Evidence map›Paper›PMID 38594257›Full record

ReviewSignal transduction and targeted therapy2024

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery.

Mingyang Zhang, Ting Chen, Xun Lu, Xiaobing Lan, Ziqiang Chen, Shaoyong Lu

Open access · goldAbstract readReview
In one paragraph

Review in Signal transduction and targeted therapy, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 249 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
249citing papers in PubMed, 1 pooled it
83.7field-weighted citation impact, top 1% 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

249 citing papers in PubMed, 1 synthesis or guideline pooled it, 359 citations in OpenAlex.

  1. Cortical 5-HTMolecular psychiatry · 2025
    Pooled it
  2. Trial
  3. Article
  4. Review
  5. The GPCRDiabetologia · 2026
    Article
  6. Review
  7. Article
  8. Article
  9. A Sesquiterpenoid fromInternational journal of molecular sciences · 2026
    Article
  10. Imaging transcriptomics in basal cell carcinoma: Coupling in vivo tumor morphology with gene expression.JID innovations : skin science from molecules to population health · 2026
    Article
  11. Review
  12. Article
  13. Article
  14. Article
  15. Advances in Cyclic Peptides Targeting G Protein-Coupled Receptors.Chembiochem : a European journal of chemical biology · 2026
    Review
  16. Article
  17. Article
  18. Article
  19. Review
  20. Review

189 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

6 authors at 4 institutions in 1 country.

Mingyang Zhang *Key Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan, 750004, China.
Ting Chen *Department of Cardiology, Changzheng Hospital, Affiliated to Naval Medical University, Shanghai, 200003, China.
Xun Lu *Medicinal Chemistry and Bioinformatics Center, Shanghai Jiao Tong University School of Medicine, Shanghai, 200025, China.
Xiaobing LanKey Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan, 750004, China.
Ziqiang ChenDepartment of Orthopedics, Changhai Hospital, Affiliated to Naval Medical University, Shanghai, 200433, China. ziqiang_chensuper81@vip.163.com.
Shaoyong LuKey Laboratory of Protection, Development and Utilization of Medicinal Resources in Liupanshan Area, Ministry of Education, Peptide & Protein Drug Research Center, School of Pharmacy, Ningxia Medical University, Yinchuan, 750004, China. lushaoyong@sjtu.edu.cn.
Shanghai Jiao Tong University · CNNingxia Medical University · CNSecond Military Medical University · CNShanghai Changzheng Hospital · CN

Funding

National Natural Science Foundation of China (National Science Foundation of China) 22077082
6 · The paper itself

Abstract

G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and an important class of drug targets, play a role in maintaining numerous physiological processes. Agonist or antagonist, orthosteric effects or allosteric effects, and biased signaling or balanced signaling, characterize the complexity of GPCR dynamic features. In this study, we first review the structural advancements, activation mechanisms, and functional diversity of GPCRs. We then focus on GPCR drug discovery by revealing the detailed drug-target interactions and the underlying mechanisms of orthosteric drugs approved by the US Food and Drug Administration in the past five years. Particularly, an up-to-date analysis is performed on available GPCR structures complexed with synthetic small-molecule allosteric modulators to elucidate key receptor-ligand interactions and allosteric mechanisms. Finally, we highlight how the widespread GPCR-druggable allosteric sites can guide structure- or mechanism-based drug design and propose prospects of designing bitopic ligands for the future therapeutic potential of targeting this receptor family.

Indexed as

Drug DiscoveryReceptors, G-Protein-CoupledAllosteric SiteDrug DesignHumansLigandsUnited StatesLigandsReceptors, G-Protein-Coupled

Identifiers

PMID38594257
PMCPMC11004190
OpenAlexW4394623467

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.