Regulation of TRPV1 Ion Channel by Phosphoinositide (4,5)-Bisphosphate

Senning, Eric N.; Collins, Marcus D.; Stratiievska, Anastasiia; Ufret-Vincenty, Carmen A.; Gordon, Sharona E.

doi:10.1074/jbc.m114.553180

Cited by 50 publications

(54 citation statements)

References 35 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…They also conclude that doseresponse curves for activation of TRPV1 have underestimated the selectivity of PIP 2 for this channel 15 and that PIP 2 incorporation to the intracellular plasma membrane leaflet leads to potentiation of capsaicin-activated currents. 16 Moreover, in another study by the Gordon group, it was shown that the TRPV1 channel displays specificity for regulation of capsaicin activation by PIP 2 since phosphatidylinositol 4-phosphate (PI(4)P) does not support activation of the channel by this vanilloid compound. 17 With respect to the molecular interactions of PIP 2 with TRPV1, it has been proposed that this molecule binds to the C-terminus of the channel.…”

Section: Trpv Subfamilymentioning

confidence: 99%

Regulation of thermoTRPs by lipids

2016

View full text Add to dashboard Cite

The family of Transient Receptor Potential (TRP) ion channels is constituted by 7 subfamilies among which are those that respond to temperature, the thermoTRPs. These channels are versatile molecules of a polymodal nature that have been shown to be modulated in various fashions by molecules of a lipidic nature. Some of these molecules interact directly with the channels on specific regions of their structures and some of these promote changes in membrane fluidity or modify their gating properties in response to their agonists. Here, we have discussed how some of these lipids regulate the activity of thermoTRPs and included some of the available evidence for the molecular mechanisms underlying their effects on these channels.

show abstract

Section: Trpv Subfamilymentioning

confidence: 99%

Regulation of thermoTRPs by lipids

2016

View full text Add to dashboard Cite

show abstract

“…PI(4,5)P 2 also directly modulates the function of several ion channels and transporters (Suh and Hille, 2005;Robertson, 2007), including members of the TRP channel family (Qin, 2007;Rohacs, 2014). The mode of action of PI(4,5) P 2 in TRPV1 channels has been the subject of debate (cf., Cao et al, 2013a;Senning et al, 2014); however, there is apparent consensus that PI(4,5)P 2 behaves as a TRPV1 channel agonist Lukacs et al, 2007;Ufret-Vincenty et al, 2011Senning et al, 2014;Poblete et al, 2015). Brauchi et al (2007) showed that alanine replacement of two positively charged residues (R701 and K710) located at the C-terminal region of the TRPV1 channel shifted the dose-response curve of PI(4,5)P 2 to the right.…”

Section: Modulation Of Trpv1 Channel Gating By Lipidsmentioning

confidence: 99%

Structure-Driven Pharmacology of Transient Receptor Potential Channel Vanilloid 1

et al. 2016

View full text Add to dashboard Cite

The transient receptor potential vanilloid 1 (TRPV1) ion channel is a polymodal receptor that mediates the flux of cations across the membrane in response to several stimuli, including heat, voltage, and ligands. The best known agonist of TRPV1 channels is capsaicin, the pungent component of "hot" chili peppers. In addition, peptides found in the venom of poisonous animals, along with the lipids phosphatidylinositol 4,5-biphosphate, lysophosphatidic acid, and cholesterol, bind to TRPV1 with high affinity to modulate channel gating. Here, we discuss the functional evidence regarding ligand-dependent activation of TRPV1 channels in light of structural data recently obtained by cryoelectron microscopy. This review focuses on the mechanistic insights into ligand binding and allosteric gating of TRPV1 channels and the relevance of accurate polymodal receptor biophysical characterization for drug design in novel pain therapies.

show abstract

“…Electrophysiological and genetic studies demonstrated that TRPV1 is activated by heat (more than 42°C), acid pH, specific ligands (i.e. : Capsaicin) and by a number of chemical factors produced during inflammation (i.e., Diacyl-glycerol-DAG-, phosphatidylinositol 4,5-biphosphate-PIP2-, anandamide and other negatively charged lipids) that can directly potentiate the effects of capsaicin or heat (Tominaga et al, 1998;Jordt et al, 2000;Sprague et al, 2001;Lukacs et al, 2013;Senning et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

Transient Receptor Potential Vanilloid 1 Involvement in Animal Pain Perception

Vercelli¹,

Barbero²

2015

American Journal of Animal and Veterinary Sciences

View full text Add to dashboard Cite

In last decades, Transient Receptor Potential Vanilloid 1 (TRPV1) has been the target of a large number of scientific investigations. It has been identified as a polymodal transducer molecule on a sub-set of primary sensory neurons which responds to various endogenous and exogenous stimuli including noxious heat (more than 42°C), protons and vanilloids such as capsaicin, the hot ingredient of chilli peppers. In mammals, TRPV1 displays a wide tissue and cellular expression including both the peripheral and central nervous system, with broad distribution and functions, in physiological and pathological conditions. Its primary localisation in sensory neurons reveals its key nodal point in pain transmission pathways. Nowadays, it is clear that TRPV1 is involved in inflammation, pain perception and thermoregulation in the majority of animals, including humans. Recently, a lot of studies tried to investigate some analgesic treatments applied on TRPV1. The aim of this review is to give to the readers a short overview of the TRPV1 involvement in pain perception and possible therapeutic applications, highlighting this topic in species of interest in veterinary medicine.

show abstract

Regulation of TRPV1 Ion Channel by Phosphoinositide (4,5)-Bisphosphate

Cited by 50 publications

References 35 publications

Regulation of thermoTRPs by lipids

Regulation of thermoTRPs by lipids

Structure-Driven Pharmacology of Transient Receptor Potential Channel Vanilloid 1

Transient Receptor Potential Vanilloid 1 Involvement in Animal Pain Perception

Contact Info

Product

Resources

About