Guangxitoxin-1E. A Potent Gating Modifier of K\v\2.1, K\v\2.2 and K\v\4.3 K+ Channels.
Guangxitoxin-1E is a 36 amino acid peptidyl toxin isolated from the Chilobrachys jingzhao (Chinese earth tiger) tarantula venom and belongs to the huwentoxin-1 family.
Guangxitoxin-1E is a gating modifier of K\v\2.1 (KCNB1, IC50 of 1 nM), K\v\2.2 (KCNB2, IC50 of 3 nM) and K\v\4.3 (KCND3, IC50 of 50 nM) channels. In pancreatic betacells, it enhances glucose-stimulated insulin secretion by broadening the cell action potential and enhancing calcium oscillations.
The physiological modulation of K\v\2.1 channels during glucose-induced insulin secretion is MgATP-mediated. No significant effect was found on K\v\1.2 (KCNA2), K\v\1.3 (KCNA3), K\v\1.5 (KCNA5), K\v\3.2 (KCNC2), Cav1.2 (CACNA1C), Cav2.2 (CACNA1B), Nav1.5 (SCN5A), Nav1.7 (SCN9A) or Nav1.8 (SCN10A) channels.
Ion Channel Modulators; K+ Channel Blockers