Guangxitoxin 1E



Chemische Beschreibung:

Sequence: [Cys4-Cys19, Cys11-Cys24, Cys18-Cys31]; H-Glu-Gly-Glu-Cys4-Gly-Gly-Phe-Trp-Trp-Lys-Cys11-Gly-Ser-Gly-Lys-Pro-Ala-Cys18-Cys19-Pro-Lys-Tyr-Val-Cys24-Ser-Pro-Lys-Trp-Gly-Leu-Cys31-Asn-Phe-Pro-Met-Pro-OH


3948,60 g/mol

GxTx-1E was isolated from the venom of Chilobrachys jingzhao (Chinese earth tiger tarantula). It was shown to block Kv2.1/KCNB1, Kv2.2/KCNB2 and Kv4.3/KCND3 channels without significant effect on Kv1.2/KCNA2, Kv1.3/KCNA3, Kv1.5/KCNA5, Kv3.2/KCNC2, Cav1.2/CACNA1C, Cav2.2/CACNA1B, Nav1.5/SCN5A, Nav1.7/SCN9A or Nav1.8/SCN10A channels. GxTx-1E inhibits Kv2.1 with an IC50 value of 1 nM and Kv2.2 with an IC50 value of 3 nM. Block of Kv4.3 occurs at 10-20 fold higher concentrations. It acts as a gating modifier since it shifts the voltage-dependence of Kv2.1 K+ currents towards depolarized potentials. In pancreatic b cells, it enhances glucose-stimulated insulin secretion by broadening the cell action potential and enhancing calcium oscillations.

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Guangxitoxin 1E

Synthetische Toxine

Toxine kommen bekanntlich in einer ganzen Reihe von Tierarten vor. Stellvertretend für die Vielzahl an Toxinen sei Apamin, das Bienengift oder Conotoxin, ein Meeresschneckengift erwähnt. Einige der Meeresschnecken-Gifte (cone snail) enthalten ...

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