Key result
Azaspiracids dose-dependently block the hERG potassium channel by occluding the cytoplasmic mouth of the open pore.
Why the study?
Azaspiracids are marine toxins with unknown molecular targets that pose emerging human health risks including cytotoxicity and possible carcinogenicity.
Population
hERG potassium channels expressed in HEK-293 cells and Xenopus oocytes
Comparison
Azaspiracid analogues AZA1, AZA2, and AZA3 vs control
Design
Preclinical experimental study using voltage clamp, binding, and flux assays
Authors
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May signal azaspiracid cardiotoxicity risk in exposed patients; leaves open clinical translation from in vitro hERG data.
Effect estimate: IC50 0.64-0.84 μM
Azaspiracids (AZA1, AZA2, AZA3) are open-state blockers of the hERG potassium channel, suggesting a potential mechanism for their toxicity.
Twiner et al. (2012) studied this question. Azaspiracids (AZA1, AZA2, AZA3) was evaluated on Inhibition of K(+) current (IC50 0.64-0.84 μM). Azaspiracids (AZA1, AZA2, and AZA3) block the hERG potassium channel in a concentration-dependent manner (IC50 0.64-0.84 μM) by occluding the cytoplasmic mouth of the open pore.
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