May 27, 2020

Native expression of ASIC1a and ASIC1b human homologues in the HEK 293 cell line allows pharmacological evaluation of analgesics targeting acid sensation in humans

Ya Lan Yang, Ted Weita Lai


Nociceptors arising from the dorsal root ganglia (DRG) express acid-sensing ion channel-1 (ASIC1) subtypes to mediate the perception of inflammatory and neuropathic pain, and as such, these receptors are attractive targets for the development of analgesics for these painful conditions. Nevertheless, given that the human and rodent DRG differ considerably in subtype proportions of ASIC1 and that the pharmacological properties of rodent ASIC1 subtypes and their human homologues are distinct, ASIC1 inhibitors that demonstrate analgesic properties in rodents may not necessarily be effective in preventing pain in humans. In this study, we show that human embryonic kidney (HEK) 293 cells, which are routinely used as a cellular vehicle for the heterologous expression and pharmacological characterization of receptors and ion channels, natively transcribe the human homologues of ASIC1a and ASIC1b at similar proportions to those found in the human DRG. Importantly, HEK 293 ASIC1 is sensitive to inhibition by amiloride, ethylisopropyl amiloride, and the snake toxin mambalgin-1, but insensitive to inhibition by the ASIC1a inhibitor psalmotoxin-1 when applied at a physiological conditioning pH. Given that the human DRG transcribes the same ...Continue Reading

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Mentioned in this Paper

Mambalgin-1, Dendroaspis polylepis
Enzyme Inhibitor Drugs
Subtype (Attribute)
Neurl4 protein, human
Snake Venoms
Acid Sensing Ion Channel Blockers
Protein Expression

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