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TRP Channels: Mechanisms, Functions, and Therapeutic Implications
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TRP Channels: Mechanisms, Functions, and Therapeutic Implications

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Biochemistry".

Deadline for manuscript submissions: 20 July 2026 | Viewed by 3417

Special Issue Editor

Dr. Stefan Mergler

E-Mail Website
Guest Editor
Department of Ophthalmology, Charité—Universitätsmedizin Berlin, Corporate Member of Freie Universität Berlin and Humboldt-Universität zu Berlin, 10117 Berlin, Germany
Interests: transient receptor potential (TRP) channels; calcium signaling

Special Issue Information

Dear Colleagues,

Receptor activation induces downstream events that elicit a variety of responses in diverse cell types. Transient changes in intracellular calcium levels serve as second messengers in mediating the receptor control of cellular processes that are essential for maintaining cells’ function and longevity. For cells to maintain tissue homeostasis, they must express membrane-delimited ion permeation pathways, pumps, and exchangers, which, in concert, enable calcium to serve as a second messenger as long as its intracellular levels are maintained within a certain physiological range. Transient receptor potential (TRP) channels are a class of non-selective ion channels that play a critical role, acting as sensors that enable Ca2+ to serve their essential function as a second messenger. These channels are found in numerous tissues and cell types and are phylogenetically very old; they sense temperature, pain, touch, vision, taste, and smell, and also regulate different cell processes. The function of most TRP channels, especially in non-excitable cells, requires further study. For this Special Issue of IJMS, we seek research and review articles that focus on the functional and pathophysiological roles of TRP channels in normal tissues and in tumorous pathophysiological conditions.

Dr. Stefan Mergler
Guest Editor

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Keywords

  • transient receptor potential (TRP) channels
  • calcium signaling
  • ion channels
  • tissue homeostasis
  • receptor activation

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Published Papers (4 papers)

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Research

23 pages, 5627 KB  
Article
TRP-Dependent Calcium Regulation in HCEC-12 Cells: Involvement of Ascorbic Acid and Cannabinoid Receptor Signaling
by Louay Homsi, Anisha Atul Bhamare, Uwe Pleyer and Stefan Mergler
Int. J. Mol. Sci. 2026, 27(9), 3902; https://doi.org/10.3390/ijms27093902 - 28 Apr 2026
Viewed by 148
Abstract
The human corneal endothelium (HCE) is critical for maintaining corneal transparency. Dysfunctions due to cell loss are linked to altered intracellular calcium ([Ca2+]i) homeostasis. Transient receptor potential channels (TRPs) are key regulators of [Ca2+]i, and [...] Read more.
The human corneal endothelium (HCE) is critical for maintaining corneal transparency. Dysfunctions due to cell loss are linked to altered intracellular calcium ([Ca2+]i) homeostasis. Transient receptor potential channels (TRPs) are key regulators of [Ca2+]i, and both L-ascorbic acid (Asc) and cannabinoid receptor (CB) agonists have been implicated in modulating TRP activity. This study investigated the effects of 1 mM Asc and the CB agonist WIN 55,212-2 (WIN) (10 µM) on [Ca2+]i regulation in human corneal endothelial cells (HCECs). HCEC-12 was used as the established HCE cell model. [Ca2+]i dynamics were assessed by fura-2/AM fluorescence imaging, and membrane currents were analyzed using planar patch-clamp recordings. Adding 1 mM Asc increased [Ca2+]i, which was partially suppressed by the TRPV1 blocker AMG-9810 (AMG) (20 µM) and the TRPV4 blocker GSK2193874 (GSK219) (10 µM). Furthermore, 1 mM Asc increased whole-cell currents. WIN also induced [Ca2+]i transients that were partially attenuated by AMG, the TRPM8 blocker AMTB (20 µM), GSK219, and the CB1 inverse agonist AM251 (10 µM). In addition, combined treatment with Asc and WIN enhanced [Ca2+]i elevations compared with either treatment alone. These findings provide the first evidence for a functional interaction between TRP channel activity and CB signaling in HCECs. The inhibitory effect of AM251 suggests a predominant contribution of CB1 receptors. Given the central role of Ca2+ homeostasis in corneal endothelial function and disease, these results may contribute to a better understanding of endothelial pathophysiology and support further investigation of TRPs and cannabinoid signaling as potential targets in corneal disorders. Full article
(This article belongs to the Special Issue TRP Channels: Mechanisms, Functions, and Therapeutic Implications)
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15 pages, 4152 KB  
Article
UVA Light Triggers Activation of TRPV1 and TRPA1 by Staurosporine and Midostaurin
by Sebastian Pantke, Lucas H. K. Weber, Frank G. Echtermeyer, Christine Herzog, Mirjam J. Eberhardt and Andreas Leffler
Int. J. Mol. Sci. 2026, 27(1), 227; https://doi.org/10.3390/ijms27010227 - 25 Dec 2025
Viewed by 572
Abstract
The activation of TRPV1 and TRPA1 by UVA light is a complex process involving channel modulation by reactive oxygen species (ROS). The present study describes staurosporine and midostaurin, two protein kinase inhibitors, as photosensitizers that can modulate the activity of TRPV1 and TRPA1 [...] Read more.
The activation of TRPV1 and TRPA1 by UVA light is a complex process involving channel modulation by reactive oxygen species (ROS). The present study describes staurosporine and midostaurin, two protein kinase inhibitors, as photosensitizers that can modulate the activity of TRPV1 and TRPA1 in a UVA light-dependent manner. Patch-clamp and calcium imaging were used to investigate effects of staurosporine and midostaurin on recombinant human (h) TRPV1 and TRPA1 in HEK 293T cells and on native mouse dorsal root ganglion (DRG) cells. Staurosporine applied alone did not induce channel activation, but co-application with UVA light activated both TRPV1 and TRPA1. Staurosporine with UVA light also potentiated TRPV1-mediated membrane currents induced by heat and protons. Midostaurin induced the UVA light-independent activation and sensitization of TRPV1 and TRPA1, and this effect was strongly potentiated by UVA light. Effects induced by both staurosporine and midostaurin were reversed by the reducing agent dithiothreitol (DTT). Midostaurin induced a calcium influx in TRPA1-expressing DRG neurons. Our results show that staurosporine and midostaurin modulate the activity of TRPV1 and TRPA1 channels in the presence of UVA light. These photosensitizing properties can be relevant when staurosporine is used for in vitro experiments, and they may account for the phototoxic side effects of midostaurin. Full article
(This article belongs to the Special Issue TRP Channels: Mechanisms, Functions, and Therapeutic Implications)
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12 pages, 2183 KB  
Article
Increased Expression of TRPV1 in the Central Nucleus of the Amygdala Is Involved in Orthodontic Pain in Rats
by Rui Wang, Weining Wang, Yuxin Kang, Yuhuan Jiang, Xiaoyu Tang, Yaxing Shu, Jiayi Zhou, Zhiping Hu, Shuang Wang and Hu Qiao
Int. J. Mol. Sci. 2025, 26(23), 11296; https://doi.org/10.3390/ijms262311296 - 22 Nov 2025
Viewed by 714
Abstract
Transient receptor potential vanilloid type 1 (TRPV1) is known to gate nociceptive signals, while the central amygdala (CeA) plays a key role in encoding pain and avoidance behaviors; however, whether TRPV1 within CeA mediate orthodontic tooth-moving pain remains unclear. To investigate this, we [...] Read more.
Transient receptor potential vanilloid type 1 (TRPV1) is known to gate nociceptive signals, while the central amygdala (CeA) plays a key role in encoding pain and avoidance behaviors; however, whether TRPV1 within CeA mediate orthodontic tooth-moving pain remains unclear. To investigate this, we examined the role of TRPV1 in the CeA using a rat model of experimental tooth movement. A total of 118 Sprague-Dawley rats were divided into control, 30 g, 50 g, and 80 g force groups. Micro-CT confirmed successful tooth movement, and the 50 g force was selected as optimal. Pain was assessed by mechanical hypersensitivity using the von Frey test, face-grooming, and the Rat Grimace Scale (RGS). All measures showed maximal changes at day 1 and returned to baseline by day 7. Immunohistochemistry and western blot analysis in the 50 g group revealed upregulation of TRPV1 in the CeA following force application, a trajectory that paralleled the pain behavioral responses. These findings indicate that experimental tooth movement upregulates TRPV1 in the CeA and that this channel contributes to orthodontic pain. Full article
(This article belongs to the Special Issue TRP Channels: Mechanisms, Functions, and Therapeutic Implications)
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14 pages, 1031 KB  
Article
Determinants for Activation of the Ion Channel TRPV3 by Weak Acids
by Daniel Rudolf, Inês C. A. Pombeiro Stein, Toni Sturhahn, Julian Wunder, Axel Hage and Andreas Leffler
Int. J. Mol. Sci. 2025, 26(17), 8275; https://doi.org/10.3390/ijms26178275 - 26 Aug 2025
Viewed by 1344
Abstract
Several transient receptor potential vanilloid (TRPV) ion channels are proton-sensitive, and recent structural studies have identified poorly conserved mechanisms for the proton sensitivity of TRPV1, TRPV2 and TRPV5. While such detailed studies are lacking for TRPV3, three distinct intracellular motifs were suggested to [...] Read more.
Several transient receptor potential vanilloid (TRPV) ion channels are proton-sensitive, and recent structural studies have identified poorly conserved mechanisms for the proton sensitivity of TRPV1, TRPV2 and TRPV5. While such detailed studies are lacking for TRPV3, three distinct intracellular motifs were suggested to be required for a direct channel activation by cytosolic acidification. In this study, we investigated if these mechanisms are also relevant for the activation of TRPV3 by weak acids. Wildtype (WT) and several mutants of human TRPV3 transiently expressed in HEK 293T cells were investigated by whole-cell patch clamp electrophysiology. Cells expressing TRPV3-WT generated membrane currents induced by acetic acid (HOAc), formic acid and carbonic acid at pH 5.0. Activation induced by HOAc was concentration-dependent and increased with decreasing pH values. HOAc also strongly potentiated TRPV3-mediated responses to carvacrol and heat. Among the three suggested motifs for the binding of intracellular protons, only the mutant TRPV3-Asp512Ala exhibited an almost complete loss of HOAc sensitivity. The mutation of two C-terminal charged residues (Gln689/Asp727) even resulted in a clear gain of function for both HOAc and heat, and the mutation of the 2-APB-binding site His426 did not significantly abrogate HOAc sensitivity. Finally, insertion of the recently identified binding site in TRPV2 for the weak acid probenecid into TRPV3 (Glu216His) resulted in an increased HOAc sensitivity. To conclude, our data confirm that TRPV3 is sensitized and activated by several weak acids. While Asp512 appears to be a critical intracellular proton-modulating site, a more profound understanding of the mechanisms dictating the proton sensitivity of TRPV3 may require structural studies. Full article
(This article belongs to the Special Issue TRP Channels: Mechanisms, Functions, and Therapeutic Implications)
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