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Membrane Proteins

Ion Channels

  • RyR1

    2.8 Å
    37793
    P11716
  • GABAAR-β3

    2.9 Å
    P28472
  • hERG

    2.6 Å
    37741
    Q12809

Ion channels are a class of proteins responsible for the transport of ions across cell membranes. By regulating the opening state of ion channels on the cell membrane, they maintain the balance of ion concentrations inside and outside the cell during physiological processes, thereby influencing the cell's electrical potential and ion channel permeability 【1】 .Ion channels are composed of membrane proteins that are located on the cell membrane, forming a pore that allows the passage of specific types of ions.

The structure of ion channels typically consists of protein subunits spanning the cell membrane, forming a cavity known as the channel pore. The size and shape of this pore selectively permit the passage of specific ion types, enabling the regulation of ion permeability. Furthermore, the structure of ion channels is composed of multiple segments that confer structure and function, including a signal recognition domain, an ion selectivity filter, and an ion channel gating structure 【2】 .

Dysregulation of ion channels is associated with a large number of diseases (also known as channelopathies), including cancer, dementia, diabetes, asthma, and more 【3】 .Therefore, ion channels present a significant challenge in drug design, primarily because designing selective inhibitors for them is difficult, and a lack of drug specificity can produce detrimental effects on other crucial, structurally similar ion channels.

References

【1】Petkov G V. Ion channels[M]//Pharmacology. Academic Press, 2009: 387-427.
【2】Catterall W A. Ion channel voltage sensors: structure, function, and pathophysiology[J]. Neuron, 2010, 67(6): 915-928.
【3】Zaydman M A, Silva J R, Cui J. Ion channel associated diseases: overview of molecular mechanisms[J]. Chemical reviews, 2012, 112(12): 6319-6333