylcarboxamidoadenosine and 8-Br-cAMP, whereas the selective PKA inhibitor H-89 reversed the activation of Cdc42. We demonstrated that Cdc42 is a poor substrate for PKA phosphorylation in vitro and in intact cells. Our data suggest that PKA does not phosphorylate Cdc42 directly. Instead, the proteins that modulate the GDP/GTP-bound state of Cdc42 may be the primary targets of PKA phosphorylation.

Footnotes

    • Received June 2, 2000.
    • Accepted July 31, 2000.
  • Send reprint requests to: Igor Feoktistov, M.D., Ph.D., Division of Cardiology, Department of Medicine, Rm. 315, MRB II, Vanderbilt University, Nashville, TN 37232-6300. E-mail:Igor.Feoktistov{at}mcmail.vanderbilt.edu

  • Supported by National Institutes of Health Grants R29HL55596 and HL56693.

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 58 (5)
Molecular Pharmacology
Vol. 58, Issue 5
1 Nov 2000
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Research ArticleArticle

Cyclic AMP and Protein Kinase A Stimulate Cdc42: Role of A2 Adenosine Receptors in Human Mast Cells

Igor Feoktistov, Anna E. Goldstein and Italo Biaggioni
Molecular Pharmacology November 1, 2000, 58 (5) 903-910; DOI: https://doi.org/10.1124/mol.58.5.903

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Research ArticleArticle

Cyclic AMP and Protein Kinase A Stimulate Cdc42: Role of A2 Adenosine Receptors in Human Mast Cells

Igor Feoktistov, Anna E. Goldstein and Italo Biaggioni
Molecular Pharmacology November 1, 2000, 58 (5) 903-910; DOI: https://doi.org/10.1124/mol.58.5.903
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