Evidence map›Paper›PMID 22700696›Full record

ReviewMolecular pharmacology2012

Ubiquitination of G protein-coupled receptors: functional implications and drug discovery.

Michael R Dores, JoAnn Trejo

Open access · bronzeAbstract readReview
In one paragraph

Review in Molecular pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
2.1field-weighted citation impact, top 12% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

22 citing papers in PubMed, 49 citations in OpenAlex.

  1. Proteasomal-dependent endothelial P2YPurinergic signalling · 2026
    Article
  2. Article
  3. Review
  4. Mechanisms and Regulation of Neuronal GABACurrent topics in behavioral neurosciences · 2022
    Review
  5. Review
  6. Article
  7. Review
  8. Article
  9. Article
  10. Article
  11. Diversity of structure and function of GABAProceedings of the Japan Academy. Series B, Physical and biological sciences · 2018
    Review
  12. Review
  13. Regulation of G Protein-Coupled Receptors by Ubiquitination.International journal of molecular sciences · 2017
    Review
  14. Novel Structural Approaches to Study GPCR Regulation.International journal of molecular sciences · 2016
    Review
  15. Article
  16. Review
  17. Postendocytic Sorting of Adrenergic and Opioid Receptors: New Mechanisms and Functions.Progress in molecular biology and translational science · 2015
    Review
  18. Regulation of GPCR Trafficking by Ubiquitin.Progress in molecular biology and translational science · 2015
    Review
  19. Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

2 authors at 1 institution in 1 country.

Michael R DoresDepartment of Pharmacology, University of California, San Diego, 9500 Gilman Dr., Biomedical Sciences Building, Room 3044A, La Jolla, CA 92093, USA.
JoAnn Trejo
University of California, San Diego · US

Funding

UCSD/SDSU IRACDAK12GM068524 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TREJO, JOANN · 2003 to 2025
$24.4M
Training In Cardiovascular Physiology & PharmacologyT32HL007444 · NHLBI · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI Ju Chen, Robert Scott Ross · 1985 to 2026
$11.1M
Regulation of Protease-activated Receptor-1 SignalingR01HL073328 · NHLBI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI TREJO, JOANN · 2004 to 2012
$3.6M
Mechanisms Regulating GPCR TraffickingR01GM090689 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI TREJO, JOANN · 2010 to 2018
$2.9M
NHLBI NIH HHS R01 HL073328NHLBI NIH HHS R01-HL073328NHLBI NIH HHS T32 HL007444NIGMS NIH HHS K12 GM068524NIGMS NIH HHS R01 GM090689NIGMS NIH HHS R01-GM090689
6 · The paper itself

Abstract

G protein-coupled receptors (GPCRs) comprise the largest and most diverse family of signaling receptors and control a vast array of physiological responses. Modulating the signaling responses of GPCRs therapeutically is important for the treatment of various diseases, and discovering new aspects of GPCR signal regulation is critical for future drug development. Post-translational modifications are integral to the regulation of GPCR function. In addition to phosphorylation, many GPCRs are reversibly modified with ubiquitin. Ubiquitin is covalently attached to lysine residues within the cytoplasmic domains of GPCRs by ubiquitin ligases and removed by ubiquitin-specific proteases. In many cases, ubiquitin functions as a sorting signal that facilitates trafficking of mammalian GPCRs from endosomes to lysosomes for degradation, but not all GPCRs use this pathway. Moreover, there are distinct types of ubiquitin conjugations that are known to serve diverse functions in controlling a wide range of cellular processes, suggesting broad roles for GPCR ubiquitination. In this review, we highlight recent studies that illustrate various roles for ubiquitin in regulation of GPCR function. Ubiquitination is known to target many GPCRs for lysosomal degradation, and current studies now indicate that basal ubiquitination, deubiquitination, and transubiquitination of certain GPCRs are important for controlling cell surface expression and cellular responsiveness. In addition, novel functions for ubiquitin in regulation of GPCR dimers and in mediating differential GPCR regulation induced by biased agonists have been reported. We will discuss the implications of these new discoveries for ubiquitin regulation of GPCR function in the context of drug development.

Indexed as

Drug DiscoveryUbiquitinationAnimalsCell MembraneEndoplasmic ReticulumHumansLysosomesReceptors, G-Protein-CoupledSignal TransductionUbiquitinReceptors, G-Protein-CoupledUbiquitin

Identifiers

PMID22700696
PMCPMC3463220
OpenAlexW2137589440

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.