Dimers of G-protein coupled receptors as versatile storage and response units

Michael S. Parker, Renu Sah, Ambikaipakan Balasubramaniam, Edwards A. Park, Floyd R. Sallee, Steven L. Parker

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

The status and use of transmembrane, extracellular and intracellular domains in oligomerization of heptahelical G-protein coupled receptors (GPCRs) are reviewed and for transmembrane assemblies also supplemented by new experimental evidence. The transmembrane-linked GPCR oligomers typically have as the minimal unit an asymmetric ~180 kDa pentamer consisting of receptor homodimer or heterodimer and a G-protein αβγ subunit heterotrimer. With neuropeptide Y (NPY) receptors, this assembly is converted to ~90 kDa receptor monomer-Gα complex by receptor and Gα agonists, and dimers/heteropentamers are depleted by neutralization of Gαi subunits by pertussis toxin. Employing gradient centrifugation, quantification and other characterization of GPCR dimers at the level of physically isolated and identified heteropentamers is feasible with labeled agonists that do not dissociate upon solubilization. This is demonstrated with three neuropeptide Y (NPY) receptors and could apply to many receptors that use large peptidic agonists.

Original languageEnglish (US)
Pages (from-to)4856-4877
Number of pages22
JournalInternational journal of molecular sciences
Volume15
Issue number3
DOIs
StatePublished - Mar 19 2014

Fingerprint

G-Protein-Coupled Receptors
Dimers
Neuropeptide Y Receptors
dimers
proteins
Proteins
Oligomerization
Centrifugation
Pertussis Toxin
Protein Subunits
GTP-Binding Proteins
Oligomers
Monomers
oligomers
assemblies
monomers
assembly
Neuropeptides
gradients

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

Cite this

Dimers of G-protein coupled receptors as versatile storage and response units. / Parker, Michael S.; Sah, Renu; Balasubramaniam, Ambikaipakan; Park, Edwards A.; Sallee, Floyd R.; Parker, Steven L.

In: International journal of molecular sciences, Vol. 15, No. 3, 19.03.2014, p. 4856-4877.

Research output: Contribution to journalArticle

Parker, Michael S. ; Sah, Renu ; Balasubramaniam, Ambikaipakan ; Park, Edwards A. ; Sallee, Floyd R. ; Parker, Steven L. / Dimers of G-protein coupled receptors as versatile storage and response units. In: International journal of molecular sciences. 2014 ; Vol. 15, No. 3. pp. 4856-4877.
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