Evidence map›Paper›PMID 26720709›Full record

ArticlePloS one2015

Novel Zn2+ Modulated GPR39 Receptor Agonists Do Not Drive Acute Insulin Secretion in Rodents.

Ola Fjellström, Niklas Larsson, Shin-Ichiro Yasuda, Takuma Tsuchida, Takahiro Oguma, Anna Marley, Charlotte Wennberg-Huldt, Daniel Hovdal, Hajime Fukuda, Yukimi Yoneyama and 10 more

Abstract read
In one paragraph

Article in PloS one, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed, 1 pooled it
–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

12 citing papers in PubMed, 1 synthesis or guideline pooled it.

  1. Guideline
  2. GPR39 activation inhibits AQP2 trafficking and alters cytoskeletal organization.American journal of physiology. Cell physiology · 2026
    Article
  3. Review
  4. Article
  5. Article
  6. Control of coronary vascular resistance by eicosanoids via a novel GPCR.American journal of physiology. Cell physiology · 2022
    Article
  7. Article
  8. Article
  9. Review
  10. Article
  11. Review
  12. 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

20 authors.

Ola FjellströmMedicinal Chemistry CVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Niklas LarssonDiscovery Sciences, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Shin-Ichiro YasudaPharmacology Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Takuma TsuchidaPharmacology Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Takahiro OgumaPharmacology Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Anna MarleyDiscovery Sciences, AstraZeneca R&D, Mereside, United Kingdom.
Charlotte Wennberg-HuldtBioscience CVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Daniel HovdalDMPK CVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Hajime FukudaDMPK Research Laboratories, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Yukimi YoneyamaDMPK Research Laboratories, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Kazuyo SasakiPharmacology Research Laboratories II, Mitsubishi Tanabe Pharma Corporation, Kawagishi, Toda-shi, Saitama, Japan.
Anders JohanssonMedicinal Chemistry CVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Sara LundqvistDiscovery Sciences, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Johan BrengdahlDiscovery Sciences, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Richard J IsaacsMolecular Sensing, Inc., Nashville, Tennessee, United States of America.
Daniel BrownMolecular Sensing, Inc., Nashville, Tennessee, United States of America.
Stefan GeschwindnerDiscovery Sciences, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Lambertus BenthemBioscience CVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.
Claire PriestDiscovery Sciences, AstraZeneca R&D, Mereside, United Kingdom.
Andrew TurnbullCVMD iMed, AstraZeneca R&D Gothenburg, Mölndal, Sweden.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Type 2 diabetes (T2D) occurs when there is insufficient insulin release to control blood glucose, due to insulin resistance and impaired β-cell function. The GPR39 receptor is expressed in metabolic tissues including pancreatic β-cells and has been proposed as a T2D target. Specifically, GPR39 agonists might improve β-cell function leading to more adequate and sustained insulin release and glucose control. The present study aimed to test the hypothesis that GPR39 agonism would improve glucose stimulated insulin secretion in vivo. A high throughput screen, followed by a medicinal chemistry program, identified three novel potent Zn2+ modulated GPR39 agonists. These agonists were evaluated in acute rodent glucose tolerance tests. The results showed a lack of glucose lowering and insulinotropic effects not only in lean mice, but also in diet-induced obese (DIO) mice and Zucker fatty rats. It is concluded that Zn2+ modulated GPR39 agonists do not acutely stimulate insulin release in rodents.

Indexed as

Drug DiscoveryAnimalsBlood GlucoseDose-Response Relationship, DrugGlucose Tolerance TestHigh-Throughput Screening AssaysHumansInsulinInsulin SecretionIslets of LangerhansMaleMiceRatsRats, ZuckerReceptors, G-Protein-CoupledSmall Molecule LibrariesBlood GlucoseGPR39 protein, humanGPR39 protein, mouseGPR39 protein, ratInsulinReceptors, G-Protein-CoupledSmall Molecule LibrariesZinc

Identifiers

PMID26720709
PMCPMC4697807

What OpenQuestion holds

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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.