Structural Properties, Pathophysiological Relevance and Synthetic Modulators of TRPC Channels

ABSTRACT Transient receptor potential canonical (TRPC) channels, a subfamily of calcium‐permeable cation channels, regulate diverse physiological processes and are implicated in disorders including neurological conditions, cardiovascular diseases, and chronic kidney disease. Recent advances in cryo‐electron microscopy (cryo‐EM) have elucidated TRPC structures, while subtype‐selective modulators have clarified their pathophysiological roles and therapeutic potential. This review integrates the structural and functional attributes of TRPC channels, emphasizing their contributions to health and disease. We highlight synthetic strategies and structure–activity relationships driving the development of selective pharmacological tools, several of which show preclinical promise. By uniting TRPC biology with medicinal chemistry, this study provides strategic guidance for advancing clinically viable TRPC‐targeted therapeutics.