Molecular Mechanism of Ion Channel Activation and Modulation

Ion channels are membrane proteins that allow the passage of ions across cell membranes, and their activity is crucial for a wide range of physiological functions, including muscle contraction, neuronal signaling, and hormone secretion. The activation of ion channels is typically initiated by a stimulus that causes a conformational change in the channel protein. This change can result from various factors, such as changes in membrane potential, binding of ligands, or mechanical stress. The conformational change leads to the opening of a channel pore, allowing ions to pass through the membrane. The modulatory effects on ion channels can be positive or negative and are mediated by various agents, including neurotransmitters, hormones, and drugs. The binding of a modulator to an ion channel can cause a conformational change that alters the channel's function. For example, a positive modulator may increase the affinity of the channel for its substrate or stabilize the open state of the channel, while a negative modulator may decrease the affinity of the channel for its substrate or stabilize the closed state of the channel. The molecular basis of ion channel activation and modulation is complex and varies between different types of channels. However, studies using X-ray crystallography, cryo-electron microscopy, molecular dynamics simulations, and other biophysical techniques have provided important insights into the structural changes that underlie these processes. Such studies have helped to identify key structural elements and functional domains within ion channels that are critical for their function and regulation. The ion channel activation is a highly regulated process that plays a critical role in the control of ion flux across cell membranes and in the regulation of many physiological functions. Further understanding of the underlying mechanisms could have important implications for the development of new therapeutics targeting ion channels in various diseases.

This special issue invites colleagues interested in studying ion channel function regulated by ligands using experimental or computational approaches to contribute original research or review articles. The topics of interest include, but are not limited to, the following: determination of ion channel-ligand complex structures using crystallography and cryo-electron microscopy, molecular dynamics simulations to investigate ion channel activation by ligands, mutations that alter ion channel function, exploration of dynamic interactions between ion channels and ligands using computational and experimental studies, and structure-based drug discovery.

We welcome contributions that utilize innovative approaches to shed light on the mechanisms underlying the activation of ion channels by their corresponding ligands. Our ultimate goal is to advance the development of novel therapeutic interventions.

Topic editors declare no conflict of interest.