Evidence map›Paper›PMID 36291552›Full record

ReviewBiomolecules2022

GPCRs in Intracellular Compartments: New Targets for Drug Discovery.

Irene Fasciani, Marco Carli, Francesco Petragnano, Francesco Colaianni, Gabriella Aloisi, Roberto Maggio, Marco Scarselli, Mario Rossi

Open access · goldAbstract readReview
In one paragraph

Review in Biomolecules, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.

0numbers the graph read from it
0cells of the map it votes in
29citing papers in PubMed
3.7field-weighted citation impact, top 5% 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

29 citing papers in PubMed, 44 citations in OpenAlex.

  1. Review
  2. The working lives of neuronal 5-HTRSC chemical biology · 2026
    Review
  3. Review
  4. β-Adrenergic Receptors: Not Always Outside-In.Physiology (Bethesda, Md.) · 2026
    Review
  5. Article
  6. Review
  7. Biased Signaling in Psychedelic Action.Annual review of pharmacology and toxicology · 2026
    Review
  8. Article
  9. Review
  10. Review
  11. Review
  12. Review
  13. Article
  14. Mitochondrial Localization and Function of Adenosine Receptors.International journal of biological sciences · 2025
    Article
  15. Article
  16. Article
  17. Article
  18. Class B1 GPCRs: insights into multireceptor pharmacology for the treatment of metabolic disease.American journal of physiology. Endocrinology and metabolism · 2024
    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

8 authors at 2 institutions in 1 country.

Irene FascianiDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.
Marco CarliDepartment of Translational Research on New Technologies in Medicine and Surgery, University of Pisa, 56126 Pisa, Italy.ORCID 0000-0003-1447-4947
Francesco PetragnanoDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.
Francesco ColaianniDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.
Gabriella AloisiDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.
Roberto MaggioDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.ORCID 0000-0003-4436-2356
Marco ScarselliDepartment of Translational Research on New Technologies in Medicine and Surgery, University of Pisa, 56126 Pisa, Italy.
Mario RossiDepartment of Biotechnological and Applied Clinical Sciences, University of L'Aquila, 67100 L'Aquila, Italy.ORCID 0000-0001-7004-0225
University of L'Aquila · ITUniversity of Pisa · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The architecture of eukaryotic cells is defined by extensive membrane-delimited compartments, which entails separate metabolic processes that would otherwise interfere with each other, leading to functional differences between cells. G protein-coupled receptors (GPCRs) are the largest class of cell surface receptors, and their signal transduction is traditionally viewed as a chain of events initiated from the plasma membrane. Furthermore, their intracellular trafficking, internalization, and recycling were considered only to regulate receptor desensitization and cell surface expression. On the contrary, accumulating data strongly suggest that GPCRs also signal from intracellular compartments. GPCRs localize in the membranes of endosomes, nucleus, Golgi and endoplasmic reticulum apparatuses, mitochondria, and cell division compartments. Importantly, from these sites they have shown to orchestrate multiple signals that regulate different cell pathways. In this review, we summarize the current knowledge of this fascinating phenomenon, explaining how GPCRs reach the intracellular sites, are stimulated by the endogenous ligands, and their potential physiological/pathophysiological roles. Finally, we illustrate several mechanisms involved in the modulation of the compartmentalized GPCR signaling by drugs and endogenous ligands. Understanding how GPCR signaling compartmentalization is regulated will provide a unique opportunity to develop novel pharmaceutical approaches to target GPCRs and potentially lead the way towards new therapeutic approaches.

Indexed as

Drug DiscoveryReceptors, G-Protein-CoupledLigandsPharmaceutical PreparationsReceptors, Cell SurfaceLigandsPharmaceutical PreparationsReceptors, Cell SurfaceReceptors, G-Protein-CoupledG protein-coupled receptorsmitochondrianuclear membrane

Identifiers

PMID36291552
PMCPMC9599219
OpenAlexW4296618669

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.