Selective blockade of Ca_v1.2 (α1C) versus Ca_v1.3 (α1D) L-type calcium channels by the black mamba toxin calciseptine.

ABSTRACT: L-type voltage-gated calcium channels are involved in multiple physiological functions. Currently available antagonists do not discriminate between L-type channel isoforms. Importantly, no selective blocker is available to dissect the role of L-type isoforms Ca_v1.2 and Ca_v1.3 that are concomitantly co-expressed in the heart, neuroendocrine and neuronal cells. Here we show that calciseptine, a snake toxin purified from mamba venom, selectively blocks Ca_v1.2 -mediated L-type calcium currents (I_CaL) at concentrations leaving Ca_v1.3-mediated I_CaL unaffected in both native cardiac myocytes and HEK-293T cells expressing recombinant Ca_v1.2 and Ca_v1.3 channels. Functionally, calciseptine potently inhibits cardi

SUBMITTER: Mesirca P 

PROVIDER: S-EPMC10762068 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature