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Selective blockade of Cav1.2 (α1C) versus Cav1.3 (α1D) L-type calcium channels by the black mamba toxin calciseptine
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 v 1.2 and Ca v 1.3 that are concomitan...
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Published in: | Nature communications 2024-01, Vol.15 (1), p.54-54, Article 54 |
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Main Authors: | , , , , , , , , , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
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Summary: | 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
v
1.2 and Ca
v
1.3 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
v
1.2 -mediated L-type calcium currents (I
CaL
) at concentrations leaving Ca
v
1.3-mediated I
CaL
unaffected in both native cardiac myocytes and HEK-293T cells expressing recombinant Ca
v
1.2 and Ca
v
1.3 channels. Functionally, calciseptine potently inhibits cardiac contraction without altering the pacemaker activity in sino-atrial node cells, underscoring differential roles of Ca
v
1.2− and Ca
v
1.3 in cardiac contractility and automaticity. In summary, calciseptine is a selective L-type Ca
v
1.2 Ca
2+
channel blocker and should be a valuable tool to dissect the role of these L-channel isoforms.
L-type voltage-gated calcium channels are involved in multiple physiological functions. Here the authors identify calciseptine, a toxin purified from black mamba venom, as a selective inhibitor of Ca
v
1.2 L-type Ca
2+
channels. |
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ISSN: | 2041-1723 2041-1723 |
DOI: | 10.1038/s41467-023-43502-w |