ArticleAnalytical chemistry2009
Automated cell-based assay for screening of aquaporin inhibitors.
Article in Analytical chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
What it found
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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.
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.
Who cites it
43 citing papers in PubMed, 71 citations in OpenAlex.
- Supramolecular aggregation of aquaporin-4 shapes astrocyte collective migration and mechanics.Scientific reports · 2026Article
- Distinctive roles of aquaporins and novel therapeutic opportunities against cancer.RSC medicinal chemistry · 2025Review
- MOMASTAntioxidants (Basel, Switzerland) · 2024Article
- Update on the intriguing roles of AQP4 expression and redistribution in the progression and treatment of glioma.Annals of medicine · 2024Review
- Toward New AQP4 Inhibitors: ORI-TRN-002.International journal of molecular sciences · 2024Article
- TRPML1-Induced Lysosomal CaInternational journal of molecular sciences · 2023Article
- Methods for studying mammalian aquaporin biology.Biology methods & protocols · 2023Review
- AQP4-independent TRPV4 modulation of plasma membrane water permeability.Frontiers in cellular neuroscience · 2023Article
- Aquaporin Inhibitors.Advances in experimental medicine and biology · 2023Article
- Review
- Transcription factor-based direct conversion of human fibroblasts to functional astrocytes.Stem cell reports · 2022Article
- Aquaglyceroporin Modulators as Emergent Pharmacological Molecules for Human Diseases.Frontiers in molecular biosciences · 2022Review
- dDAVP Downregulates the AQP3-Mediated Glycerol TransportFrontiers in cell and developmental biology · 2022Article
- A Repurposed Drug Screen for Compounds Regulating Aquaporin 5 Stability in Lung Epithelial Cells.Frontiers in pharmacology · 2022Article
- Development of a High-throughput NanoBRET Screening Platform to Identify Modulators of the RAS/RAF Interaction.Molecular cancer therapeutics · 2021Article
- Article
- AQP1 Is Up-Regulated by Hypoxia and Leads to Increased Cell Water Permeability, Motility, and Migration in Neuroblastoma.Frontiers in cell and developmental biology · 2021Article
- Article
- Functionalized Phenylbenzamides Inhibit Aquaporin-4 Reducing Cerebral Edema and Improving Outcome in Two Models of CNS Injury.Neuroscience · 2019Article
- AQP4ex is crucial for the anchoring of AQP4 at the astrocyte end-feet and for neuromyelitis optica antibody binding.Acta neuropathologica communications · 2019Article
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
Abstract
Aquaporins form water channels that play major roles in a variety of physiological processes so that altered expression or function may underlie pathological conditions. In order to identify compounds that modulate aquaporin function, we have implemented a functional assay based on rapid measurement of osmotically induced cell volume changes to screen several libraries of diverse drugs. The time course of fluorescence changes in calcein-loaded cells was analyzed during an osmotic challenge using a 96-multiwell fluorescence plate reader. This system was validated using astrocyte primary cultures and fibroblasts that strongly express endogenous AQP4 and AQP1 proteins, respectively, as well as AQP4-transfected cells. We screened 3575 compounds, including 418 FDA-approved and commercially available drugs, for their effect on AQP-mediated water transport. Primary screening yielded 10 compounds that affected water transport activity in both astrocytes and AQP4-transfected cells and 42 compounds that altered cell volume regulation in astrocytes. Selected drugs were then analyzed on AQP1-expressing erythrocytes and AQP4-expressing membrane vesicles by stopped-flow light scattering. Four molecules of the National Cancer Institute's chemical library (NSC164914, NSC670229, NSC168597, NSC301460) were identified that differentially affected both AQP4 and AQP1 mediated water transport, with EC50 values between 20 and 50 microM. This fluorescence microplate reader-based assay may, thus, provide a platform for high-throughput screening which, when coupled to a secondary evaluation to confirm target specificity, should allow discovery of AQP-specific compounds for novel therapeutic strategies in the treatment of water balance disorders.
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Registered trials
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.