Ion channels are macromolecular protein embedded within reflexed channel pores in the membrane lipid bilayer, which selectively allow ions to flow in response to a range of physical and chemical signals. They play crucial roles in a series of physiological function such as cellular excitability, neuronal transmission, hormone secretion, sensory transduction and blood pressure regulation. Precise control of the ion channel activity is essential for maintaining the basic function of cells. Hyper- and hypo-activation of ion channels have been proved to cause a wide range of disorders termed channelopathies, which include cystic fibrosis, Dent’s disease, long QT syndrome, short QT syndrome, myasthenia gravis, periodic paralysis (hyperkalemic, hypokalemic and normokalemic), epilepsy, and autoimmune encephalitis.
Ion channels are considered to be important drug targets for the treatment of channelopathies. In fact, they are well-recognized as the second largest drug target class after G protein-coupled receptors. Meanwhile, the molecular mechanism of channel function and drug action is not yet fully understood due to the lack of high-resolution structures. Thanks to the recent technological advances, cryo-EM keeps on breaking the atomic resolution barrier and becomes widely used in the field of structure biology. As a matter of fact, a burst of high-resolution structures of ion channel assemblies have been elucidated by cryo-EM in recent years. These advancements are revolutionizing the study of ion channel function, as well as the discovery of novel drug targeting to the ion channels. This Research Topic focuses on the atomic-resolution structures of ion channels resolved by cryo-EM recently, discusses how these structural advancements speed up the basic understanding of ion channel function and the development of ion channel-based drugs.
The following subtopics will be included in the Research Topic, but are not limited to
1. Structural elucidation of ion channel gating mechanism and function.
2. Molecular insights about how these inherited ion channel mutations cause channelopathies.
3. Drug binding site and action mechanism in various subtypes of ion channels.
4. Integrate high-resolution structures and artificial intelligent based drug design to speed up the future therapeutic development.
Ion channels are macromolecular protein embedded within reflexed channel pores in the membrane lipid bilayer, which selectively allow ions to flow in response to a range of physical and chemical signals. They play crucial roles in a series of physiological function such as cellular excitability, neuronal transmission, hormone secretion, sensory transduction and blood pressure regulation. Precise control of the ion channel activity is essential for maintaining the basic function of cells. Hyper- and hypo-activation of ion channels have been proved to cause a wide range of disorders termed channelopathies, which include cystic fibrosis, Dent’s disease, long QT syndrome, short QT syndrome, myasthenia gravis, periodic paralysis (hyperkalemic, hypokalemic and normokalemic), epilepsy, and autoimmune encephalitis.
Ion channels are considered to be important drug targets for the treatment of channelopathies. In fact, they are well-recognized as the second largest drug target class after G protein-coupled receptors. Meanwhile, the molecular mechanism of channel function and drug action is not yet fully understood due to the lack of high-resolution structures. Thanks to the recent technological advances, cryo-EM keeps on breaking the atomic resolution barrier and becomes widely used in the field of structure biology. As a matter of fact, a burst of high-resolution structures of ion channel assemblies have been elucidated by cryo-EM in recent years. These advancements are revolutionizing the study of ion channel function, as well as the discovery of novel drug targeting to the ion channels. This Research Topic focuses on the atomic-resolution structures of ion channels resolved by cryo-EM recently, discusses how these structural advancements speed up the basic understanding of ion channel function and the development of ion channel-based drugs.
The following subtopics will be included in the Research Topic, but are not limited to
1. Structural elucidation of ion channel gating mechanism and function.
2. Molecular insights about how these inherited ion channel mutations cause channelopathies.
3. Drug binding site and action mechanism in various subtypes of ion channels.
4. Integrate high-resolution structures and artificial intelligent based drug design to speed up the future therapeutic development.