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Biophys Chem ; 254: 106246, 2019 11.
Article in English | MEDLINE | ID: mdl-31426023

ABSTRACT

The inhibitory effect of the flavonoid naringenin on plant and human Two-Pore Channels (TPCs) was assessed by means of electrophysiological measurements. By acting on human TPC2, naringenin, was able to dampen intracellular calcium responses to VEGF in cultured human endothelial cells and to impair angiogenic activity in VEGF-containing matrigel plugs implanted in mice. Molecular docking predicts selective binding sites for naringenin in the TPC structure, thus suggesting a specific interaction between the flavonoid and the channel.


Subject(s)
Calcium Channels/chemistry , Flavanones/chemistry , Plants/metabolism , Animals , Binding Sites , Calcium/chemistry , Calcium/metabolism , Calcium Channels/metabolism , Collagen/chemistry , Drug Combinations , Endothelial Cells/cytology , Endothelial Cells/metabolism , Flavanones/metabolism , Humans , Laminin/chemistry , Mice , Molecular Docking Simulation , Patch-Clamp Techniques , Plant Proteins/antagonists & inhibitors , Plant Proteins/metabolism , Proteoglycans/chemistry
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