Article
Mechanism of hERG inhibition by gating-modifier toxin, APETx1, deduced by functional characterization.
BMC molecular and cell biology - 7 Jan 2021
Matsumura Kazuki, Shimomura Takushi, Kubo Yoshihiro, Oka Takayuki, Kobayashi Naohiro, Imai Shunsuke, Yanase Naomi, Akimoto Madoka, Fukuda Masahiro, Yokogawa Mariko, Ikeda Kazuyoshi, Kurita Jun-Ichi, Nishimura Yoshifumi, Shimada Ichio, Osawa Masanori
Abstract excerpt
BACKGROUND: Human ether-à-go-go-related gene potassium channel 1 (hERG) is a voltage-gated potassium channel, the voltage-sensing domain (VSD) of which is targeted by a gating-modifier toxin, APETx1. APETx1 is a 42-residue peptide toxin of sea anemone Anthopleura elegantissima and inhibits hERG by stabilizing the resting state. A previous study that conducted cysteine-scanning analysis of hERG identified two...
Topics
- Amino Acid Sequence
- Animals
- Cnidarian Venoms
- DNA Mutational Analysis
- ERG1 Potassium Channel
- HEK293 Cells
- Humans
- Hydrogen-Ion Concentration
- Hydrophobic and Hydrophilic Interactions