The mammalian transient receptor potential (TRP) superfamily of ion channels consists of voltage-independent, non-selective cation channels that are expressed in excitable and non-excitable cells. The biologic roles of TRP channels are diverse and include vascular tone, thermosensation, irritant stimuli sensing and flow sensing in the kidney. TRP channels are a relatively new target in therapeutic drug discovery. During the past few years, pharmaceutical companies have focused their discovery efforts on developing TRP channel modulators with potential therapeutic value. This review focuses on the potential therapeutic benefits of drugs targeting TRP ion channels.
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http://dx.doi.org/10.1517/14728222.11.3.391 | DOI Listing |
Lipids Health Dis
January 2025
Department of Cardiology, West China Hospital, Sichuan University West China School of Medicine, 37 Guoxue Road, Chengdu, Sichuan, 610041, China.
Background: Atrial fibrillation (AF) is the most prevalent arrhythmia encountered in clinical practice. Triglyceride glucose index (Tyg), a convenient evaluation variable for insulin resistance, has shown associations with adverse cardiovascular outcomes. However, studies on the Tyg index's predictive value for adverse prognosis in patients with AF without diabetes are lacking.
View Article and Find Full Text PDFPharmaceutics
January 2025
Department of Pharmaceutical Bioscience, Translational Drug Discovery and Development, Uppsala University, SE-75124 Uppsala, Sweden.
: N-acetyl-galactosamine small interfering RNAs (GalNAc-siRNA) are an emerging class of drugs due to their durable knockdown of disease-related proteins. Direct conjugation of GalNAc onto the siRNA enables targeted uptake into hepatocytes via GalNAc recognition of the Asialoglycoprotein Receptor (ASGPR). With a transient plasma exposure combined with a prolonged liver half-life, GalNAc-siRNA exhibits distinct disposition characteristics.
View Article and Find Full Text PDFNutrients
January 2025
Instituto de Bioeletricidade Celular (IBIOCEL): Ciência & Saúde, Departamento de Bioquímica, Centro de Ciências Biológicas, Universidade Federal de Santa Catarina, Rua João Pio Duarte Silva, 241, Sala G 301, Florianópolis 88038-000, SC, Brazil.
Diabetes mellitus is a metabolic syndrome that has grown globally to become a significant public health challenge. Hypothesizing that the plasma membrane protein, transient receptor potential ankyrin-1, is a pivotal target in insulin resistance, we investigated the mechanism of action of cinnamaldehyde (CIN), an electrophilic TRPA1 agonist, in skeletal muscle, a primary insulin target. Specifically, we evaluated the effect of CIN on insulin resistance, hepatic glycogen accumulation and muscle and adipose tissue glucose uptake.
View Article and Find Full Text PDFInsects
January 2025
College of Plant Protection, Nanjing Agricultural University, Nanjing 210095, China.
Inwardly rectifying potassium (Kir) channels regulate essential physiological processes in insects and have been identified as potential targets for developing new insecticides. Flonicamid has been reported to inhibit Kir channels, disrupting the functions of salivary glands and renal tubules. However, the precise molecular target of flonicamid remains debated.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Shanghai Engineering Research Center of Tooth Restoration and Regeneration & Tongji Research Institute of Stomatology & Department of Oral Mucosal Diseases, Shanghai Tongji Stomatological Hospital and Dental School, Tongji University, Shanghai 200072, China.
The distinctive clinicopathologic characteristics of OLP indicated that both microbial dysbiosis and neurogenic inflammation may be jointly involved in its progression, and transient receptor potential vanilloid receptor-1 (TRPV1) may be a crucial element. The purpose of this study was to explore how TRPV1 mediated -induced inflammation. Meanwhile, we aimed to unravel how IL-36γ dysregulated the barrier function in oral keratinocytes.
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