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Transient receptor potential ankyrin 1 (TRPA1) channel serves as a critical mediator of nociceptive signaling across neural circuits, modulating pathophysiological processes from asthma to neurogenic inflammation through its unique ability to integrate chemical, thermal, and mechanical stimuli. Real-time monitoring conformational dynamics of TRPA1 is of significance for dissecting the roles of TRPA1 channel. Here, we present a small molecular fluorescence probe FPTRP-1 featuring a state-dependent fluorescence signature that directly correlates with TRPA1 gating status. Confocal imaging verifies that the probe FPTRP-1 has high selectivity for TRPA1 channel, and can monitor the on-off states of TRPA1 in real time, providing a potential pharmacological tool to further elucidate the physiological and pathological roles of TRPA1 channel in biological systems.
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http://dx.doi.org/10.1016/j.bioorg.2025.108744 | DOI Listing |
Int J Biol Macromol
September 2025
College of Pharmacy, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China; Key Laboratory of Traditional Chinese Medicine Classical Theory, Ministry of Education, Shandong University of Traditional Chinese Medicine, Jinan, 250355, China. Electronic address:
The thermosensitive transient receptor potential (Thermo-TRP) channel proteins comprise TRPA1, TRPV1-V4, and TRPM8. TRP channels are mainly situated on cellular surfaces and react to a range of external factors, including heat, cold, acidity, osmotic pressure, chemical signals, and flavors, as well as intracellular signals such as Ca, Na, and cytokines. The thermo-TRP channels are associated with many physiological signal pathways, with their distinct molecular structure making them promising drug targets for respiratory diseases.
View Article and Find Full Text PDFACS Omega
September 2025
Neuroscience and Ageing Biology Division, CSIR- Central Drug Research Institute (CDRI), Lucknow 226031, India.
The TRPA1 channel has recently emerged as a critical target for pain relief since its antagonists target the beginning of the pain transduction pathway and, thus, are devoid of side effects such as sedation, dizziness, somnolence, or cognitive impairment. Despite this clinical significance, currently, no TRPA1 inhibitors suitable for therapeutic usage exist to target these channels. Since ancient times, natural products have been known to be a rich source of new drugs, useful therapeutic agents, as well as pharmacological tools.
View Article and Find Full Text PDFLung
September 2025
The Wellcome-Wolfson Institute for Experimental Medicine, School of Medicine, Dentistry and Biomedical Sciences, Queen's University Belfast, 97 Lisburn Road, Belfast, Belfast BT9 7BL, UK.
Introduction: Rhinovirus (RV) is the leading cause of exacerbations of lung disease. A sensory neuronal model, derived from human dental pulp stem cells and differentiated into peripheral neuronal equivalents (PNEs), was used to examine RV's effects on airway sensory nerves. We investigated whether RV can directly infect and alter PNEs or whether it exerts effects indirectly via the release of mediators from infected epithelial cells.
View Article and Find Full Text PDFJ Headache Pain
September 2025
Faculty of Medicine, Collegium Medicum, The Mazovian University in Plock, Plock, 09-402, Poland.
Background: Epigenetic studies in migraine provided results on the occurrence or lack of epigenetic modifications of genes whose products are important in migraine pathogenesis. However, these studies focus on single genes without analyzing how epigenetic modifications can affect complex signaling pathways. This narrative/hypothesis review aims to provide information on how the reactive oxygen and nitrogen species (RONS)-transient receptor potential cation channel subfamily A member 1 (TRPA1)-calcitonin gene-related peptide (CGRP) axis functions, suggesting that its epigenetic modifications could be a significant factor in migraine pathophysiology.
View Article and Find Full Text PDFJ Biol Chem
August 2025
Department of Pain Medicine, The State Key Specialty in Pain Medicine, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, 510260, P.R. China; Stem Cell Translational Medicine Center, The Second Affiliated Hospital, Guangzhou Medical University, Guangzhou, P. R. of China. Electr
Demyelination of peripheral nerve injury is a vital cause of neuropathic pain. Schwann cells play an important role in supporting and maintaining the removal and regeneration of myelin debris from neuronal axons in the peripheral nervous system. Creating a good immune microenvironment would promote the Schwann cells to repair the injured nerve and reverse the allodynia of neuropathic pain.
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