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903 Results Found

  • Article
  • Open Access
3 Citations
1,818 Views
18 Pages

Tranilast Does Not Inhibit TRPV2

  • Tabea C. Fricke,
  • Nele Stein,
  • Christine Herzog,
  • Frank G. Echtermeyer and
  • Andreas Leffler

21 December 2025

Transient receptor potential vanilloid 2 (TRPV2) is a non-selective cation channel involved in diverse physiological and pathological processes. Tranilast has frequently been described and used as a rather specific inhibitor of TRPV2. However, the mo...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels and Health and Disease)
  • Review
  • Open Access
15 Citations
6,352 Views
13 Pages

Trafficking of Stretch-Regulated TRPV2 and TRPV4 Channels Inferred Through Interactomics

  • Pau Doñate-Macián,
  • Jennifer Enrich-Bengoa,
  • Irene R. Dégano,
  • David G. Quintana and
  • Alex Perálvarez-Marín

27 November 2019

Transient receptor potential cation channels are emerging as important physiological and therapeutic targets. Within the vanilloid subfamily, transient receptor potential vanilloid 2 (TRPV2) and 4 (TRPV4) are osmo- and mechanosensors becoming critica...

(This article belongs to the Special Issue Trafficking of Cardiac Ion Channels – Mechanisms and Alterations Leading to Disease)
  • Communication
  • Open Access
34 Citations
6,169 Views
10 Pages

Marine Cyclic Guanidine Alkaloids Monanchomycalin B and Urupocidin A Act as Inhibitors of TRPV1, TRPV2 and TRPV3, but not TRPA1 Receptors

  • Yuliya Korolkova,
  • Tatyana Makarieva,
  • Kseniya Tabakmakher,
  • Larisa Shubina and ,
  • Ekaterina Kudryashova,
  • Yaroslav Andreev,
  • Irina Mosharova,
  • Hyi-Seung Lee,
  • Yeon-Ju Lee and
  • Sergey Kozlov
  • + 5 authors+ 0 author

23 March 2017

Marine sponges contain a variety of low-molecular-weight compounds including guanidine alkaloids possessing different biological activities. Monanchomycalin B and urupocidin A were isolated from the marine sponge Monanchora pulchra. We found that the...

(This article belongs to the Collection Bioactive Compounds from Marine Invertebrates)
  • Review
  • Open Access
25 Citations
6,336 Views
13 Pages

Muscular dystrophy and dilated cardiomyopathy are intractable diseases and their treatment options are very limited. Transient receptor potential cation channel subfamily V, member 2 (TRPV2), is a stretch-sensitive Ca2+-permeable channel that causes...

(This article belongs to the Special Issue Muscular Dystrophy: From Molecular Basis to Therapies)
  • Article
  • Open Access
8 Citations
4,784 Views
19 Pages

Exploring the Ion Channel TRPV2 and Testicular Macrophages in Mouse Testis

  • Katja Eubler,
  • Pia Rantakari,
  • Heidi Gerke,
  • Carola Herrmann and ,
  • Annika Missel,
  • Nina Schmid,
  • Lena Walenta,
  • Shibojyoti Lahiri,
  • Axel Imhof and
  • Artur Mayerhofer
  • + 7 authors+ 2 authors

The cation channel TRPV2 is known to be expressed by murine macrophages and is crucially involved in their functionality. Macrophages are frequent cells of the mouse testis, an immune-privileged and steroid-producing organ. TRPV2 expression by testic...

(This article belongs to the Special Issue TRP Channels)
  • Article
  • Open Access
53 Citations
7,880 Views
23 Pages

The Effects of Cannabidiol and Prognostic Role of TRPV2 in Human Endometrial Cancer

  • Oliviero Marinelli,
  • Maria Beatrice Morelli,
  • Daniela Annibali,
  • Cristina Aguzzi and ,
  • Laura Zeppa,
  • Sandra Tuyaerts,
  • Consuelo Amantini,
  • Frédéric Amant,
  • Benedetta Ferretti and
  • Massimo Nabissi
  • + 7 authors+ 2 authors

Several studies support, both in vitro and in vivo, the anti-cancer effects of cannabidiol (CBD), a transient receptor potential vanilloid 2 (TRPV2) ligand. TRPV2, often dysregulated in tumors, is associated with altered cell proliferation and aggres...

(This article belongs to the Special Issue Endometrial Cancer Overview: Molecular Biology and Its Potential Clinical Application)
  • Article
  • Open Access
54 Citations
6,443 Views
15 Pages

Cannabidiol Inhibits Tumorigenesis in Cisplatin-Resistant Non-Small Cell Lung Cancer via TRPV2

  • Swati Misri,
  • Kirti Kaul,
  • Sanjay Mishra,
  • Manish Charan and ,
  • Ajeet Kumar Verma,
  • Martin P. Barr,
  • Dinesh K. Ahirwar and
  • Ramesh K. Ganju
  • + 3 authors+ 0 author

24 February 2022

Chemotherapy forms the backbone of current treatments for many patients with advanced non-small-cell lung cancer (NSCLC). However, the survival rate is low in these patients due to the development of drug resistance, including cisplatin resistance. I...

(This article belongs to the Special Issue Advances in Lung Cancer Therapy)
  • Article
  • Open Access
21 Citations
5,294 Views
13 Pages

Ca2+ Signaling and IL-8 Secretion in Human Testicular Peritubular Cells Involve the Cation Channel TRPV2

  • Katja Eubler,
  • Carola Herrmann,
  • Astrid Tiefenbacher,
  • Frank-Michael Köhn and ,
  • J. Ullrich Schwarzer,
  • Lars Kunz and
  • Artur Mayerhofer
  • + 2 authors+ 0 author

19 September 2018

Peritubular cells are part of the wall of seminiferous tubules in the human testis and their contractile abilities are important for sperm transport. In addition, they have immunological roles. A proteomic analysis of isolated human testicular peritu...

(This article belongs to the Special Issue Ion Channel and Ion-Related Signaling)
  • Article
  • Open Access
25 Citations
3,421 Views
20 Pages

The Protective Effect of CBD in a Model of In Vitro Ischemia May Be Mediated by Agonism on TRPV2 Channel and Microglia Activation

  • Daniele Lana,
  • Elisa Landucci,
  • Costanza Mazzantini,
  • Giada Magni and ,
  • Domenico Edoardo Pellegrini-Giampietro and
  • Maria Grazia Giovannini
  • + 1 author+ 0 author

12 October 2022

Cannabinoids, used for centuries for recreational and medical purposes, have potential therapeutic value in stroke treatment. Cannabidiol (CBD), a non-psychoactive compound and partial agonist of TRPV2 channels, is efficacious in many neurological di...

(This article belongs to the Section Molecular Neurobiology)
  • Review
  • Open Access
26 Citations
5,959 Views
14 Pages

6 March 2019

Recently, the finding of cancer stem cells in brain tumors has increased the possibilities

for advancing new therapeutic approaches with the aim to overcome the limits of current available

treatments. In addition, a role for ion channels, particularly...

(This article belongs to the Special Issue Ion Channels in Cancer)
  • Article
  • Open Access
30 Citations
3,841 Views
14 Pages

Oxidative Stress-Induced TRPV2 Expression Increase Is Involved in Diabetic Cataracts and Apoptosis of Lens Epithelial Cells in a High-Glucose Environment

  • Linghui Chen,
  • Yanzhuo Chen,
  • Wen Ding,
  • Tao Zhan and ,
  • Jie Zhu,
  • Lesha Zhang,
  • Han Wang,
  • Bing Shen and
  • Yong Wang
  • + 4 authors+ 0 author

2 April 2022

Cataracts are a serious complication of diabetes. In long-term hyperglycemia, intracellular Ca2+ concentration ([Ca2+]i) and reactive oxygen species (ROS) are increased. The apoptosis of lens epithelial cells plays a key role in the development of ca...

(This article belongs to the Special Issue TRP Channels in Oxidative Stress Signalling)
  • Article
  • Open Access
1 Citations
1,863 Views
16 Pages

4D-DIA-Based Quantitative Proteomic Analysis Reveals the Involvement of TRPV2 Protein in Duck Tembusu Virus Replication

  • Jimin Chen,
  • Fan Yang,
  • Lianjie Lai,
  • Huihuang Li and ,
  • Chengfu Pan,
  • Xinguo Bao,
  • Weimin Lin and
  • Ruiyi Lin
  • + 3 authors+ 0 author

26 November 2024

Duck Tembusu virus (DTMUV), a novel positive-sense RNA virus, has caused significant economic losses in the poultry industry of Eastern and Southeast Asia since its outbreak in 2010. Furthermore, the rapid transmission and potential zoonotic nature o...

(This article belongs to the Section Animal Viruses)
  • Article
  • Open Access
5 Citations
3,354 Views
16 Pages

Intracellular Helix-Loop-Helix Domain Modulates Inactivation Kinetics of Mammalian TRPV5 and TRPV6 Channels

  • Lisandra Flores-Aldama,
  • Daniel Bustos,
  • Deny Cabezas-Bratesco,
  • Wendy Gonzalez and
  • Sebastian E. Brauchi

24 February 2023

TRPV5 and TRPV6 are calcium-selective ion channels expressed at the apical membrane of epithelial cells. Important for systemic calcium (Ca2+) homeostasis, these channels are considered gatekeepers of this cation transcellular transport. Intracellula...

(This article belongs to the Special Issue Ion Channels and Biosignal Transduction)
  • Article
  • Open Access
6 Citations
3,992 Views
15 Pages

CRISPR Deletion of a SVA Retrotransposon Demonstrates Function as a cis-Regulatory Element at the TRPV1/TRPV3 Intergenic Region

  • Emma Price,
  • Olympia Gianfrancesco,
  • Patrick T. Harrison,
  • Bernhard Frank and ,
  • Vivien J. Bubb and
  • John P. Quinn
  • + 1 author+ 0 author

15 February 2021

SINE-VNTR-Alu (SVA) retrotransposons are a subclass of transposable elements (TEs) that exist only in primate genomes. TE insertions can be co-opted as cis-regulatory elements (CREs); however, the regulatory potential of SVAs has predominantly been d...

(This article belongs to the Special Issue The Role of Polymorphic Variation in Non-coding DNA in Predicting Disease)
  • Article
  • Open Access
9 Citations
5,384 Views
17 Pages

Comparative Analysis of Single-Molecule Dynamics of TRPV1 and TRPV4 Channels in Living Cells

  • Yutaro Kuwashima,
  • Masataka Yanagawa,
  • Mitsuhiro Abe,
  • Michio Hiroshima and ,
  • Masahiro Ueda,
  • Makoto Arita and
  • Yasushi Sako
  • + 2 authors+ 0 author

TRPV1 and TRPV4, members of the transient receptor potential vanilloid family, are multimodal ion channels activated by various stimuli, including temperature and chemicals. It has been demonstrated that TRPV channels function as tetramers; however,...

(This article belongs to the Special Issue Applications of Advanced Imaging and Analytical Microscopic Techniques on Molecular and Cell Biology)
  • Article
  • Open Access
35 Citations
9,208 Views
13 Pages

Expression of Transient Receptor Potential Vanilloid (TRPV) Channels in Different Passages of Articular Chondrocytes

  • Ismail M. Hdud,
  • Abdelrafea A. El-Shafei,
  • Paul Loughna,
  • Richard Barrett-Jolley and
  • Ali Mobasheri

10 April 2012

Ion channels play important roles in chondrocyte mechanotransduction. The transient receptor potential vanilloid (TRPV) subfamily of ion channels consists of six members. TRPV1-4 are temperature sensitive calcium-permeable, relatively non-selective c...

(This article belongs to the Special Issue Membrane Transport)
  • Review
  • Open Access
33 Citations
7,621 Views
24 Pages

Pathophysiological Roles of the TRPV4 Channel in the Heart

  • Sébastien Chaigne,
  • Solène Barbeau,
  • Thomas Ducret,
  • Romain Guinamard and
  • David Benoist

17 June 2023

The transient receptor potential vanilloid 4 (TRPV4) channel is a non-selective cation channel that is mostly permeable to calcium (Ca2+), which participates in intracellular Ca2+ handling in cardiac cells. It is widely expressed through the body and...

(This article belongs to the Section Cells of the Cardiovascular System)
  • Review
  • Open Access
61 Citations
13,114 Views
17 Pages

TRPV3 in Drug Development

  • Lisa M. Broad,
  • Adrian J. Mogg,
  • Elizabeth Eberle,
  • Marcia Tolley and ,
  • Dominic L. Li and
  • Kelly L. Knopp
  • + 1 author+ 0 author

9 September 2016

Transient receptor potential vanilloid 3 (TRPV3) is a member of the TRP (Transient Receptor Potential) super-family. It is a relatively underexplored member of the thermo-TRP sub-family (Figure 1), however, genetic mutations and use of gene knock-out...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
13 Citations
8,359 Views
17 Pages

29 October 2024

Transient receptor potential vanilloid (TRPV) channel proteins belong to the superfamily of TRP proteins that form cationic channels in the animal cell membranes. These proteins have various subtype-specific functions, serving, for example, as sensor...

(This article belongs to the Special Issue Feature Papers in Biosensors Section 2024)
  • Article
  • Open Access
17 Citations
3,975 Views
17 Pages

Regulation of the Membrane Trafficking of the Mechanosensitive Ion Channels TRPV1 and TRPV4 by Zonular Tension, Osmotic Stress and Activators in the Mouse Lens

  • Yosuke Nakazawa,
  • Rosica S. Petrova,
  • Yuki Sugiyama,
  • Noriaki Nagai and ,
  • Hiroomi Tamura and
  • Paul J. Donaldson
  • + 1 author+ 0 author

23 November 2021

Lens water transport generates a hydrostatic pressure gradient that is regulated by a dual-feedback system that utilizes the mechanosensitive transient receptor potential vanilloid (TRPV) channels, TRPV1 and TRPV4, to sense changes in mechanical tens...

(This article belongs to the Special Issue TRP Channels in Physiology and Pathophysiology)
  • Review
  • Open Access
41 Citations
9,857 Views
28 Pages

TRPV3: Structure, Diseases and Modulators

  • Wuyue Su,
  • Xue Qiao,
  • Wumei Wang,
  • Shengnan He and ,
  • Ke Liang and
  • Xuechuan Hong
  • + 1 author+ 0 author

12 January 2023

Transient receptor potential vanillin 3 (TRPV3) is a member of the transient receptor potential (TRP) superfamily. As a Ca2+-permeable nonselective cation channel, TRPV3 can recognize thermal stimulation (31–39 °C), and it plays an importan...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
9 Citations
3,957 Views
19 Pages

TRPV6 Regulation by Cis-22a and Cholesterol

  • Christina Humer,
  • Sonja Lindinger,
  • Aline L. Carrel,
  • Christoph Romanin and
  • Carmen Höglinger

The highly calcium-selective transient receptor potential vanilloid-type channel TRPV6 is important for epithelial Ca2+ transport. Proper regulation of the inherently constitutively active TRPV6 channels is intricate in preserving Ca2+ homeostasis, w...

(This article belongs to the Special Issue Lipid-Gating and Lipid-Protein Interactions in Ion Channels)
  • Article
  • Open Access
24 Citations
6,430 Views
19 Pages

Regulation of TGFβ Signalling by TRPV4 in Chondrocytes

  • Steven Woods,
  • Evelyn A. Humphreys,
  • Nicola Bates,
  • Sophie Alice Richardson and ,
  • Shweta Yogesh Kuba,
  • Imogen R. Brooks,
  • Stuart A. Cain and
  • Susan J. Kimber
  • + 3 authors+ 0 author

24 March 2021

The growth factor TGFβ and the mechanosensitive calcium-permeable cation channel TRPV4 are both important for the development and maintenance of many tissues. Although TRPV4 and TGFβ both affect core cellular functions, how their signals are integrat...

  • Article
  • Open Access
53 Citations
7,282 Views
10 Pages

15 June 2018

The Transient Receptor Potential (TRP) family of selective and non-selective ion channels is well represented throughout the mammalian gastrointestinal track. Several members of the Transient Receptor Potential Vanilloid (TRPV) subfamily have been id...

(This article belongs to the Special Issue TRP Channels in Health and Disease)
  • Article
  • Open Access
14 Citations
2,858 Views
13 Pages

14 January 2023

Previously, we reported a mechanosensitive ion channel, TRPV4, along with functional connexin hemichannels on the basolateral surface of the ocular nonpigmented ciliary epithelium (NPE). In the lens, TRPV4-mediated hemichannel opening is part of a fe...

(This article belongs to the Special Issue TRP Channels in Physiology and Pathophysiology)
  • Feature Paper
  • Review
  • Open Access
3 Citations
1,676 Views
18 Pages

The Role of TRPV1 in Type 1 Diabetes

  • Kelly Silva-Picazo and
  • Euan R. O. Allan

18 December 2025

Transient receptor potential vanilloid 1 (TRPV1) is an ion channel expressed in sensory neurons, immune cells, pancreatic islets, and vascular tissues. Initially recognized for its role in thermosensation and nociception, TRPV1 has emerged as a key r...

  • Review
  • Open Access
29 Citations
8,212 Views
22 Pages

TRPV3 Ion Channel: From Gene to Pharmacology

  • Aleksandr P. Kalinovskii,
  • Lyubov L. Utkina,
  • Yuliya V. Korolkova and
  • Yaroslav A. Andreev

Transient receptor potential vanilloid subtype 3 (TRPV3) is an ion channel with a sensory function that is most abundantly expressed in keratinocytes and peripheral neurons. TRPV3 plays a role in Ca2+ homeostasis due to non-selective ionic conductivi...

(This article belongs to the Special Issue Ion Channels as Therapeutic Target: Drug Design and Pharmacological Investigation)
  • Article
  • Open Access
1,729 Views
14 Pages

Determinants for Activation of the Ion Channel TRPV3 by Weak Acids

  • Daniel Rudolf,
  • Inês C. A. Pombeiro Stein,
  • Toni Sturhahn,
  • Julian Wunder and ,
  • Axel Hage and
  • Andreas Leffler
  • + 1 author+ 0 author

26 August 2025

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 l...

(This article belongs to the Special Issue TRP Channels: Mechanisms, Functions, and Therapeutic Implications)
  • Review
  • Open Access
29 Citations
7,593 Views
15 Pages

Novel Insights into the Role of Keratinocytes-Expressed TRPV3 in the Skin

  • Yaotao Guo,
  • Yajuan Song,
  • Wei Liu,
  • Tong Wang and ,
  • Xianjie Ma and
  • Zhou Yu
  • + 1 author+ 0 author

10 March 2023

TRPV3 is a non-selective cation channel that is highly expressed in keratinocytes in the skin. Traditionally, keratinocytes-expressed TRPV3 is involved in multiple physiological and pathological functions of the skin, such as itching, heat pain, and...

(This article belongs to the Section Biomacromolecules: Proteins, Nucleic Acids and Carbohydrates)
  • Article
  • Open Access
45 Citations
9,700 Views
23 Pages

Expression and Activity of TRPA1 and TRPV1 in the Intervertebral Disc: Association with Inflammation and Matrix Remodeling

  • Takuya Kameda,
  • Joel Zvick,
  • Miriam Vuk,
  • Aleksandra Sadowska and ,
  • Wai Kit Tam,
  • Victor Y. Leung,
  • Kata Bölcskei,
  • Zsuzsanna Helyes,
  • Lee Ann Applegate and
  • Karin Wuertz-Kozak
  • + 8 authors+ 3 authors

Transient receptor potential (TRP) channels have emerged as potential sensors and transducers of inflammatory pain. The aims of this study were to investigate (1) the expression of TRP channels in intervertebral disc (IVD) cells in normal and inflamm...

(This article belongs to the Special Issue Ion Channels of Nociception)
  • Review
  • Open Access
4 Citations
2,074 Views
29 Pages

25 February 2026

Cardiovascular disease (CVD) remains the leading cause of morbidity and mortality worldwide, necessitating a deeper understanding of novel regulatory mechanisms and therapeutic targets. Transient receptor potential vanilloid subtype 1 (TRPV1), a non-...

(This article belongs to the Special Issue TRP Channels in Cardiovascular and Inflammatory Disease, 2nd Edition)
  • Review
  • Open Access
26 Citations
8,202 Views
13 Pages

TRPV1 channels are polymodal cation channels located predominantly on primary afferent neurons that are activated by inflammatory mediators, capsaicin (the active component in chili peppers), and noxious heat. TRPV1 channel antagonists are potential...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)
  • Review
  • Open Access
43 Citations
8,497 Views
21 Pages

TRPV4 Role in Neuropathic Pain Mechanisms in Rodents

  • Patrícia Rodrigues,
  • Náthaly Andrighetto Ruviaro and
  • Gabriela Trevisan

22 December 2022

Neuropathic pain is a chronic pain caused by a disease or damage to the somatosensory nervous system. The knowledge about the complete mechanisms is incomplete, but the role of oxidative compounds has been evaluated. In this context, we highlight the...

(This article belongs to the Section ROS, RNS and RSS)
  • Article
  • Open Access
19 Citations
3,933 Views
21 Pages

TRPV1 Hyperfunction Contributes to Renal Inflammation in Oxalate Nephropathy

  • Chien-Lin Lu,
  • Te-Yi Teng,
  • Min-Tser Liao and
  • Ming-Chieh Ma

Inflammation worsens oxalate nephropathy by exacerbating tubular damage. The transient receptor potential vanilloid 1 (TRPV1) channel is present in kidney and has a polymodal sensing ability. Here, we tested whether TRPV1 plays a role in hyperoxaluri...

(This article belongs to the Section Molecular Toxicology)
  • Article
  • Open Access
3 Citations
3,585 Views
16 Pages

The Endocannabinoid Peptide RVD-Hemopressin Is a TRPV1 Channel Blocker

  • Constanza Suárez-Suárez,
  • Sebastián González-Pérez,
  • Valeria Márquez-Miranda,
  • Ingrid Araya-Duran and ,
  • Isabel Vidal-Beltrán,
  • Sebastián Vergara,
  • Ingrid Carvacho and
  • Fernando Hinostroza
  • + 3 authors+ 0 author

8 September 2024

Neurotransmission is critical for brain function, allowing neurons to communicate through neurotransmitters and neuropeptides. RVD-hemopressin (RVD-Hp), a novel peptide identified in noradrenergic neurons, modulates cannabinoid receptors CB1 and CB2....

  • Article
  • Open Access
11 Citations
4,914 Views
15 Pages

TRPV1 Channel in Human Eosinophils: Functional Expression and Inflammatory Modulation

  • Tobias Weihrauch,
  • Natalie Gray,
  • Daniela Wiebe,
  • Martin Schmelz and ,
  • Maren M. Limberg and
  • Ulrike Raap
  • + 1 author+ 0 author

5 February 2024

The transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel expressed on sensory neurons and immune cells. We hypothesize that TRPV1 plays a role in human eosinophil function and is modulated by inflammatory conditions. TRP...

(This article belongs to the Special Issue Inflammation in Skin and Joints)
  • Review
  • Open Access
158 Citations
22,558 Views
29 Pages

TRPV1: A Potential Drug Target for Treating Various Diseases

  • Rafael Brito,
  • Sandeep Sheth,
  • Debashree Mukherjea,
  • Leonard P. Rybak and
  • Vickram Ramkumar

23 May 2014

Transient receptor potential vanilloid 1 (TRPV1) is an ion channel present on sensory neurons which is activated by heat, protons, capsaicin and a variety of endogenous lipids termed endovanilloids. As such, TRPV1 serves as a multimodal sensor of nox...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels)
  • Review
  • Open Access
36 Citations
7,523 Views
18 Pages

The Multifaceted Functions of TRPV4 and Calcium Oscillations in Tissue Repair

  • Dongsheng Jiang,
  • Ruiji Guo,
  • Ruoxuan Dai,
  • Samuel Knoedler and ,
  • Jin Tao,
  • Hans-Günther Machens and
  • Yuval Rinkevich
  • + 2 authors+ 0 author

18 January 2024

The transient receptor potential vanilloid 4 (TRPV4) specifically functions as a mechanosensitive ion channel and is responsible for conveying changes in physical stimuli such as mechanical stress, osmotic pressure, and temperature. TRPV4 enables the...

(This article belongs to the Collection Feature Papers in “Molecular Biology”)
  • Review
  • Open Access
19 Citations
10,120 Views
16 Pages

28 December 2023

Transient receptor potential vanilloid 1 (TRPV1) is a transmembrane and non-selective cation channel protein, which can be activated by various physical and chemical stimuli. Recent studies have shown the strong pathogenetic associations of TRPV1 wit...

  • Article
  • Open Access
13 Citations
3,505 Views
27 Pages

In Silico Drug Repurposing Framework Predicts Repaglinide, Agomelatine and Protokylol as TRPV1 Modulators with Analgesic Activity

  • Corina Andrei,
  • Dragos Paul Mihai,
  • Anca Zanfirescu,
  • George Mihai Nitulescu and
  • Simona Negres

Pain is one of the most common symptoms experienced by patients. The use of current analgesics is limited by low efficacy and important side effects. Transient receptor potential vanilloid-1 (TRPV1) is a non-selective cation channel, activated by cap...

(This article belongs to the Special Issue In Silico Pharmacology for Evidence-Based and Precision Medicine)
  • Article
  • Open Access
8 Citations
4,048 Views
19 Pages

21 March 2021

Several years ago, the crystallographic structures of the transient receptor potential vanilloid 1 (TRPV1) in the presence of agonists and antagonists were reported, providing structural information about its chemical activation and inactivation. TRP...

(This article belongs to the Special Issue Computational Methods for Drug Discovery and Design II)
  • Review
  • Open Access
96 Citations
18,251 Views
20 Pages

TRPV1: A Target for Rational Drug Design

  • Vincenzo Carnevale and
  • Tibor Rohacs

23 August 2016

Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective, Ca2+ permeable cation channel activated by noxious heat, and chemical ligands, such as capsaicin and resiniferatoxin (RTX). Many compounds have been developed that either activate o...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts)
  • Review
  • Open Access
56 Citations
7,771 Views
14 Pages

TRPV4 Mechanotransduction in Fibrosis

  • Ravi K. Adapala,
  • Venkatesh Katari,
  • Lakshminarayan Reddy Teegala,
  • Sathwika Thodeti and ,
  • Sailaja Paruchuri and
  • Charles K. Thodeti
  • + 1 author+ 0 author

6 November 2021

Fibrosis is an irreversible, debilitating condition marked by the excessive production of extracellular matrix and tissue scarring that eventually results in organ failure and disease. Differentiation of fibroblasts to hypersecretory myofibroblasts i...

(This article belongs to the Special Issue Biomechanical Signaling and Fibrosis)
  • Review
  • Open Access
48 Citations
16,826 Views
19 Pages

TRPV1 Antagonists and Chronic Pain: Beyond Thermal Perception

  • Michael R. Brandt,
  • Chad E. Beyer and
  • Stephen M. Stahl

2 February 2012

In the last decade, considerable evidence as accumulated to support the development of Transient Receptor Potential Vanilloid 1 (TRPV1) antagonists for the treatment of various chronic pain conditions. Whereas there is a widely accepted rationale for...

(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
  • Review
  • Open Access
27 Citations
7,756 Views
25 Pages

TRPV Channels in Osteoarthritis: A Comprehensive Review

  • Changshun Chen,
  • Fei Yang,
  • Rongjin Chen,
  • Chenhui Yang and ,
  • Hefang Xiao,
  • Bin Geng and
  • Yayi Xia
  • + 2 authors+ 0 author

29 February 2024

Osteoarthritis (OA) is a debilitating joint disorder that affects millions of people worldwide. Despite its prevalence, our understanding of the underlying mechanisms remains incomplete. In recent years, transient receptor potential vanilloid (TRPV)...

(This article belongs to the Special Issue TRP Channels in Cardiovascular and Inflammatory Disease)
  • Article
  • Open Access
2 Citations
2,677 Views
15 Pages

Quantitative Predictive Studies of Multiple Biological Activities of TRPV1 Modulators

  • Xinmiao Wei,
  • Tengxin Huang,
  • Zhijiang Yang,
  • Li Pan and ,
  • Liangliang Wang and
  • Junjie Ding
  • + 1 author+ 0 author

5 January 2024

TRPV1 channel agonists and antagonists, which have powerful analgesic effects without the addictive qualities associated with traditional analgesics, have become a focus area for the development of novel analgesics. In this study, quantitative struct...

(This article belongs to the Special Issue Recent Progress for Structure and Function Prediction of Protein and RNA)
  • Review
  • Open Access
38 Citations
9,632 Views
19 Pages

16 October 2017

Beyond providing evolutionary advantages, venoms offer unique research tools, as they were developed to target functionally important proteins and pathways. As a key pain receptor in the nociceptive pathway, transient receptor potential vanilloid 1 (...

(This article belongs to the Special Issue Toxins in Drug Discovery and Pharmacology)
  • Article
  • Open Access
29 Citations
9,238 Views
11 Pages

Unique Responses are Observed in Transient Receptor Potential Ankyrin 1 and Vanilloid 1 (TRPA1 and TRPV1) Co-Expressing Cells

  • Laura R. Sadofsky,
  • Koti T. Sreekrishna,
  • Yakang Lin,
  • Renee Schinaman and ,
  • Kate Gorka,
  • Yogita Mantri,
  • John Christian Haught,
  • Thomas G. Huggins,
  • Robert J. Isfort and
  • Alyn H. Morice
  • + 6 authors+ 1 author

11 June 2014

Transient receptor potential (TRP) ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1) receptors are implicated in modulation of cough and nociception. In vivo, TRPA1 and TRPV1 are often co-expressed in neurons and TRPA1V1 hetero-tetramer formation is noted in...

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels)
  • Review
  • Open Access
47 Citations
8,420 Views
17 Pages

TRPV1 Channel: A Noxious Signal Transducer That Affects Mitochondrial Function

  • Rebeca Juárez-Contreras,
  • Karina Angélica Méndez-Reséndiz,
  • Tamara Rosenbaum,
  • Ricardo González-Ramírez and
  • Sara Luz Morales-Lázaro

24 November 2020

The Transient Receptor Vanilloid 1 (TRPV1) or capsaicin receptor is a nonselective cation channel, which is abundantly expressed in nociceptors. This channel is an important transducer of several noxious stimuli, having a pivotal role in pain develop...

(This article belongs to the Section Biochemistry)
  • Review
  • Open Access
56 Citations
7,794 Views
8 Pages

Role of the TRPV Channels in the Endoplasmic Reticulum Calcium Homeostasis

  • Aurélien Haustrate,
  • Natalia Prevarskaya and
  • V’yacheslav Lehen’kyi

28 January 2020

It has been widely established that transient receptor potential vanilloid (TRPV) channels play a crucial role in calcium homeostasis in mammalian cells. Modulation of TRPV channels activity can modify their physiological function leading to some dis...

(This article belongs to the Section Intracellular and Plasma Membranes)

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