PKC inhibition results in a Kv 1.5 + Kv β1.3 pharmacology closer to Kv 1.5 channels.

ABSTRACT:

Background and purpose

The Kv β1.3 subunit modifies the gating and pharmacology of Kv 1.5 channels in a PKC-dependent manner, decreasing channel sensitivity to bupivacaine- and quinidine-mediated blockade. Cardiac Kv 1.5 channels associate with receptor for activated C kinase 1 (RACK1), the Kv β1.3 subunit and different PKC isoforms, resulting in the formation of a functional channelosome. The aim of the present study was to investigate the effects of PKC inhibition on bupivacaine and quinidine block of Kv 1.5 + Kv β1.3 channels.

Experimental approach

HEK293 cells were transfected with Kv 1.5 + Kv β1.3 channels, and currents were recorded using the whole-cell configuration of the patch-clamp technique. PKC inhibition was achieved by incubating the cells with either calphosti

SUBMITTER: Macias A 

PROVIDER: S-EPMC4294114 | biostudies-literature | 2014 Nov

REPOSITORIES: biostudies-literature