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Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma.

Publication ,  Journal Article
Lodowski, DT; Pitcher, JA; Capel, WD; Lefkowitz, RJ; Tesmer, JJG
Published in: Science
May 23, 2003

The phosphorylation of heptahelical receptors by heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptor kinases (GRKs) is a universal regulatory mechanism that leads to desensitization of G protein signaling and to the activation of alternative signaling pathways. We determined the crystallographic structure of bovine GRK2 in complex with G protein beta1gamma2 subunits. Our results show how the three domains of GRK2-the RGS (regulator of G protein signaling) homology, protein kinase, and pleckstrin homology domains-integrate their respective activities and recruit the enzyme to the cell membrane in an orientation that not only facilitates receptor phosphorylation, but also allows for the simultaneous inhibition of signaling by Galpha and Gbetagamma subunits.

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Published In

Science

DOI

EISSN

1095-9203

Publication Date

May 23, 2003

Volume

300

Issue

5623

Start / End Page

1256 / 1262

Location

United States

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Signal Transduction
  • Protein Structure, Tertiary
  • Protein Structure, Secondary
  • Protein Structure, Quaternary
  • Protein Conformation
  • Protein Binding
  • Phosphorylation
  • Molecular Sequence Data
  • Models, Molecular
 

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Lodowski, D. T., Pitcher, J. A., Capel, W. D., Lefkowitz, R. J., & Tesmer, J. J. G. (2003). Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma. Science, 300(5623), 1256–1262. https://doi.org/10.1126/science.1082348
Lodowski, David T., Julie A. Pitcher, W Darrell Capel, Robert J. Lefkowitz, and John J. G. Tesmer. “Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma.Science 300, no. 5623 (May 23, 2003): 1256–62. https://doi.org/10.1126/science.1082348.
Lodowski DT, Pitcher JA, Capel WD, Lefkowitz RJ, Tesmer JJG. Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma. Science. 2003 May 23;300(5623):1256–62.
Lodowski, David T., et al. “Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma.Science, vol. 300, no. 5623, May 2003, pp. 1256–62. Pubmed, doi:10.1126/science.1082348.
Lodowski DT, Pitcher JA, Capel WD, Lefkowitz RJ, Tesmer JJG. Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma. Science. 2003 May 23;300(5623):1256–1262.
Journal cover image

Published In

Science

DOI

EISSN

1095-9203

Publication Date

May 23, 2003

Volume

300

Issue

5623

Start / End Page

1256 / 1262

Location

United States

Related Subject Headings

  • beta-Adrenergic Receptor Kinases
  • Signal Transduction
  • Protein Structure, Tertiary
  • Protein Structure, Secondary
  • Protein Structure, Quaternary
  • Protein Conformation
  • Protein Binding
  • Phosphorylation
  • Molecular Sequence Data
  • Models, Molecular