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
  • View Affiliations

  • Published online on: April 1, 2000     https://doi.org/10.3892/ijmm.5.4.335
  • Pages: 335-375
Metrics: Total Views: 0 (Spandidos Publications: | PMC Statistics: )
Total PDF Downloads: 0 (Spandidos Publications: | PMC Statistics: )


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.

Related Articles

Journal Cover

Apr 2000
Volume 5 Issue 4

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

Sign up for eToc alerts

Recommend to Library

Copy and paste a formatted citation
x
Spandidos Publications style
Usui H, Nishiyama M, Moroi K, Shibasaki T, Zhou J, Ishida J, Fukamizu A, Haga T, Sekiya S, Kimura S, Kimura S, et al: RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.. Int J Mol Med 5: 335-375, 2000
APA
Usui, H., Nishiyama, M., Moroi, K., Shibasaki, T., Zhou, J., Ishida, J. ... 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, 335-375. https://doi.org/10.3892/ijmm.5.4.335
MLA
Usui, H., Nishiyama, M., Moroi, K., Shibasaki, T., Zhou, J., Ishida, J., Fukamizu, A., Haga, T., Sekiya, S., Kimura, S."RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.". International Journal of Molecular Medicine 5.4 (2000): 335-375.
Chicago
Usui, H., Nishiyama, M., Moroi, K., Shibasaki, T., Zhou, J., Ishida, J., Fukamizu, A., Haga, T., Sekiya, S., Kimura, S."RGS domain in the amino-terminus of G protein-coupled receptor kinase 2 inhibits Gq-mediated signaling.". International Journal of Molecular Medicine 5, no. 4 (2000): 335-375. https://doi.org/10.3892/ijmm.5.4.335