ArticleMolecular pharmacology2012
Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells.
Article in Molecular pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 46 papers.
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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.
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Who cites it
46 citing papers in PubMed.
- Article
- TRP (transient receptor potential) ion channel family: structures, biological functions and therapeutic interventions for diseases.Signal transduction and targeted therapy · 2023Review
- Review
- Vascular mechanotransduction.Physiological reviews · 2023Review
- Article
- Mechanisms and physiological implications of cooperative gating of clustered ion channels.Physiological reviews · 2022Review
- Restricted Intimal CaFrontiers in physiology · 2022Article
- Regulation of the Membrane Trafficking of the Mechanosensitive Ion Channels TRPV1 and TRPV4 by Zonular Tension, Osmotic Stress and Activators in the Mouse Lens.International journal of molecular sciences · 2021Article
- Role of TRP ion channels in cerebral circulation and neurovascular communication.Neuroscience letters · 2021Review
- The Calcium Signaling Mechanisms in Arterial Smooth Muscle and Endothelial Cells.Comprehensive Physiology · 2021Article
- Transient Receptor Potential Vanilloid in the Brain Gliovascular Unit: Prospective Targets in Therapy.Pharmaceutics · 2021Review
- The role of TRPV4 channels in ocular function and pathologies.Experimental eye research · 2020Review
- Endothelial CaThe Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology · 2020Review
- TRPV4: A Physio and Pathophysiologically Significant Ion Channel.International journal of molecular sciences · 2020Review
- Polymodal Sensory Transduction in Mouse Corneal Epithelial Cells.Investigative ophthalmology & visual science · 2020Article
- Ablation of Endothelial TRPV4 Channels Alters the Dynamic CaInternational journal of molecular sciences · 2020Article
- Elevated TRPV4 Levels Contribute to Endothelial Damage and Scarring in Experimental Spinal Cord Injury.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2020Article
- Endothelial TRPV4 channels and vasodilator reactivity.Current topics in membranes · 2020Review
- Regulation of vascular tone by transient receptor potential ankyrin 1 channels.Current topics in membranes · 2020Review
- Molecular and Functional Study of Transient Receptor Potential Vanilloid 1-4 at the Rat and Human Blood-Brain Barrier Reveals Interspecies Differences.Frontiers in cell and developmental biology · 2020Article
Corrections and comments
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Authors and funding
5 authors.
Funding
Abstract
Critical functions of the vascular endothelium are regulated by changes in intracellular [Ca(2+)]. Endothelial dysfunction is tightly associated with cardiovascular disease, and improved understanding of Ca(2+) entry pathways in these cells will have a significant impact on human health. However, much about Ca(2+) influx channels in endothelial cells remains unknown because they are difficult to study using conventional patch-clamp electrophysiology. Here we describe a novel, highly efficient method for recording and analyzing Ca(2+)-permeable channel activity in primary human endothelial cells using a unique combination of total internal reflection fluorescence microscopy (TIRFM), custom software-based detection, and selective pharmacology. Our findings indicate that activity of the vanilloid (V) transient receptor potential (TRP) channel TRPV4 can be rapidly recorded and characterized at the single-channel level using this method, providing novel insight into channel function. Using this method, we show that although TRPV4 protein is evenly distributed throughout the plasma membrane, most channels are silent even during maximal stimulation with the potent TRPV4 agonist N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A). Furthermore, our findings indicate that GSK1016790A acts by recruiting previously inactive channels, rather than through increasing elevation of basal activity.
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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.