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https://www.readbyqxmd.com/read/28154143/single-residue-molecular-switch-for-high-temperature-dependence-of-vanilloid-receptor-trpv3
#1
Beiying Liu, Feng Qin
Thermal transient receptor potential (TRP) channels, a group of ion channels from the transient receptor potential family, play important functions in pain and thermal sensation. These channels are directly activated by temperature and possess strong temperature dependence. Furthermore, their temperature sensitivity can be highly dynamic and use-dependent. For example, the vanilloid receptor transient receptor potential 3 (TRPV3), which has been implicated as a warmth detector, becomes responsive to warm temperatures only after intensive stimulation...
February 1, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28076819/full-spectral-multiplexing-of-bioluminescence-resonance-energy-transfer-in-three-trpv-channels
#2
Hermanus Johannes Ruigrok, Guillaume Shahid, Bertrand Goudeau, Florence Poulletier de Gannes, Emmanuelle Poque-Haro, Annabelle Hurtier, Isabelle Lagroye, Pierre Vacher, Stéphane Arbault, Neso Sojic, Bernard Veyret, Yann Percherancier
Multiplexed bioluminescence resonance energy transfer (BRET) assays were developed to monitor the activation of several functional transient receptor potential (TRP) channels in live cells and in real time. We probed both TRPV1 intramolecular rearrangements and its interaction with Calmodulin (CaM) under activation by chemical agonists and temperature. Our BRET study also confirmed that: (1) capsaicin and heat promoted distinct transitions, independently coupled to channel gating, and that (2) TRPV1 and Ca(2+)-bound CaM but not Ca(2+)-free CaM were preassociated in resting live cells, while capsaicin activation induced both the formation of more TRPV1/CaM complexes and conformational changes...
January 10, 2017: Biophysical Journal
https://www.readbyqxmd.com/read/28024685/decreases-in-15-lipoxygenase-metabolites-in-olmsted-syndrome-model-rats
#3
Masato Wakabayashi, Takeshi Yoshioka, Kenichi Higashino, Yoshito Numata, Yasuyuki Igarashi, Akio Kihara
BACKGROUND: Olmsted syndrome (OS) is a congenital dermatosis characterized by palmoplantar keratoderma and periorificial keratotic plaque. TRPV3 (transient receptor potential vanilloid subtype 3) encodes a thermosensitive Ca(2+) channel and is the causative gene of OS. However, the molecular mechanism that causes the pathological development of OS is unclear. OBJECTIVE: We aimed to investigate the molecular mechanisms underlying OS pathology from the perspective of lipid metabolism...
December 15, 2016: Journal of Dermatological Science
https://www.readbyqxmd.com/read/27934457/stereoselective-synthesis-of-a-dipyridyl-transient-receptor-potential-vanilloid-3-trpv3-antagonist
#4
Eric A Voight, Jerome F Daanen, Robert G Schmidt, Arthur Gomtsyan, Michael J Dart, Philip R Kym
An efficient asymmetric synthesis of dipyridyl TRPV3 antagonist 1 is reported. The four-step route involves two C-C bond-forming steps, a highly diastereoselective alkene hydration, and asymmetric ketone hydrosilylation in 97% ee.
December 2, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27875791/localization-and-expression-patterns-of-trp-channels-in-submandibular-gland-development
#5
Motoya Fujiseki, Masahito Yamamoto, Sobhan Ubaidus, Takashi Shinomiya, Shinichi Abe, Masakazu Tazaki, Hitoshi Yamamoto
OBJECTIVE: Expression of Transient receptor potential (TRP) channels: TRP canonical (TRPC)1, TRP vanilloid (TRPV)3, TRPV4 and TRP melastatin (TRPM)8 in adult rat salivary gland has recently been reported. The authors investigated expression of these TRP channels in the submandibular gland during early developmental stage in which the cell constitution is different, and discussed the function of TRP in the submandibular gland in early development. DESIGN: Using rat submandibular gland at embryonic days (E)18 and E20 and postnatal days (PN)0 and PN5 and PN28, expression of TRPV3, TRPV4, TRPC1 and TRPM8 was investigated using real-time polymerase chain reaction (RT-PCR) and immunohistochemistry...
February 2017: Archives of Oral Biology
https://www.readbyqxmd.com/read/27757589/trp-channels-potential-drug-target-for-neuropathic-pain
#6
REVIEW
Lovish Marwaha, Yashika Bansal, Raghunath Singh, Priyanka Saroj, Ranjana Bhandari, Anurag Kuhad
Neuropathic pain is a debilitating disease which affects central as well as peripheral nervous system. Transient receptor potential (TRP) channels are ligand-gated ion channels that detect physical and chemical stimuli and promote painful sensations via nociceptor activation. TRP channels have physiological role in the mechanisms controlling several physiological responses like temperature and mechanical sensations, response to painful stimuli, taste, and pheromones. TRP channel family involves six different TRPs (TRPV1, TRPV2, TRPV3, TRPV4, TRPM8, and TRPA1) which are expressed in pain sensing neurons and primary afferent nociceptors...
December 2016: Inflammopharmacology
https://www.readbyqxmd.com/read/27754757/trpv3-mutants-causing-olmsted-syndrome-induce-impaired-cell-adhesion-and-nonfunctional-lysosomes
#7
Manoj Yadav, Chandan Goswami
TRPV3 is a non-selective cationic channel and is important for several physiological functions. It can be activated by physiological temperature and selective endogenous and exogenous compounds. TRPV3 is one of the key ion channel involved in Ca(2+)-signaling in keratinocyte and thus involved in skin-related functions. Recently, naturally occurring mutations in TRPV3, namely G573A, G573S, G573C and W692G have been detected which are linked with the development of pathophysiological conditions such as Olmsted Syndrome (OS) and other skin disorders...
October 18, 2016: Channels
https://www.readbyqxmd.com/read/27618069/trpv3-in-drug-development
#8
REVIEW
Lisa M Broad, Adrian J Mogg, Elizabeth Eberle, Marcia Tolley, Dominic L Li, Kelly L Knopp
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-outs and selective pharmacological tools are helping to provide insights into its role and therapeutic potential. TRPV3 is highly expressed in skin, where it is implicated in skin physiology and pathophysiology, thermo-sensing and nociception. Gain of function TRPV3 mutations in rodent and man have enabled the role of TRPV3 in skin health and disease to be particularly well defined...
September 9, 2016: Pharmaceuticals
https://www.readbyqxmd.com/read/27604134/whole-exome-sequencing-analysis-reveals-trpv3-as-a-risk-factor-for-cardioembolic-stroke
#9
Caty Carrera, Jordi Jiménez-Conde, Sophia Derdak, Kelly Rabionet, Cristofol Vives-Bauzá, Carolina Soriano-Tárrega, Eva Giralt-Steinhauer, Marina Mola-Caminal, Rosa M Diaz-Navarro, Silvia Tur, Elena Muiño, Cristina Gallego-Fabrega, Sergi Beltran, Jaume Roquer, Agustin Ruiz, Oscar Sotolongo-Grau, Jurek Krupinski, Jin-Moo Lee, Carlos Cruchaga, Pilar Delgado, Rainer Malik, Brad B Worrall, Sudha Seshadri, Joan Montaner, Israel Fernández-Cadenas
Genetic studies suggest that hundreds of genes associated with stroke remain unidentified. Exome sequencing proves useful for finding new genes associated with stroke. We aimed to find new genetic risk factors for cardioembolic stroke by analysing exome sequence data using new strategies. For discovery, we analysed 42 cardioembolic stroke cases and controls with extreme phenotypes (cohort 1), and for replication, 32 cardioembolic stroke cases and controls (cohort 2) using the SeqCapExome capture kit. We then analysed the replicated genes in two new cohorts that comprised 834 cardioembolic strokes and controls (cohort 3) and 64,373 cardioembolic strokes and controls (cohort 4)...
November 30, 2016: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/27563416/the-role-of-c-fibers-in-spinal-microglia-induction-and-possible-relation-with-trpv3-expression-during-chronic-inflammatory-arthritis-in-rats
#10
Sasan Gazerani, Jalal Zaringhalam, Homa Manaheji, Sahar Golabi
INTRODUCTION: Stimulation of peptidergic fibers activates microglia in the dorsal horn. Microglia activation causes fractalkine (FKN) release, a neuron-glia signal, which enhances pain. The transient vanilloid receptor 1 (TRPV1) mediates the release of neuropeptides, which can subsequently activate glia. TRPV1 and TRPV2 are generally expressed on C and Aδ fibers, respectively. Expression of both proteins is upregulated during inflammation, but expression of TRPV3 after induction of inflammation is unclear...
July 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27541952/increased-activity-of-trpv3-in-keratinocytes-in-hypertrophic-burn-scars-with-post-burn-pruritus
#11
Hye One Kim, Yong Se Cho, Sook Young Park, In Suk Kwak, Min Gyu Choi, Bo Young Chung, Chun Wook Park, Jun Young Lee
Post burn pruritus is a common distressing sequela of burn wounds. Empirical antipruritic treatment often fails to have a satisfactory outcome, as the mechanism of it has not been fully elucidated. The aim of this study was to evaluate the manifestation of transient receptor potential vanilloid 3 (TRPV3), transient receptor potential ankyrin 1 (TRPA1) and other related receptors in post burn pruritus. Sixty-five burn patients with (n = 40) or without (n = 25) pruritus were investigated, including skin biopsies...
August 19, 2016: Wound Repair and Regeneration
https://www.readbyqxmd.com/read/27533035/the-trpm2-ion-channel-is-required-for-sensitivity-to-warmth
#12
Chun-Hsiang Tan, Peter A McNaughton
Thermally activated ion channels are known to detect the entire thermal range from extreme heat (TRPV2), painful heat (TRPV1, TRPM3 and ANO1), non-painful warmth (TRPV3 and TRPV4) and non-painful coolness (TRPM8) through to painful cold (TRPA1). Genetic deletion of each of these ion channels, however, has only modest effects on thermal behaviour in mice, with the exception of TRPM8, the deletion of which has marked effects on the perception of moderate coolness in the range 10-25 °C. The molecular mechanism responsible for detecting non-painful warmth, in particular, is unresolved...
August 25, 2016: Nature
https://www.readbyqxmd.com/read/27498155/pure-%C3%AE-9-tetrahydrocannabivarin-and-a-cannabis-sativa-extract-with-high-content-in-%C3%AE-9-tetrahydrocannabivarin-inhibit-nitrite-production-in-murine-peritoneal-macrophages
#13
Barbara Romano, Ester Pagano, Pierangelo Orlando, Raffaele Capasso, Maria Grazia Cascio, Roger Pertwee, Vincenzo Di Marzo, Angelo A Izzo, Francesca Borrelli
Historical and scientific evidence suggests that Cannabis use has immunomodulatory and anti-inflammatory effects. We have here investigated the effect of the non-psychotropic phytocannabinoid Δ(9)-tetrahydrocannabivarin (THCV) and of a Cannabis sativa extract with high (64.8%) content in THCV (THCV-BDS) on nitric oxide (NO) production, and on cannabinoid and transient receptor potential (TRP) channel expression in lipopolysaccharide (LPS)-stimulated murine peritoneal macrophages. THCV-BDS and THCV exhibited similar affinity in radioligand binding assays for CB1 and CB2 receptors, and inhibited, via CB2 but not CB1 cannabinoid receptors, nitrite production evoked by LPS in peritoneal macrophages...
August 3, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27352042/neuroactive-and-anti-inflammatory-frankincense-cembranes-a-structure-activity-study
#14
Federica Pollastro, Samantha Golin, Giuseppina Chianese, Masteria Yunovilsa Putra, Aniello Schiano Moriello, Luciano De Petrocellis, Victor García, Eduardo Munoz, Orazio Taglialatela-Scafati, Giovanni Appendino
An expeditious isolation method for the cembrane diterpene alcohols incensol (1a) and serratol (2) has been developed from respectively African and Indian frankincense. The two native alcohols and a series of semisynthetic derivatives of incensol were evaluated for transient receptor potential vanilloid 3 (TRPV3) activation and the inhibition of NF-κB, the putative molecular targets underlying the psychotropic and anti-inflammatory activities of incensol acetate (IA, 1b). Serratol (2) was the most potent TRPV3 activator, outperforming by 2 orders of magnitude the reference agonist thymol and by 1 order of magnitude incensol acetate (1b)...
July 22, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27273692/two-familial-cases-of-olmsted-like-syndrome-with-a-g573v-mutation-of-the-trpv3-gene
#15
Y P Zhi, J Liu, J W Han, Y P Huang, Z Q Gao, Y Yang, R N Wu
Olmsted syndrome (OS) is a rare disease, characterized by symmetrical, sharply defined, hyperkeratotic, mutilating plaques on the palms and soles, which are associated with periorificial keratotic plaques. Other clinical manifestations of OS include diffuse alopecia, leucokeratosis of the oral mucosa, onychodystrophy, hyperkeratotic linear streaks, follicular hyperkeratosis and constriction of the digits. A recent study identified de novo mutations in the gene for transient receptor potential vanilloid 3 (TRPV3), causing constitutive activation of the TRPV3 channel, as a cause of OS...
July 2016: Clinical and Experimental Dermatology
https://www.readbyqxmd.com/read/27184746/evidence-for-the-functional-involvement-of-members-of-the-trp-channel-family-in-the-uptake-of-na-and-nh4-by-the-ruminal-epithelium
#16
Julia Rosendahl, Hannah S Braun, Katharina T Schrapers, Holger Martens, Friederike Stumpff
Large quantities of protein are degraded in the fermentative parts of the gut to ammonia, which is absorbed, detoxified to urea, and excreted, leading to formation of nitrogenous compounds such as N2O that are associated with global warming. In ruminants, channel-mediated uptake of NH4 (+) from the rumen predominates. The molecular identity of these channels remains to be clarified. Ruminal cells and epithelia from cows and sheep were investigated using patch clamp, Ussing chamber, microelectrode techniques, and qPCR...
August 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/27084697/transient-receptor-potential-vanilloid-3-trpv3-in-the-ventral-tegmental-area-of-rat-role-in-modulation-of-the-mesolimbic-dopamine-reward-pathway
#17
Uday Singh, Santosh Kumar, Gajanan P Shelkar, Manoj Yadav, Dadasaheb M Kokare, Chandan Goswami, Ronald M Lechan, Praful S Singru
While dopamine (DA) neurons in the ventral tegmental area (VTA) drive the mesolimbic-reward pathway, confluent lines of evidence underscore the importance of transient receptor potential vanilloid (TRPV) channels as novel regulators of these neurons. Among the TRPV-subfamily, TRPV3 is of particular interest in reward, since active ingredients of flavour-enhancing spices in food serve as TRPV3 agonists and modulate DAergic neurotransmission. The nature of TRPV3 elements in the VTA and their role in driving the mesolimbic-DA-reward pathway has however, remained unexplored...
November 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27079220/polymorphisms-of-the-trpv2-and-trpv3-genes-associated-with-fibromyalgia-in-a-korean-population
#18
Dong-Jin Park, Seong-Ho Kim, Seong-Su Nah, Ji Hyun Lee, Seong-Kyu Kim, Yeon-Ah Lee, Seung-Jae Hong, Hyun-Sook Kim, Hye-Soon Lee, Hyoun Ah Kim, Chung-Il Joung, Sang-Hyon Kim, Shin-Seok Lee
OBJECTIVE: Researchers continue to gather evidence that transient receptor potential vanilloid (TRPV) channels contribute towards pain signalling pathways. However, it is unknown whether polymorphisms of the TRPV gene are associated with FM. For the first time, we investigated the association between the polymorphisms of the TRPV2 and TRPV3 genes, FM susceptibility and the severity of the symptoms. METHODS: A total of 409 patients with FM and 423 controls were enrolled from 10 medical centres that participated in the Korean nationwide FM survey...
August 2016: Rheumatology
https://www.readbyqxmd.com/read/27077528/synthesis-and-pharmacology-of-pyridin-2-yl-methanol-derivatives-as-novel-and-selective-transient-receptor-potential-vanilloid-3-antagonists
#19
Arthur Gomtsyan, Robert G Schmidt, Erol K Bayburt, Gregory A Gfesser, Eric A Voight, Jerome F Daanen, Diana L Schmidt, Marlon D Cowart, Huaqing Liu, Robert J Altenbach, Michael E Kort, Bruce Clapham, Phil B Cox, Anurupa Shrestha, Rodger Henry, David N Whittern, Regina M Reilly, Pamela S Puttfarcken, Jill-Desiree Brederson, Ping Song, Bin Li, Susan M Huang, Heath A McDonald, Torben R Neelands, Steve P McGaraughty, Donna M Gauvin, Shailen K Joshi, Patricia N Banfor, Jason A Segreti, Mohamad Shebley, Connie R Faltynek, Michael J Dart, Philip R Kym
Transient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recent studies suggest that TRPV3 may play a role in inflammation, pain sensation, and skin disorders. TRPV3 studies have been challenging, in part due to a lack of research tools such as selective antagonists. Herein, we provide the first detailed report on the development of potent and selective TRPV3 antagonists featuring a pyridinyl methanol moiety...
May 26, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27073026/trpv3-expression-and-vasodilator-function-in-isolated-uterine-radial-arteries-from-non-pregnant-and-pregnant-rats
#20
Timothy V Murphy, Arjna Kanagarajah, Sianne Toemoe, Paul P Bertrand, T Hilton Grayson, Fiona C Britton, Leo Leader, Sevvandi Senadheera, Shaun L Sandow
This study investigated the expression and function of transient receptor potential vanilloid type-3 ion channels (TRPV3) in uterine radial arteries isolated from non-pregnant and twenty-day pregnant rats. Immunohistochemistry (IHC) suggested TRPV3 is primarily localized to the smooth muscle in arteries from both non-pregnant and pregnant rats. IHC using C' targeted antibody, and qPCR of TRPV3 mRNA, suggested pregnancy increased arterial TRPV3 expression. The TRPV3 activator carvacrol caused endothelium-independent dilation of phenylephrine-constricted radial arteries, with no difference between vessels from non-pregnant and pregnant animals...
August 2016: Vascular Pharmacology
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