Transient receptor potential vanilloid (TRPV) channels are a member of the TRP superfamily, which consists of six proteins and is expressed in many neuronal and non-neuronal cells. Among them, TRPV1-4 are non-selective cation channels that are highly sensitive to temperature changes, while TRPV5-6 are channels that are highly selective to Ca2+. These cation channels have attracted great interest academically, especially from a pharmacological perspective. TRPV channels play a vital role in many physiological processes and can be regulated by a variety of endogenous stimuli as well as a range of natural and synthetic compounds. The regulation of their activities can lead to a variety of diseases and disorders, such as neurodegenerative diseases, pain, cancer, and skin diseases. In fact, several TRPV1 and TRPV3 modulators have been developed for clinical use. Therefore, the development of TRPV channel modulators has important clinical significance and value. Herein, we focused on and summarized the latest research progress of endogenous and exogenous ligands of six TRPV channels and their pharmacological effects on related diseases.
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http://dx.doi.org/10.2174/0115680266294569241115053420 | DOI Listing |
Curr Top Med Chem
January 2025
School of Pharmacy & School of Biological and Food Engineering, Changzhou University, Changzhou, 213164, Jiangsu, PR China.
Neurochem Res
January 2025
Department of Physiology, Faculty of Medicine, University of Ondokuz Mayıs, Samsun, Türkiye.
In the present study, the effects of the acetylcholinesterase (AChE) enzyme inhibitor rivastigmine (RIVA) on spike-wave discharges (SWDs), memory impairment, anxiety-like behavior, and the transient receptor potential vanilloid 1 (TRPV1) gene expression were investigated in genetic absence epileptic Wistar Albino Glaxo/Rijswijk (WAG/Rij) rats. After tripolar electrodes were implanted on the WAG/Rij rats' skulls, single doses of 0.125, 0.
View Article and Find Full Text PDFCardiovasc Ther
January 2025
Department of Cardiovascular Medicine, Third Hospital of Shanxi Medical University, Shanxi Bethune Hospital, Shanxi Academy of Medical Sciences, Tongji Shanxi Hospital, Taiyuan, Shanxi Province 030032, China.
This research is aimed at unravelling the intricate relationship between transient receptor potential vanilloid 6 (TRPV6), protein kinase A (PKA), uncoupling protein 2 (UCP2), and atherosclerosis. By shedding light on the role of the TRPV6/PKA/UCP2 pathway in inhibiting inflammatory response and cell apoptosis in coronary atherosclerotic plaques, this study provides valuable insights into potential therapeutic targets for treating coronary artery disease (CAD). We established animal and cell models of atherosclerosis.
View Article and Find Full Text PDFPlant Foods Hum Nutr
December 2024
College of Food Science and Technology, Huazhong Agricultural University, No. 1, Shuzishan Road, Wuhan, 8430070, China.
This study aimed to investigate the protective effect of a novel capsaicinoid glucoside (CG) against HO-induced oxidative stress in HepG2 cells and elucidate its underlying molecular mechanism. CG treatment significantly reduced HO-induced cell mortality and attenuated the production of lactate dehydrogenase and malondialdehyde in a dose-dependent manner. Moreover, CG drastically reduced the ROS levels 18.
View Article and Find Full Text PDFSci Rep
December 2024
Institute of Molecular and Cell Biology (IMCB), Agency for Science, Technology and Research (A*STAR), 61 Biopolis Drive, Proteos, Singapore, 138673, Republic of Singapore.
Signaling interplay between the histamine 1 receptor (H1R) and transient receptor potential cation channel subfamily V member 1 (TRPV1) in mediating histaminergic itch has been well-established in mammalian models, but whether this is conserved in humans remains to be confirmed due to the difficulties in obtaining human sensory neurons (SNs) for experimentation. Additionally, previously reported species-specific differences in TRPV1 function indicate that use of human SNs is vital for drug candidate screening to have a higher chance of identifying clinically effective TRPV1 antagonists. In this study, we built a histamine-dependent itch model using peripheral SNs derived from human induced pluripotent stem cells (hiPSC-SNs), which provides an accessible source of human SNs for pre-clinical drug screening.
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