Basic Information
ID: ALA4725288
Journal: Bioorg Med Chem
Title: Modulation of TRPV4 and BKCa for treatment of brain diseases.
Authors: Liu N,Yan F,Ma Q,Zhao J
Abstract: As a member of transient receptor potential family, the transient receptor potential vanilloid 4 (TRPV4) is a kind of nonselective calcium-permeable cation channel, which belongs to non-voltage gated Ca channel. Large-conductance Ca-activated K channel (BKCa) represents a unique superfamily of Ca-activated K channel (KCa) that is both voltage and intracellular Ca dependent. Not surprisingly, aberrant function of either TRPV4 or BKCa in neurons has been associated with brain disorders, such as Alzheimer's disease, cerebral ischemia, brain tumor, epilepsy, as well as headache. In these diseases, vascular dysfunction is a common characteristic. Notably, endothelial and smooth muscle TRPV4 can mediate BKCa to regulate cerebral blood flow and pressure. Therefore, in this review, we not only discuss the diverse functions of TRPV4 and BKCa in neurons to integrate relative signaling pathways in the context of cerebral physiological and pathological situations respectively, but also reveal the relationship between TRPV4 and BKCa in regulation of cerebral vascular tone as an etiologic factor. Based on these analyses, this review demonstrates the effective mechanisms of compounds targeting these two channels, which may be potential therapeutic strategies for diseases in the brain.
CiteXplore: 32690264
DOI: 10.1016/j.bmc.2020.115609
Patent ID: ┄
Associated Items: Associated Bioactivities Associated Assays Associated Compounds Associated Targets