Acid-sensing Ion Channel Related Drug Discovery Products
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The Acid-Sensing Ion Channel (ASIC) family comprises a group of proton-gated ion channels that discernibly respond to extracellular pH fluctuations, thereby modulating an array of physiological processes. In view of their functional implications, ASICs have attracted considerable attention as prospective therapeutic targets in diverse pathological conditions.
Fig.1 "Closed-fist" model of ASICs.1,2
As a leader in the field of drug discovery, Creative Biolabs can offer high-quality acid-sensing ion channel assays and products to our customers:
Overview of Acid-sensing Ion Channel
Within the comprehensive DEG/ENaC superfamily resides a distinct subclass, ASICs, which comprise six unique subunits (ASIC1a, ASIC1b, ASIC2a, ASIC2b, ASIC3, and ASIC4). These subunits coalesce into homotrimeric or heterotrimeric channels that demonstrate a particular predilection for the nervous system. Permeable predominantly to sodium ions and, to a lesser degree, calcium ions, these channels exhibit a diverse and intricate tissue distribution pattern. Functioning as modulators of neuronal excitability and synaptic transmission in the presence of extracellular acidification, the functional heterogeneity of ASICs renders them indispensable for an array of physiological processes. These encompass a wide range of phenomena, including nociception, mechanosensation, and the complex interplay of learning and memory, further underscoring their crucial role in maintaining homeostasis and ensuring optimal functioning of the nervous system.
Acid-sensing Ion Channel Drug Discovery
The development of therapeutic strategies targeting Acid-Sensing Ion Channels (ASICs) has garnered considerable attention due to their involvement in a variety of physiological and pathological processes, including neuronal excitability, synaptic transmission, nociception, and inflammation. The pharmaceutical exploitation of ASICs aims to modulate their activity, either by inhibiting or potentiating their function, depending on the desired therapeutic outcome.
Researchers have identified a diverse array of compounds that interact with ASICs, ranging from small organic molecules to peptides and monoclonal antibodies. These compounds exhibit different mechanisms of action, such as direct interaction with the ion channel pore, allosteric modulation, or interference with subunit assembly. The development of subtype-selective modulators is of particular interest, as it may allow for precise targeting of specific ASICs implicated in a given pathological condition while minimizing potential off-target effects.
Drug delivery strategies for ASIC-targeting compounds are tailored to ensure adequate biodistribution and access to the relevant tissues or cells, including crossing the blood-brain barrier when targeting central nervous system ASICs. Various approaches, including nanoparticle-based formulations, liposomal carriers, and conjugation with targeting ligands, have been explored to improve the pharmacokinetics and bioavailability of ASIC modulators.
References
- Sivils, Andy, et al. "Acid-sensing ion channel 2: Function and modulation." Membranes 12.2 (2022): 113.
- Image retrieved from Figure 1 "“Closed-fist” model of ASICs." Sivils, et al. 2022, used under CC BY 4.0. The original image was modified by extracting and the title was changed to " Closed-fist” model of ASICs.".
