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Acid-sensing Ion Channel Assays

Background of Acid-sensing Ion Channel

Acid-sensing ion channels (ASICs) are voltage-insensitive proton-gated ion channels that belong to the ENaC (Epithelial Na+ Channel)/DEG (Degenerin)/ASIC (Acid-sensing ion channel) superfamily of ion channels. Till now, there are six ASIC subtypes have been identified, including ASIC1a, ASIC1b, ASIC2a, ASIC2b, ASIC3, and ASIC4. Different combinations of ASIC subtypes exhibit different electrophysiological properties.

Expression and Functions of Acid-sensing Ion Channel

In humans, the expression of ASICs can be observed in various tissues and is associated with diverse pathologies. In general, most ASIC subtypes are present in the peripheral nervous system (PNS), whereas ASIC1a can be expressed at high levels in the central nervous system (CNS) and is associated with a variety of CNS diseases. ASIC can be activated by extracellular protons permeable to Na+ and triggers a large number of different effector proteins and signaling molecules, resulting in different cellular responses.

Fig.1 ASICs localize in a variety of somatosensory nerve terminals responsible for both chemo-sensing and mechano-sensing functions.Fig.1. ASICs localize in a variety of somatosensory nerve terminals responsible for both chemo-sensing and mechano-sensing functions. (Cheng, 2018)

Diseases Associated with Acid-sensing Ion Channel

Studies have shown that knockout of the ASIC1a gene results in enhanced seizure activity, so ASIC1a channels play a role in preventing seizures. Activation of ASIC1a channels can also lead to small increases in Ca2+ permeability and inward Ca2+ flux that contribute to the pathology of ischemic brain injury. What's more, ASICs can protect against retinal damage in bright light. In summary, ASICs have served as potential drug targets for the treatment of a wide variety of conditions associated with both the CNS and PNS.

Assay List of Acid-sensing Ion Channel

Creative Biolabs can provide a range of assays of acid-sensing ion channels. You can choose the assay in the list or contact us for more information:

Acid-sensing Ion Channel
Assay No. Assay Name Host Cell Assay Type Datasheet
S01YF-0722-KX278 Magic™ Human ASIC1 In Vitro Electrophysiology Assay, CHO-K1 CHO-K1 Electrophysiology Assay

Published Data

Paper Title Acid-sensing ion channels as potential therapeutic targets
Journal Trends in Pharmacological Sciences
Published 2021
Abstract With the ability to sense changes in pH, acid-sensitive ion channels (ASICs) have been identified as potential drug targets. In recent years, a series of modulators have been developed for the inhibition of ASICs. In this paper, we evaluate the therapeutic potential of ASICs in diseases such as ischemic stroke, various pain-related processes, anxiety, and cardiac pathology through animal models. In the future, we will provide new insights into the treatment of ASICs.
Result In this review, researchers discuss the expression, localization, and mechanism of ASICs to gain deeper insights into ASICs. Based on numerous studies mainly from animal models, ASICs have been identified as potential targets for multiple indications in a range of neurological and psychiatric diseases. A better understanding of the relevant molecular mechanisms and signaling pathways needed in future studies will help to elucidate the future role of ASICs.

Fig.2 ASICs are activated by extracellular protons (H+) and are primarily permeable to Na+ (Ca<sup>2+</sup> to a lesser degree).Fig.2. ASICs are activated by extracellular protons (H+) and are primarily permeable to Na+ (Ca2+ to a lesser degree). (Heusser & Pless, 2021)

References

  1. Cheng, Y.; et al. Acid-sensing ion channels: dual function proteins for chemo-sensing and mechano-sensing. Journal of biomedical science. 2018, 25(1): 1-14.
  2. Heusser, S.A.; Pless, S.A. Acid-sensing ion channels as potential therapeutic targets. Trends in Pharmacological Sciences. 2021, 42(12): 1035-1050.
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