Evidence map›Paper›PMID 36231080›Full record

ArticleCells2022

Characterization of the Aquaporin-9 Inhibitor RG100204 In Vitro and in

Marilina Florio, Angelica Engfors, Patrizia Gena, Jessica Larsson, Alessandro Massaro, Stella Timpka, Martina Kvist Reimer, Per Kjellbom, Eric Beitz, Urban Johanson and 2 more

Open access · goldAbstract read
In one paragraph

Article in Cells, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
0.9field-weighted citation impact, top 28% 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

9 citing papers in PubMed, 11 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Article
  5. Review
  6. Review
  7. Article
  8. Aquaporins in Glandular Secretion.Advances in experimental medicine and biology · 2023
    Article
  9. Methods for studying mammalian aquaporin biology.Biology methods & protocols · 2023
    Review
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

12 authors at 5 institutions in 3 countries.

Marilina FlorioDepartment of Biosciences, Biotechnologies and Environment, University of Bari Aldo Moro, 70125 Bari, Italy.
Angelica EngforsDivision of Biochemistry and Structural Biology, Department of Chemistry, Lund University, 22100 Lund, Sweden.
Patrizia GenaDepartment of Biosciences, Biotechnologies and Environment, University of Bari Aldo Moro, 70125 Bari, Italy.
Jessica LarssonRed Glead Discovery AB, Medicon Village, 22381 Lund, Sweden.
Alessandro MassaroDepartment of Management, Finance and Technology, Libera Università Mediterranea (LUM) "Giuseppe Degennaro" LUM University, 70010 Casamassima, Italy.ORCID 0000-0003-1744-783X
Stella TimpkaRed Glead Discovery AB, Medicon Village, 22381 Lund, Sweden.
Martina Kvist ReimerRed Glead Discovery AB, Medicon Village, 22381 Lund, Sweden.
Per KjellbomDivision of Biochemistry and Structural Biology, Department of Chemistry, Lund University, 22100 Lund, Sweden.
Eric BeitzDepartment of Pharmaceutical and Medicinal Chemistry, Pharmaceutical Institute, Christian-Albrechts-University of Kiel, Gutenbergstr. 76, 24118 Kiel, Germany.ORCID 0000-0001-5912-6626
Urban JohansonDivision of Biochemistry and Structural Biology, Department of Chemistry, Lund University, 22100 Lund, Sweden.ORCID 0000-0001-8862-128X
Michael RützlerDivision of Biochemistry and Structural Biology, Department of Chemistry, Lund University, 22100 Lund, Sweden.ORCID 0000-0001-5597-8880
Giuseppe CalamitaDepartment of Biosciences, Biotechnologies and Environment, University of Bari Aldo Moro, 70125 Bari, Italy.ORCID 0000-0003-4666-9546
Lund University · SEMedicon Village · SEUniversity of Bari Aldo Moro · ITChristian-Albrechts-Universität zu Kiel · DELUM Jean Monnet University · IT

Funding

Italian government FISR2020IP_04051
6 · The paper itself

Abstract

Aquaporin-9 (AQP9) is a facilitator of glycerol and other small neutral solute transmembrane diffusion. Identification of specific inhibitors for aquaporin family proteins has been difficult, due to high sequence similarity between the 13 human isoforms, and due to the limited channel surface areas that permit inhibitor binding. The few AQP9 inhibitor molecules described to date were not suitable for in vivo experiments. We now describe the characterization of a new small molecule AQP9 inhibitor, RG100204 in cell-based calcein-quenching assays, and by stopped-flow light-scattering recordings of AQP9 permeability in proteoliposomes. Moreover, we investigated the effects of RG100204 on glycerol metabolism in mice. In cell-based assays, RG100204 blocked AQP9 water permeability and glycerol permeability with similar, high potency (~5 × 10

Indexed as

AquaporinsGlycerolAnimalsBlood GlucoseHumansLiverMiceMice, Inbred StrainsThiadiazolesWaterAquaporinsBlood GlucoseGlycerolRG100204ThiadiazolesWateraquaglyceroporinscalcein quenchingenergy balancegluconeogenesisglycerol metabolismmembrane transportmetabolic homeostasisPichia pastorisproteoliposomesstopped-flow light scattering

Identifiers

PMID36231080
PMCPMC9562188
OpenAlexW4303628908

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.