Canonical transient receptor potential 4(TRPC4) forms non-selective cation channels that contribute to phospholipase C-dependent Ca2+ entry into cells following stimulation of G protein coupled receptors and receptor ...Canonical transient receptor potential 4(TRPC4) forms non-selective cation channels that contribute to phospholipase C-dependent Ca2+ entry into cells following stimulation of G protein coupled receptors and receptor tyrosine kinases.Moreover,the channels are regulated by pertussis toxin-sensitive Gi/o proteins,lipids,and various other signaling mechanisms.TRPC4-containing channels participate in the regulation of a variety of physiological functions,including excitability of both gastrointestinal smooth muscles and brain neurons.This review is to present recent advances in the understanding of physiology and development of small molecular modulators of TRPC4 channels.展开更多
Intracellular Ca2+homeostasis is essential for vascular function and blood pressure regulation.Because of their unique roles in regulating intracellular Ca2+concentration and vascular function,a novel class of non-sel...Intracellular Ca2+homeostasis is essential for vascular function and blood pressure regulation.Because of their unique roles in regulating intracellular Ca2+concentration and vascular function,a novel class of non-selective cation channels,called transient receptor potential(TRP)channels,have emerged at the frontier of hypertension research.Based on their role in vasculature function regulation,TRP channels can be divided into two functional subtypes:one that participates in vasoconstriction and one that participates in vasodilatation.A functional imbalance of these two subtypes of TRP channels may disturb intracellular calcium([Ca2+]i)homeostasis,and the consequent vascular dysfunction may contribute to the development of hypertension.The potential of these TRP channels as novel pharmacological targets for the treatment of human hypertension is of great interest.展开更多
基金supported in part by the National Natural Science Foundation of China(81228021)US National Institutes of Health(DK081654)
文摘Canonical transient receptor potential 4(TRPC4) forms non-selective cation channels that contribute to phospholipase C-dependent Ca2+ entry into cells following stimulation of G protein coupled receptors and receptor tyrosine kinases.Moreover,the channels are regulated by pertussis toxin-sensitive Gi/o proteins,lipids,and various other signaling mechanisms.TRPC4-containing channels participate in the regulation of a variety of physiological functions,including excitability of both gastrointestinal smooth muscles and brain neurons.This review is to present recent advances in the understanding of physiology and development of small molecular modulators of TRPC4 channels.
文摘Intracellular Ca2+homeostasis is essential for vascular function and blood pressure regulation.Because of their unique roles in regulating intracellular Ca2+concentration and vascular function,a novel class of non-selective cation channels,called transient receptor potential(TRP)channels,have emerged at the frontier of hypertension research.Based on their role in vasculature function regulation,TRP channels can be divided into two functional subtypes:one that participates in vasoconstriction and one that participates in vasodilatation.A functional imbalance of these two subtypes of TRP channels may disturb intracellular calcium([Ca2+]i)homeostasis,and the consequent vascular dysfunction may contribute to the development of hypertension.The potential of these TRP channels as novel pharmacological targets for the treatment of human hypertension is of great interest.
