Ligand-Mediated Conformational Plasticity of the Pore Domain of TRPV6 Ion Channel

TRPV6 is a Ca2+-selective ion channel that plays a vital role in calcium homeostasis in the human body, including the absorption of dietary calcium. Dysfunction of TRPV6 can contribute to the development of various diseases, including several types of cancer. Therefore, identifying and studying the molecules involved in the regulation of TRPV6 function is a crucial task in modern pharmacology, requiring a thorough understanding of its mechanisms of action and ligand-mediated regulation at a molecular level. The ion-conducting pore is a key functional domain of TRPV6, which is a conformationally plastic nanotube with a complex structural and hydrophobic organization that is capable of responding to various physical and chemical stimuli. This review provides an overview of recent experimental and computational studies of the TRPV6 pore properties in different conformational states, and its response to various endogenous and exogenous molecular modulators.