• SyncroPatch 384/768i

    APC with highest throughput on the market
  • SyncroPatch 384/768i

    384 cells in parallel => upgradable to 768
  • SyncroPatch 384/768i

    True HTS AND Gigaohm seals
  • SyncroPatch 384/768i

    Analysis Software even more powerful than before
  • SyncroPatch 384/768i

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2020 - Mechanism of hERG inhibition by gating-modifier toxin, APETx1, deduced by functional characterization

 icon sp96   SyncroPatch 384PE (a predecessor model of the SyncroPatch 384i instrument) pre-publication in bioRxiv (2020)

Matsumura K., Shimomura T., Kubo Y., Oka T., Kobayashi N., Imai S., Yanase N., Akimoto M., Fukuda M., Yokogawa M., Ikeda K., Kurita J., Nishimura Y., Shimada I., Osawa M.


bioRxiv (2020) doi: 10.1101/2020.07.22.215491


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. Although it is known that APETx1 inhibits hERG by stabilizing the resting state, it remains unclear where and how APETx1 interacts with the VSD in the resting state. Here, we prepared a recombinant APETx1, which is structurally and functionally equivalent to the natural product. Electrophysiological analyses using wild type and mutants of APETx1 and hERG revealed that their hydrophobic residues, in addition to a previously reported acidic hERG residue, play key roles in the inhibition of hERG by APETx1. Docking models of the APETx1-VSD complex that satisfy the results of mutational analysis suggest a molecular recognition mode between APETx1 and the resting state of hERG; this would provide a structural basis for designing ligands that control hERG function by binding to the VSD.

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