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| http://dx.doi.org/10.1165/rcmb.2019-0292ED | DOI Listing |
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Structure- and Ligand-Based Virtual Screening for Identification of Novel TRPV4 Antagonists.
Molecules
December 2024
Structural Bioinformatics Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Tykistökatu 6, 20520 Turku, Finland.
Transient receptor potential vanilloid (TRPV) 4 is involved in signaling pathways specifically mediating pain and inflammation, making it a promising target for the treatment of various painful and inflammatory conditions. However, only one drug candidate targeting TRPV4 has entered the clinical trials. To identify potential TRPV4 inhibitors for drug development, we screened a library of ion channel-modulating compounds using both structure- and ligand-based virtual screening approaches.
View Article and Find Full Text PDFTracheal tuft cells release ATP and link innate to adaptive immunity in pneumonia.
Nat Commun
January 2025
Institute of Anatomy and Cell Biology, Saarland University, Homburg, Germany.
Tracheal tuft cells shape immune responses in the airways. While some of these effects have been attributed to differential release of either acetylcholine, leukotriene C4 and/or interleukin-25 depending on the activating stimuli, tuft cell-dependent mechanisms underlying the recruitment and activation of immune cells are incompletely understood. Here we show that Pseudomonas aeruginosa infection activates mouse tuft cells, which release ATP via pannexin 1 channels.
View Article and Find Full Text PDFProtein dynamics underlies strong temperature dependence of heat receptors.
Proc Natl Acad Sci U S A
January 2025
Department of Physiology and Biophysical Sciences, State University of New York at Buffalo, Buffalo, NY 14214.
Ion channels are generally allosteric proteins, involving specialized stimulus sensor domains conformationally linked to the gate to drive channel opening. Temperature receptors are a group of ion channels from the transient receptor potential family. They exhibit an unprecedentedly strong temperature dependence and are responsible for temperature sensing in mammals.
View Article and Find Full Text PDFNeuronal TRPV1-CGRP axis regulates peripheral nerve regeneration through ERK/HIF-1 signaling pathway.
J Neurochem
January 2025
State Key Laboratory of Oral Diseases & National Center for Stomatology & National Clinical Research Center for Oral Diseases, West China Hospital of Stomatology, Sichuan University, Chengdu, China.
Severe trauma frequently leads to nerve damage. Peripheral nerves possess a degree of regenerative ability, and actively promoting their recovery can help restore the sensory and functional capacities of tissues. The neuropeptide calcitonin gene-related peptide (CGRP) is believed to regulate the repair of injured peripheral nerves, with neuronal transient receptor potential vanilloid type 1 (TRPV1) potentially serving as a crucial upstream factor.
View Article and Find Full Text PDFImmunohistochemical investigation of transient receptor potential melastatin-2 and spexin immunoreactivity in atopic dermatitis and mycosis fungoides.
Arch Dermatol Res
January 2025
Department of Dermatology, Firat University Hospital, Elazig, TR23119, Turkey.
Background: Atopic dermatitis (AD) is a chronic, pruritic, and inflammatory dermatosis seen in individuals with an atopic predisposition. This study aimed to examine the immunoreactivity of spexin and TRPM2 in skin samples from patients with AD and MF lesions using immunohistochemical methods.
Materials And Methods: The study utilized a total of 60 skin samples, comprising 20 from AD patients, 20 from MF patients, and 20 from control subjects.
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