Evidence map›Paper›PMID 26993802›Full record

ArticleMolecular pharmacology2016

Experimental Evaluation of Proposed Small-Molecule Inhibitors of Water Channel Aquaporin-1.

Cristina Esteva-Font, Byung-Ju Jin, Sujin Lee, Puay-Wah Phuan, Marc O Anderson, A S Verkman

Open access · bronzeAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Molecular pharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
2.4field-weighted citation impact, top 11% 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

15 citing papers in PubMed, 33 citations in OpenAlex.

  1. Review
  2. Review
  3. Review
  4. Aquaporin-mediated dysregulation of cell migration in disease states.Cellular and molecular life sciences : CMLS · 2023
    Review
  5. Article
  6. Review
  7. COJournal of enzyme inhibition and medicinal chemistry · 2021
    Article
  8. Review
  9. HAuClFrontiers in physiology · 2020
    Article
  10. Article
  11. Article
  12. Review
  13. Aquaporin-Targeted Therapeutics: State-of-the-Field.Advances in experimental medicine and biology · 2017
    Review
  14. Aquaporin Water Channels and Hydrocephalus.Pediatric neurosurgery · 2017
    Review
  15. 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

6 authors at 2 institutions in 1 country.

Cristina Esteva-FontDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.).
Byung-Ju JinDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.).
Sujin LeeDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.).
Puay-Wah PhuanDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.).
Marc O AndersonDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.).
A S VerkmanDepartments of Medicine and Physiology, University of California, San Francisco, California (C.E.-F., B.-J.J., S.L., P.-W.P., A.S.V.); Department of Chemistry and Biochemistry, San Francisco State University, San Francisco, California (M.O.A.) Alan.Verkman@ucsf.edu.
University of California, San Francisco · USSan Francisco State University · US

Funding

SynthesisP30DK072517 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2005 to 2022
$18.1M
Translational Approaches to Develop Drug Therapy for DiarrheaR24DK099803 · NIDDK · JOHNS HOPKINS UNIVERSITY · PI DONOWITZ, MARK · 2014 to 2019
$8.9M
Functional Role of Aquaporins in Eye PhysiologyR01EY013574 · NEI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2002 to 2022
$7.6M
MECHANISMS OF WATER TRANSPORT IN RENAL EPITHELIAR37DK035124 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 1999 to 2008
$4.2M
Application of Novel Optical Methods to Cell DynamicsR37EB000415 · NIBIB · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2007 to 2016
$4.1M
Urea transport inhibitors as a new class of diureticsR01DK101373 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2014 to 2018
$1.7M
Application of Novel Optical Methods to Cell DynamicsR01EB000415 · NIBIB · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 2002 to 2006
$1.7M
WATER AND NON-ELECTROLYTE TRANSPORT IN RENAL VESICLESR01DK035124 · NIDDK · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI VERKMAN, ALAN S · 1986 to 2014
$1.4M
NEI NIH HHS R01 EY013574NIBIB NIH HHS R01 EB000415NIBIB NIH HHS R37 EB000415NIDDK NIH HHS P30 DK072517NIDDK NIH HHS R01 DK035124NIDDK NIH HHS R01 DK101373NIDDK NIH HHS R24 DK099803NIDDK NIH HHS R37 DK035124
6 · The paper itself

Abstract

The aquaporin-1 (AQP1) water channel is a potentially important drug target, as AQP1 inhibition is predicted to have therapeutic action in edema, tumor growth, glaucoma, and other conditions. Here, we measured the AQP1 inhibition efficacy of 12 putative small-molecule AQP1 inhibitors reported in six recent studies, and one AQP1 activator. Osmotic water permeability was measured by stopped-flow light scattering in human and rat erythrocytes that natively express AQP1, in hemoglobin-free membrane vesicles from rat and human erythrocytes, and in plasma membrane vesicles isolated from AQP1-transfected Chinese hamster ovary cell cultures. As a positive control, 0.3 mM HgCl2 inhibited AQP1 water permeability by >95%. We found that none of the tested compounds at 50 µM significantly inhibited or increased AQP1 water permeability in these assays. Identification of AQP1 inhibitors remains an important priority.

Indexed as

AnimalsAquaporin 1Cell MembraneCell Membrane PermeabilityCell ShapeCHO CellsCricetinaeCricetulusErythrocytesFluoresceinsHemoglobinsHumansOsmosisRats, WistarSmall Molecule LibrariesWaterAquaporin 1FluoresceinsfluorexonHemoglobinsSmall Molecule LibrariesWater

Identifiers

PMID26993802
PMCPMC4885500
OpenAlexW2300481076

What OpenQuestion holds

Textmetadata
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.