keyword
https://read.qxmd.com/read/38514041/small-molecules-targeting-canonical-transient-receptor-potential-channels-an-update
#1
REVIEW
Hua Liu, Min Fu, Yifan Zhang, Qidong You, Lei Wang
Transient receptor potential canonical (TRPC) channels belong to an important class of non-selective cation channels. This channel family consists of multiple members that widely participate in various physiological and pathological processes. Previous studies have uncovered the intricate regulation of these channels, as well as the spatial arrangement of TRPCs and the binding sites for various small molecule compounds. Multiple small molecules have been identified as selective agonists or inhibitors targeting different subtypes of TRPC, including potential preclinical drug candidates...
March 19, 2024: Drug Discovery Today
https://read.qxmd.com/read/38511066/role-of-trp-channels-in-carcinogenesis-and-metastasis-pathophysiology-and-regulation-by-non-coding-rnas
#2
REVIEW
Assiya Turgambayeva, Samal Duisekova, Gulnara Tashenova, Aigul Tulebayeva, Gulnara Kapanova, Aida Akhenbekova, Ammad Ahmad Farooqi
In 2021, David Julius and Ardem Patapoutian received Nobel Prize in Physiology or Medicine for their ground-breaking discoveries in the functional characterization of receptors for temperature and touch. Transient receptor potential (TRP) channels have captivated tremendous appreciation as promising drug targets over the past few years because of central involvement in different cancers. Based on the insights gleaned from decades of high-quality research, basic and clinical scientists have unveiled how Transient receptor potential channels regulated cancer onset and progression...
June 2024: Non-Coding RNA Research
https://read.qxmd.com/read/38490377/porcine-transient-receptor-potential-channel-1-trpc1-regulates-muscle-growth-via-the-wnt-%C3%AE-catenin-and-wnt-ca-2-pathways
#3
JOURNAL ARTICLE
Xin Hao, Yu Fu, Shixin Li, Jingru Nie, Bo Zhang, Hao Zhang
Transient receptor potential canonical (TRPC) channels allow the intracellular entry of Ca2+ and play important roles in several physio-pathological processes. In this study, we constructed transgenic mice expressing porcine TRPC1 (Tg-pTRPC1) to verify the effects of TRPC1 on skeletal muscle growth and elucidate the underlying mechanism. Porcine TRPC1 increased the muscle mass, fiber cross-sectional area, and exercise endurance of mice and accelerated muscle repair and regeneration. TRPC1 overexpression enhanced β-catenin expression and promoted myogenesis, which was partly reversed by inhibitors of β-catenin...
March 13, 2024: International Journal of Biological Macromolecules
https://read.qxmd.com/read/38423141/transient-receptor-potential-trp-channels-in-sebastes-schlegelii-genome-wide-identification-and-thermotrp-expression-analysis-under-high-temperature
#4
JOURNAL ARTICLE
Jinwei Huang, Xueying Wang, Xiaoyang Guo, Qinghua Liu, Jun Li
Transient Receptor Potential (TRP) channels, essential for sensing environmental stimuli, are widely distributed. Among them, thermosensory TRP channels play a crucial role in temperature sensing and regulation. Sebastes schlegelii, a significant aquatic economic species, exhibits sensitivity to temperature across multiple aspects. In this study, we identified 18 SsTRP proteins using whole-genome scanning. Motif analysis revealed motif 2 in all TRP proteins, with conserved motifs in subfamilies. TRP-related domains, anchored repeats, and ion-transmembrane domains were found...
February 27, 2024: Gene
https://read.qxmd.com/read/38397074/pharmacological-activation-of-trpc6-channel-prevents-colitis-progression
#5
JOURNAL ARTICLE
Kazuhiro Nishiyama, Yuri Kato, Akiyuki Nishimura, Xinya Mi, Ryu Nagata, Yasuo Mori, Yasu-Taka Azuma, Motohiro Nishida
We recently reported that transient receptor potential canonical (TRPC) 6 channel activity contributes to intracellular Zn2+ homeostasis in the heart. Zn2+ has also been implicated in the regulation of intestinal redox and microbial homeostasis. This study aims to investigate the role of TRPC6-mediated Zn2+ influx in the stress resistance of the intestine. The expression profile of TRPC1-C7 mRNAs in the actively inflamed mucosa from inflammatory bowel disease (IBD) patients was analyzed using the GEO database...
February 18, 2024: International Journal of Molecular Sciences
https://read.qxmd.com/read/38384797/direct-modulation-of-trpc-ion-channels-by-g%C3%AE-proteins
#6
REVIEW
Hana Kang, Jinhyeong Kim, Christine Haewon Park, Byeongseok Jeong, Insuk So
GPCR-Gi protein pathways are involved in the regulation of vagus muscarinic pathway under physiological conditions and are closely associated with the regulation of internal visceral organs. The muscarinic receptor-operated cationic channel is important in GPCR-Gi protein signal transduction as it decreases heart rate and increases GI rhythm frequency. In the SA node of the heart, acetylcholine binds to the M2 receptor and the released Gβγ activates GIRK (I(K,ACh)) channel, inducing a negative chronotropic action...
2024: Frontiers in Physiology
https://read.qxmd.com/read/38279926/structural-and-accessibility-studies-highlight-the-differential-binding-of-clemizole-to-trpc5-and-trpc6
#7
JOURNAL ARTICLE
Uzma Saqib, Isaac S Demaree, Alexander G Obukhov, Mirza S Baig, Mohd Shahnawaz Khan, Nojood Altwaijry, Mochammad Arfin Fardiansyah Nasution, Kenji Mizuguchi, Krishnan Hajela
Transient Receptor Potential Canonical 5 (T RP C5) and T RP C6 channels play critical physiological roles in various cell types. Their involvement in numerous disease progression mechanisms has led to extensive searches for their inhibitors. Although several potent T RP C inhibitors have been developed and the structure of their binding sites were mapped using cryo electron microscopy, a comprehensive understanding of the molecular interactions within the inhibitor binding site of T RP Cs remains elusive. This study aimed to decipher the structural determinants and molecular mechanisms contributing to the differential binding of clemizole to T RP C5 and T RP C6, with a particular focus on the accessibility of binding site residues...
January 27, 2024: Journal of Biomolecular Structure & Dynamics
https://read.qxmd.com/read/38233779/identification-of-transient-receptor-potential-channel-genes-from-the-swimming-crab-portunus-trituberculatus-and-their-expression-profiles-under-acute-temperature-stress
#8
JOURNAL ARTICLE
Yichen Qian, Qiaoling Yu, Jun Zhang, Yaoyao Han, Xi Xie, Dongfa Zhu
BACKGROUND: Temperature is an important environment factor that is critical to the survival and growth of crustaceans. However, the mechanisms by which crustaceans detect changes in temperature are still unclear. The transient receptor potential (TRP) channels are non-selective cation channels well known for properties in temperature sensation. However, comprehensive understandings on TRP channels as well as their temperature sensing functions are still lacking in crustaceans. RESULTS: In this study, a total of 26 TRP genes were identified in the swimming crab, Portunus trituberculatus, which can be classified into TRPA, TRPC, TRPP, TRPM, TRPML, TRPN and TRPV...
January 17, 2024: BMC Genomics
https://read.qxmd.com/read/38185057/discovery-of-n-alkyl-n-benzyl-thiazoles-as-novel-trpc-antagonists-for-the-treatment-of-glioblastoma-multiforme
#9
JOURNAL ARTICLE
Shanshan Wang, Xiaoxue Li, Yuemiao Hu, Lin Wang, Guangyao Lv, Yuxin Feng, Ziqiang Sun, Zhengyu Cao, Yi Liu, Hongbo Wang
Glioblastoma multiforme represents a substantial clinical challenge. Transient receptor potential channel (TRPC) antagonists might provide new therapeutic options for this aggressive cancer. In this study, a series of N-alkyl-N-benzoyl and N-alkyl-N-benzyl thiazoles were designed and prepared using a scaffold-hopping strategy and evaluated as TRPC6 antagonists. This resulted in the discovery of 15g, a potent TRPC antagonist that exhibited suitable inhibitory micromolar activities against TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7 and displayed noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines...
December 22, 2023: European Journal of Medicinal Chemistry
https://read.qxmd.com/read/38174113/canonical-transient-receptor-potential-channel-1-aggravates-myocardial-ischemia-and-reperfusion-injury-by-upregulating-reactive-oxygen-species
#10
JOURNAL ARTICLE
Hui-Nan Zhang, Meng Zhang, Wen Tian, Wei Quan, Fan Song, Shao-Yuan Liu, Xiao-Xiao Liu, Dan Mo, Yang Sun, Yuan-Yuan Gao, Wen Ye, Ying-Da Feng, Chang-Yang Xing, Chen Ye, Lei Zhou, Jing-Ru Meng, Wei Cao, Xiao-Qiang Li
The canonical transient receptor potential channel (TRPC) proteins form Ca2+ -permeable cation channels that are involved in various heart diseases. However, the roles of specific TRPC proteins in myocardial ischemia/reperfusion (I/R) injury remain poorly understood. We observed that TRPC1 and TRPC6 were highly expressed in the area at risk (AAR) in a coronary artery ligation induced I/R model. Trpc1 -/- mice exhibited improved cardiac function, lower serum Troponin T and serum creatine kinase level, smaller infarct volume, less fibrotic scars, and fewer apoptotic cells after myocardial-I/R than wild-type or Trpc6 -/- mice...
November 2023: Journal of Pharmaceutical Analysis
https://read.qxmd.com/read/38141370/full-length-transcriptome-reveals-the-circularly-polarized-light-response-related-molecular-genetic-characteristics-of-oratosquilla-oratoria
#11
JOURNAL ARTICLE
Fangrui Lou, Zhongjie Ren, Yongzheng Tang, Zhiqiang Han
The mantis shrimp is the only animal that can recognize circularly polarized light (CPL), but its molecular genetic characteristics are unclear. Multi-tissue level full-length (FL) transcriptome sequencing of Oratosquilla oratoria, a representative widely distributed mantis shrimp, was performed in the present study. We used comparative transcriptomics to explore the critical genes of O. oratoria selected by CPL and the GNβ gene associated with CPL signal transduction was hypothesized to be positively selected...
December 22, 2023: Comparative Biochemistry and Physiology. Part D, Genomics & Proteomics
https://read.qxmd.com/read/38132974/increased-susceptibility-to-pilocarpine-induced-status-epilepticus-and-reduced-latency-in-trpc1-4-double-knockout-mice
#12
JOURNAL ARTICLE
Fang Zheng, Kevin D Phelan, U Thaung Shwe
Canonical transient receptor potential channels (TRPCs) are a family of calcium-permeable cation channels. Previous studies have shown that heteromeric channels comprising TRPC1 and TRPC4 mediate epileptiform bursting in lateral septal neurons and hippocampal CA1 pyramidal neurons, suggesting that TRPC1/4 channels play a pro-seizure role. In this study, we utilized electroencephalography (EEG) recording and spectral analysis to assess the role of TRPC1/4 channels in the pilocarpine model of status epilepticus (SE)...
December 6, 2023: Neurology International
https://read.qxmd.com/read/38067118/store-operated-calcium-entry-increases-nuclear-calcium-in-adult-rat-atrial-and-ventricular-cardiomyocytes
#13
JOURNAL ARTICLE
Julia Hermes, Vesela Borisova, Jens Kockskämper
Store-operated calcium entry (SOCE) in cardiomyocytes may be involved in cardiac remodeling, but the underlying mechanisms remain elusive. We hypothesized that SOCE may increase nuclear calcium, which alters gene expression via calcium/calmodulin-dependent enzyme signaling, and elucidated the underlying cellular mechanisms. An experimental protocol was established in isolated adult rat cardiomyocytes to elicit SOCE by re-addition of calcium following complete depletion of sarcoplasmic reticulum (SR) calcium and to quantify SOCE in relation to the electrically stimulated calcium transient (CaT) measured in the same cell before SR depletion...
November 23, 2023: Cells
https://read.qxmd.com/read/38051199/%C3%AE-arrestin-pathway-activation-by-selective-atr1-agonism-promotes-calcium-influx-in-podocytes-leading-to-glomerular-damage
#14
JOURNAL ARTICLE
Marharyta Semenikhina, Mykhailo Fedoriuk, Mariia Stefanenko, Christine A Klemens, Alena Cherezova, Brendan Marshall, Gentzon Hall, Vladislav Levchenko, Asish Kumar Solanki, Joshua H Lipschutz, Daria V Ilatovskaya, Alexander Staruschenko, Oleg Palygin
Angiotensin Receptor blockers (ARBs) are the first-line treatment for hypertension; they act by inhibiting signaling through the angiotensin 1 receptor (AT1R). Recently, a novel biased AT1R agonist, TRV120027 (TRV), that selectively activates the β-arrestin cascade and blocks the G-protein-coupled receptor pathway has been proposed as a potential blood pressure medication. Here, we explored the effects of TRV and associated β-arrestin signaling in podocytes, essential cells of the kidney filter...
December 5, 2023: Clinical Science (1979-)
https://read.qxmd.com/read/38019356/effect-of-bi-1358894-on-cholecystokinin-tetrapeptide-cck-4-induced-anxiety-panic-symptoms-and-stress-biomarkers-a-phase-i-randomized-trial-in-healthy-males
#15
JOURNAL ARTICLE
Markus Goettel, Rene Fuertig, Salome Rebecca Mack, Stefan Just, Vikas Sharma, Andreas Wunder, Johan den Boer
INTRODUCTION: Depression, anxiety, and/or panic disorder are often comorbid and have a complex etiology mediated through the same neuronal network. Cholecystokinin-tetrapeptide (CCK-4), a synthetic analog of the endogenous neuropeptide cholecystokinin (CCK), is thought to be implicated in this network. The CCK-4 challenge model is an accepted method of investigating the pathophysiology of panic and has been shown to mediate neuronal activation via the transient receptor potential canonical (TRPC) ion channels...
November 29, 2023: CNS Drugs
https://read.qxmd.com/read/38019355/effects-of-single-and-multiple-ascending-doses-of-bi-1358894-in-healthy-male-volunteers-on-safety-tolerability-and-pharmacokinetics-two-phase-i-partially-randomised-studies
#16
JOURNAL ARTICLE
René Fuertig, Markus Goettel, Lena Herich, Josef Hoefler, Sabrina T Wiebe, Vikas Sharma
INTRODUCTION: The transient receptor potential canonical (TRPC) ion channels have been implicated in the pathophysiology of major depressive disorder (MDD), and TRPC inhibition has been shown to reduce depressive-like behaviour in rodent models of depression. BI 1358894, a small-molecule inhibitor of TRPC ion channels, is currently being developed for the treatment of MDD. OBJECTIVE: Two phase I studies assessed the safety, tolerability, and pharmacokinetics (PK) of oral BI 1358894 in fed and fasted states following a single ascending dose (SAD) [NCT03210272/1402-0001] and multiple ascending doses (MAD) [NCT03754959/1402-0002] in healthy male volunteers...
November 29, 2023: CNS Drugs
https://read.qxmd.com/read/38003608/a-putative-role-for-trpc6-in-immune-mediated-kidney-injury
#17
REVIEW
Daan C 't Hart, Johan van der Vlag, Tom Nijenhuis
Excessive activation of the immune system is the cause of a wide variety of renal diseases. However, the pathogenic mechanisms underlying the aberrant activation of the immune system in the kidneys often remain unknown. TRPC6, a member of the Ca2+ -permeant family of TRPC channels, is important in glomerular epithelial cells or podocytes for the process of glomerular filtration. In addition, TRPC6 plays a crucial role in the development of kidney injuries by inducing podocyte injury. However, an increasing number of studies suggest that TRPC6 is also responsible for tightly regulating the immune cell functions...
November 16, 2023: International Journal of Molecular Sciences
https://read.qxmd.com/read/37995056/trp-channels-in-stroke
#18
REVIEW
Pengyu Zong, Cindy X Li, Jianlin Feng, Mara Cicchetti, Lixia Yue
Ischemic stroke is a devastating disease that affects millions of patients worldwide. Unfortunately, there are no effective medications for mitigating brain injury after ischemic stroke. TRP channels are evolutionally ancient biosensors that detect external stimuli as well as tissue or cellular injury. To date, many members of the TRP superfamily have been reported to contribute to ischemic brain injury, including the TRPC subfamily (1, 3, 4, 5, 6, 7), TRPV subfamily (1, 2, 3, 4) and TRPM subfamily (2, 4, 7)...
November 23, 2023: Neuroscience Bulletin
https://read.qxmd.com/read/37971274/the-versatility-of-the-putative-transient-receptor-potential-ion-channels-in-regulating-the-calcium-signaling-in-aspergillus-nidulans
#19
JOURNAL ARTICLE
Hongchen Wang, Renwei Gao, Yuanwei Zhang, Ling Lu
Transient receptor potential (TRP) ion channels are evolutionarily conserved integral membrane proteins with non-selective ion permeability, and they are widely distributed in mammals and single-cell yeast and serve as crucial mediators of sensory signals. However, the relevant information concerning TRP channels in Aspergillus nidulans remains inadequately understood. In this study, by gene deletion, green fluorescent protein tagging, and cytosolic Ca2+ transient monitoring techniques, the biological functions of three potential TRP channels (TrpA, TrpB, and TrpC) have been explored for which they play distinct and multiple roles in hyphal growth, conidiation, responsiveness to external stress, and regulation of intracellular Ca2+ homeostasis...
November 16, 2023: MSphere
https://read.qxmd.com/read/37945647/orai1%C3%AE-and-orai1%C3%AE-support-calcium-entry-and-mammosphere-formation-in-breast-cancer-stem-cells
#20
JOURNAL ARTICLE
Isaac Jardin, Sandra Alvarado, Vanesa Jimenez-Velarde, Joel Nieto-Felipe, Jose J Lopez, Gines M Salido, Tarik Smani, Juan A Rosado
Orai1 is the pore-forming subunit of the Ca2+ -release activated Ca2+ channels that mediate store-operated Ca2+ entry (SOCE) in excitable and non-excitable cells. Two Orai1 forms have been identified in mammalian cells, the full-length variant Orai1α, and the short form Orai1β, lacking the N-terminal 63 amino acids. Stem cells were isolated from non-tumoral breast epithelial cells of the MCF10A cell line, and the most representative ER+ , HER2 or triple negative breast cancer cell lines MCF7, SKBR3 and MDA-MB-231, respectively...
November 9, 2023: Scientific Reports
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