Jingzhaotoxin-III selectively inhibits the activation of the voltage-dependent Nav1.5 channels (IC50 = 350 nM) in heart or cancer cells, but displays no effect on other isoforms,like NaV1.2, NaV1.4, NaV1.6 and NaV1.7. It also inhibits Kv2.1 channel (IC50 = 700 nM).
CAT No: R0983
CAS No:925463-91-8
Synonyms/Alias:jingzhaotoxin-III;925463-91-8;Jingzhaotoxin III;AMB46391;AKOS024458414;DA-54534;PD079774;
Jingzhaotoxin-III (JZTX-III) is a peptide toxin isolated from the venom of the Chinese spider Chilobrachys jingzhao that inhibits Nav channels of rat cardiac myocytes by modifying voltage-dependent gating and also binds to Kv2.1 channel (Kd=0.43 μM) with an action model similar to that of hanatoxin1 and SGTx1. The solution structure of JZTX-III was determined by 1H 2D NMR method. The toxin adopts an ICK motif composed of three β-strands connected by four turns. Structural comparison of JZTX-III with those of other ICK motif peptides shows that they all adopt a conserved surface profile, a hydrophobic patch surrounded by charged residues, which might be the crucial site for voltage-gating ion channel inhibition. Furthermore, the similar action model of JZTX-III affecting both Kv and Nav channels implies that JZTX-III recognized a conserved receptor within the voltage sensing domains, which is similar to that of hanatoxin1 binding to both Kv and Cav channels.
Solution structure of Jingzhaotoxin-III, a peptide toxin inhibiting both Nav1.5 and Kv2.1 channels
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