GsMTx-4
A Blocker of Voltage-Gated \v\1.7 Na\+\Channels.
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GsMTX-4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.
This toxin inhibits different channels and in addition has antimicrobial activity. It blocks cation-selective mechanosensitive ion channels (strech-activated channels, SACs), without having effect on whole-cell voltage-sensitive currents.
In addition, it inhibits atrial fibrillation as well as the membrane motor of outer hair cells at low doses. A medium toxicity on a large spectra of voltage-gated Na\+\channels, namely \v\1.1, \v\1.2, \v\1.3, \v\1.4, \v\1.5, \v\1.6 and \v\1.7 was reported.
GsMTx-4 also inhibits K\+\ channels K\v\11.1 and K\v\11.2, whereas it does not inhibit K\+\ channels K\V\1.1 (ICK\50\ > 85 μM), K\V\1.4 (ICK\50\ > 85 μM) and K\V\11.3 (ICK\50\ = 53 μM).
GsMTX-4 was also found to inhibit both TRPC1 and TRPC6 channels.
Antimicrobial activity is shown against several Gram-positive and Gram-negative bacteria as well.
Ion Channel Modulators; Voltage - Gated Na+ Channel Blockers, TRP Channel Modulators