A small-molecule LF3 abrogates β-catenin/TCF4-mediated suppression of NaV1.5 expression in HL-1 cardiomyocytes

Increased nuclear β-catenin interacting with T-cell factor 4 (TCF4) affects the expression of target genes including SCN5A in ischemic heart disease, which is characterized by frequent ventricular tachycardia/fibrillation. A complex of β-catenin and TCF4 inhibits cardiac Na+ channel activity by reducing NaV1.5 expr ession through suppressing SCN5A promoter activity in HL-1 cardiomyocytes. LF3, a 4-thioureido-benzenesulfonamide derivative and an inhibitor of β-catenin/TCF4 interaction, has been shown to block the self-renewal capacity of cancer stem cells.
Source: Journal of Molecular and Cellular Cardiology - Category: Cytology Authors: Source Type: research