Artificial pore blocker acts specifically on voltage-gated potassium channel isoform K_V1.6.

ABSTRACT: Among voltage-gated potassium channel (K_V) isoforms, K_V1.6 is one of the most widespread in the nervous system. However, there are little data concerning its physiological significance, in part due to the scarcity of specific ligands. The known high-affinity ligands of K_V1.6 lack selectivity, and conversely, its selective ligands show low affinity. Here, we present a designer peptide with both high affinity and selectivity to K_V1.6. Previously, we have demonstrated that K_V isoform-selective peptides can be constructed based on the simplistic α-hairpinin scaffold, and we obtained a number of artificial Tk-hefu peptides showing selective blockage of K_V1.3 in the submicromolar range. We have now proposed amino acid substitution

SUBMITTER: Gigolaev AM 

PROVIDER: S-EPMC9637586 | biostudies-literature | 2022 Nov

REPOSITORIES: biostudies-literature