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alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro.

Publication ,  Journal Article
Freeman, JL; Pitcher, JA; Li, X; Bennett, V; Lefkowitz, RJ
Published in: FEBS Lett
May 19, 2000

G protein-coupled receptor kinases (GRKs) phosphorylate G protein-coupled receptors, thereby terminating receptor signaling. Herein we report that alpha-actinin potently inhibits all GRK family members. In addition, calcium-bound calmodulin and phosphatidylinositol 4,5-bisphosphate (PIP2), two regulators of GRK activity, coordinate with alpha-actinin to modulate substrate specificity of the GRKs. In the presence of calmodulin and alpha-actinin, GRK5 phosphorylates soluble, but not membrane-incorporated substrates. In contrast, in the presence of PIP2 and alpha-actinin, GRK5 phosphorylates membrane-incorporated, but not soluble substrates. Thus, modulation of alpha-actinin-mediated inhibition of GRKs by PIP2 and calmodulin has profound effects on both GRK activity and substrate specificity.

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Published In

FEBS Lett

DOI

ISSN

0014-5793

Publication Date

May 19, 2000

Volume

473

Issue

3

Start / End Page

280 / 284

Location

England

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Substrate Specificity
  • Rhodopsin
  • Protein Serine-Threonine Kinases
  • Phosphorylation
  • Phosphatidylinositol 4,5-Diphosphate
  • G-Protein-Coupled Receptor Kinase 5
  • Cyclic AMP-Dependent Protein Kinases
  • Chickens
  • Caseins
 

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Freeman, J. L., Pitcher, J. A., Li, X., Bennett, V., & Lefkowitz, R. J. (2000). alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro. FEBS Lett, 473(3), 280–284. https://doi.org/10.1016/s0014-5793(00)01543-x
Freeman, J. L., J. A. Pitcher, X. Li, V. Bennett, and R. J. Lefkowitz. “alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro.FEBS Lett 473, no. 3 (May 19, 2000): 280–84. https://doi.org/10.1016/s0014-5793(00)01543-x.
Freeman JL, Pitcher JA, Li X, Bennett V, Lefkowitz RJ. alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro. FEBS Lett. 2000 May 19;473(3):280–4.
Freeman, J. L., et al. “alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro.FEBS Lett, vol. 473, no. 3, May 2000, pp. 280–84. Pubmed, doi:10.1016/s0014-5793(00)01543-x.
Freeman JL, Pitcher JA, Li X, Bennett V, Lefkowitz RJ. alpha-Actinin is a potent regulator of G protein-coupled receptor kinase activity and substrate specificity in vitro. FEBS Lett. 2000 May 19;473(3):280–284.
Journal cover image

Published In

FEBS Lett

DOI

ISSN

0014-5793

Publication Date

May 19, 2000

Volume

473

Issue

3

Start / End Page

280 / 284

Location

England

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Substrate Specificity
  • Rhodopsin
  • Protein Serine-Threonine Kinases
  • Phosphorylation
  • Phosphatidylinositol 4,5-Diphosphate
  • G-Protein-Coupled Receptor Kinase 5
  • Cyclic AMP-Dependent Protein Kinases
  • Chickens
  • Caseins