Evidence map›Paper›PMID 21158738›Full record

ReviewThe Biochemical journal2011

Exploring a role for heteromerization in GPCR signalling specificity.

Raphael Rozenfeld, Lakshmi A Devi

Abstract readReview
In one paragraph

Review in The Biochemical journal, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.

0numbers the graph read from it
0cells of the map it votes in
65citing papers in PubMed
–field-weighted citation impact
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

65 citing papers in PubMed.

  1. Review
  2. Review
  3. Review
  4. Design principles of ciliary signaling.Journal of cell science · 2025
    Review
  5. Review
  6. Is the Neuropeptide PEN a Ligand of GPR83?International journal of molecular sciences · 2023
    Article
  7. Review
  8. Article
  9. Article
  10. Review
  11. Article
  12. Article
  13. Review
  14. Review
  15. Review
  16. Article
  17. Article
  18. Article
  19. Article
  20. Article

5 more citing papers are in PubMed but not listed here.

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.

Raphael RozenfeldDepartment of Pharmacology and Systems Therapeutics, Mount Sinai School of Medicine, New York, NY 10029, USA.
Lakshmi A Devi

Funding

System Biology Center in New YorkP50GM071558 · NIGMS · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZAPH, SUSANA NEVES · 2007 to 2017
$22.8M
Regulation Of Opioid Receptor Signaling by Endogenous PeptidesR01DA008863 · NIDA · NEW YORK UNIVERSITY SCHOOL OF MEDICINE · PI Lakshmi A Devi, Elyssa Margolis · 1995 to 2026
$6.1M
Post-translational Regulation of Opioid and Cannabinoid Receptors.R37DA008863 · NIDA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI DEVI, LAKSHMI A · 2012 to 2021
$4.6M
Project 2P20AA017067 · NIAAA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI FIEL, MARIA ISABEL · 2008 to 2012
$2.5M
POST-TRANSLATIONAL REGULATION OF OPIOID RECEPTORSK05DA019521 · NIDA · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI DEVI, LAKSHMI A · 2005 to 2014
$1.2M
Post-translational regulation of opioid receptorsR56DA008863 · NIDA · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI DEVI, LAKSHMI A · 2007 to 2007
$381k
NIAAA NIH HHS AA017067NIAAA NIH HHS P20 AA017067NIDA NIH HHS DA01952NIDA NIH HHS DA08863NIDA NIH HHS K05 DA019521NIDA NIH HHS R01 DA008863NIDA NIH HHS R37 DA008863NIDA NIH HHS R56 DA008863NIGMS NIH HHS GM071558NIGMS NIH HHS P50 GM071558Telethon GGP06166
6 · The paper itself

Abstract

The critical involvement of GPCRs (G-protein-coupled receptors) in nearly all physiological processes, and the presence of these receptors at the interface between the extracellular and the intracellular milieu, has positioned these receptors as pivotal therapeutic targets. Although a large number of drugs targeting GPCRs are currently available, significant efforts have been directed towards understanding receptor properties, with the goal of identifying and designing improved receptor ligands. Recent advances in GPCR pharmacology have demonstrated that different ligands binding to the same receptor can activate discrete sets of downstream effectors, a phenomenon known as 'ligand-directed signal specificity', which is currently being explored for drug development due to its potential therapeutic advantage. Emerging studies suggest that GPCR responses can also be modulated by contextual factors, such as interactions with other GPCRs. Association between different GPCR types leads to the formation of complexes, or GPCR heteromers, with distinct and unique signalling properties. Some of these heteromers activate discrete sets of signalling effectors upon activation by the same ligand, a phenomenon termed 'heteromer-directed signalling specificity'. This has been shown to be involved in the physiological role of receptors and, in some cases, in disease-specific dysregulation of a receptor effect. Hence targeting GPCR heteromers constitutes an emerging strategy to select receptor-specific responses and is likely to be useful in achieving specific beneficial therapeutic effects.

Indexed as

AnimalsDrug Delivery SystemsHumansProtein MultimerizationReceptors, G-Protein-CoupledSignal TransductionReceptors, G-Protein-Coupled

Identifiers

PMID21158738
PMCPMC3115900

What OpenQuestion holds

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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.