Evidence map›Paper›PMID 30202096›Full record

ArticleScientific reports2018

Urate transporter inhibitor lesinurad is a selective peroxisome proliferator-activated receptor gamma modulator (sPPARγM) in vitro.

Pascal Heitel, Leonie Gellrich, Jan Heering, Tamara Goebel, Astrid Kahnt, Ewgenij Proschak, Manfred Schubert-Zsilavecz, Daniel Merk

Open access · goldAbstract read
In one paragraph

Article in Scientific reports, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.9field-weighted citation impact, top 15% 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

11 citing papers in PubMed, 20 citations in OpenAlex.

  1. Article
  2. Review
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  9. Study on the Multitarget Mechanism of Sanmiao Pill on Gouty Arthritis Based on Network Pharmacology.Evidence-based complementary and alternative medicine : eCAM · 2020
    Article
  10. Article
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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.

Pascal HeitelGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Leonie GellrichGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Jan HeeringProject Group Translational Medicine and Pharmacology TMP, Fraunhofer Institute for Molecular Biology and Applied Ecology IME, Theodor-Stern-Kai 7, D-60596, Frankfurt, Germany.
Tamara GoebelGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Astrid KahntGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Ewgenij ProschakGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Manfred Schubert-ZsilaveczGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany.
Daniel MerkGoethe University Frankfurt, Institute of Pharmaceutical Chemistry, Max-von-Laue-Str. 9, D-60438, Frankfurt, Germany. merk@pharmchem.uni-frankfurt.de.ORCID 0000-0002-5359-8128
Goethe University Frankfurt · DEFraunhofer Institute for Molecular Biology and Applied Ecology · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Gout is the most common arthritic disease in human but was long neglected and therapeutic options are not satisfying. However, with the recent approval of the urate transporter inhibitor lesinurad, gout treatment has experienced a major innovation. Here we show that lesinurad possesses considerable modulatory potency on peroxisome proliferator-activated receptor γ (PPARγ). Since gout has a strong association with metabolic diseases such as type 2 diabetes, this side-activity appears as very valuable contributing factor to the clinical efficacy profile of lesinurad. Importantly, despite robustly activating PPARγ in vitro, lesinurad lacked adipogenic activity, which seems due to differential coactivator recruitment and is characterized as selective PPARγ modulator (sPPARγM).

Indexed as

3T3 CellsAdipocytesAdipogenesisAnimalsCell DifferentiationGoutHEK293 CellsHep G2 CellsHumansMiceMolecular Docking SimulationPPAR gammaRecombinant ProteinsThioglycolatesTransfectionTriazoleslesinuradPPAR gammaPPARG protein, humanRecombinant ProteinsThioglycolatesTriazolesUricosuric Agents

Identifiers

PMID30202096
PMCPMC6131501
OpenAlexW2890378923

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.