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Am J Physiol Regul Integr Comp Physiol 280: R935-R946, 2001;
0363-6119/01 $5.00
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Vol. 280, Issue 4, R935-R946, April 2001

GRK3 mediates desensitization of CRF1 receptors: a potential mechanism regulating stress adaptation

Frank M. Dautzenberg1,2, Sandra Braun3, and Richard L. Hauger2,3

1 Pharma Division, Preclinical Research, F-Hoffmann-La Roche Ltd., CH-4070 Basel, Switzerland; 2 Department of Molecular Neuroendocrinology, Max-Planck-Institute for Experimental Medicine, 37075 Goettingen, Germany; and 3 Veterans Affairs Medical Center and Department of Psychiatry, University of California, San Diego, La Jolla, California 92093-0603

Potential G protein-coupled receptor kinase (GRK) and protein kinase A (PKA) mediation of homologous desensitization of corticotropin-releasing factor type 1 (CRF1) receptors was investigated in human retinoblastoma Y-79 cells. Inhibition of PKA activity by PKI5-22 or H-89 failed to attenuate homologous desensitization of CRF1 receptors, and direct activation of PKA by forskolin or dibutyryl cAMP failed to desensitize CRF-induced cAMP accumulation. However, treatment of permeabilized Y-79 cells with heparin, a nonselective GRK inhibitor, reduced homologous desensitization of CRF1 receptors by ~35%. Furthermore, Y-79 cell uptake of a GRK3 antisense oligonucleotide (ODN), but not of a random or mismatched ODN, reduced GRK3 mRNA expression by ~50% without altering GRK2 mRNA expression and inhibited homologous desensitization of CRF1 receptors by ~55%. Finally, Y-79 cells transfected with a GRK3 antisense cDNA construct exhibited an ~50% reduction in GRK3 protein expression and an ~65% reduction in homologous desensitization of CRF1 receptors. We conclude that GRK3 contributes importantly to the homologous desensitization of CRF1 receptors in Y-79 cells, a brain-derived cell line.

antisense; G protein-coupled receptor kinase; corticotropin-releasing factor type 1 receptor regulation; homologous and heterologous desensitization of the CRF1 receptor


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