Peptide Inhibitors of Kv1.5: An Option for the Treatment of Atrial Fibrillation.

ABSTRACT: The human voltage gated potassium channel Kv1.5 that conducts the I_Kur current is a key determinant of the atrial action potential. Its mutations have been linked to hereditary forms of atrial fibrillation (AF), and the channel is an attractive target for the management of AF. The development of I_Kur blockers to treat AF resulted in small molecule Kv1.5 inhibitors. The selectivity of the blocker for the target channel plays an important role in the potential therapeutic application of the drug candidate: the higher the selectivity, the lower the risk of side effects. In this respect, small molecule inhibitors of Kv1.5 are compromised due to their limited selectivity. A wide range of peptide toxins from venomous animals are targeting ion channels, including mammalian c

SUBMITTER: Borrego J 

PROVIDER: S-EPMC8704205 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature