RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.

  • Authors: H Usui, M Nishiyama, K Moroi, T Shibasaki, J Zhou, J Ishida, A Fukamizu, T Haga, S Sekiya, S Kimura
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  • Published online on: Saturday, April 1, 2000
  • Pages: 335-375
  • DOI: 10.3892/ijmm.5.4.335

Abstract

We have previously shown that not only G protein-coupled receptor kinase (GRK) 2, but also a catalytically inactive Lys220Trp GRK2 decreases endothelin (ET)-1-induced inositol 1,4,5-trisphosphate (IP3) formation, and demonstrated the presence of phosphorylation-independent desensitization mechanism. To clarify the role of GRK2 other than that as a kinase, we characterized an RGS (regulator of G protein signaling)-like domain in the amino-terminus of GRK2. Both GRK2(1-181) and GRK2(54-174) suppressed Ca2+ responses induced by angiotensin II (Ang II) and ET-1, and bound directly with Galphaq but not Galphas nor Galphai3 in the presence of GDP and AlF4-. These results demonstrate that GRK2 regulates Gq-mediated signaling negatively by direct interaction between its RGS domain and the transitional state of Galphaq, as well as through phosphorylation of activated receptors by its kinase domain.
Journal Cover

April 2000
Volume 5 Issue 4

Print ISSN: 1107-3756
Online ISSN:1791-244X

2012 Impact Factor: 1.957
Ranked #26/121 Medicine Research and Experimental
(total number of cites)

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APA
Usui, H., Nishiyama, M., Moroi, K., Shibasaki, T., Zhou, J., Ishida, J., Fukamizu, A., Haga, T., Sekiya, S., & Kimura, S. (2000). RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.. International Journal of Molecular Medicine, 5(4), 335-375.
MLA
Usui, Nishiyama, Moroi, Shibasaki, Zhou, Ishida, Fukamizu, Haga, Sekiya, and S Kimura. "RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.." International Journal of Molecular Medicine International Journal of Molecular Medicine 5.4 (2000): 335-375.
Chicago
Usui, Nishiyama, Moroi, Shibasaki, Zhou, Ishida, Fukamizu, Haga, Sekiya, and S Kimura. "RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.." International Journal of Molecular Medicine International Journal of Molecular Medicine 5 no. 4 (2000): 335-375.