Key result
Tertiapin, a newly identified protein inhibitor, blocks G-protein-gated (GIRK1/4) and ROMK1 inward-rectifier K+ channels with nanomolar affinities by binding to the external end of the pore.
Population
Inward-rectifier K+ channels (GIRK1/4, ROMK1, IRK1)
Design
Preclinical
Authors
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Tertiapin may enable targeted channel studies in vitro; leaves open therapeutic translation in humans.
Tertiapin is identified as a high-affinity inhibitor of specific inward-rectifier K+ channels (GIRK1/4 and ROMK1), providing a novel tool for studying these channels.
Jin et al. (1998) studied this question. tertiapin was evaluated on Inhibition of inward-rectifier K+ channels. Tertiapin, a newly identified protein inhibitor, blocks G-protein-gated (GIRK1/4) and ROMK1 inward-rectifier K+ channels with nanomolar affinities by binding to the external end of the pore.
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