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Comment
. 2020 Aug 3;152(8):e202012598.
doi: 10.1085/jgp.202012598.

Chemical regulation of Kv7 channels: Diverse scaffolds, sites, and mechanisms of action

Harley T Kurata  1
Affiliations
Comment

Chemical regulation of Kv7 channels: Diverse scaffolds, sites, and mechanisms of action

Harley T Kurata. J Gen Physiol. .

Abstract

Kv7 channels are powerfully regulated by a wide variety of physiological and pharmacological signals. Larsson et al. describe the direct modulation of Kv7 channels by endocannabinoids and explore how combinations of Kv7 activators with distinct subtype specificities might lead to effective and selective drug cocktails.

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Figures

Figure 1.
Figure 1.
Distinct sites of action for Kv7 channel activators. Likely regions of binding and the location of implicated amino acid residues are highlighted on a homology model of Kv7.2 based on PDB accession no. 5VMS. The critical tryptophan in the retigabine binding site is highlighted in yellow (Schenzer et al., 2005). Voltage sensor residues that influence effects of ICA-069673 are highlighted in cyan (Peretz et al., 2010; Li et al., 2013). Voltage sensor residues that influence ARA-S effects are highlighted in red (Larsson et al., 2020).
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