Mechanism of hERG inhibition by gating-modifier toxin, APETx1, deduced by functional characterization.
Kazuki MatsumuraTakushi ShimomuraYoshihiro KuboTakayuki OkaNaohiro KobayashiShunsuke ImaiNaomi YanaseMadoka AkimotoMasahiro FukudaMariko YokogawaKazuyoshi IkedaJun-Ichi KuritaYoshifumi NishimuraIchio ShimadaMasanori OsawaPublished in: BMC molecular and cell biology (2021)
The present study identified the key residues of APETx1 and hERG that are involved in hERG inhibition by APETx1. These results would help advance understanding of the inhibitory mechanism of APETx1, which could provide a structural basis for designing novel ligands targeting the VSDs of KV channels.