Regulating calcium ion (Ca2+) channels to improve the cell cycle and metabolism is a promising technology, ensuring increased cell growth, differentiation, and/or productivity. In this regard, the composition and structure of Ca2+channels play a vital role in controlling the gating states. In this review,Saccharomyces cerevisiae, as a model eukaryotic organism and an essential industrial microorganism, was used to discuss the effect of its type, composition, structure, and gating mechanism on the activity of Ca2+channels. Furthermore, the advances in the application of Ca2+channels in pharmacology, tissue engineering, and biochemical engineering are summarized, with a special focus on exploring the receptor site of Ca2+channels for new drug design strategies and different therapeutic uses, targeting Ca2+channels to produce functional replacement tissues, creating favorable conditions for tissue regeneration, and regulating Ca2+channels to enhance biotransformation efficiency.