Peptide GsMTx4, a stress-sensitive ion channel selective blocker

The peptide GsMTx4 (GsMTx-4, M-theraphotoxin-Gr1a) is a peptide isolated from the venom of the spider Grammostola rosea. This cationic hydrophobic peptide selectively blocks the gating of cation channels and mechanosensitive ion channels (e.g. TRPC1 or TRPC6) without any effect on whole-cell voltage-sensitive currents. The toxin acts by perturbing the interface between the channel and the lipid bilayer without having to physically contact the channel.

Product Information

Product Code: 602602

Product Purity: 98

Molecular Formula: C185H279N49O45S6

Molecular weight: 4095.8

Sequence:Gly-Cys-Leu-Glu-Phe-Trp-Trp-Lys-Cys-Asn-Pro-Asn-

Asp-Asp-Lys-Cys-Cys-Arg-Pro-Lys-Leu-Lys-Cys-Ser-Lys-Leu-Phe-Lys-Leu-Cys-Asn-Phe-Ser-Phe-NH2(disulfide bridge: Cys2&Cys17,Cys9&Cys23, Cys16&Cys30 bridge)

Duchenne muscular dystrophy is a life-limiting muscle disease, a sex-linked recessive disorder also known as pseudohypertrophic muscular dystrophy, the most symptomatic form of muscular dystrophy for which there is no effective treatment. Despite mounting evidence that dysregulation of mechanosensitive ion channels is important in the pathogenesis of dystrophies, effective pharmacological drug strategies targeting these channels are still lacking.GsMTx4 and its corresponding isomer, GsMTx4-D, are both peptide inhibitors of mechanosensitive channels with the same activity. The use of GsMTx4 in dystrophic mouse muscle was effective in reducing the reduction of muscle mass and muscle contraction-induced damage.GsMTx4 represents a promising new therapy that could somewhat slow down such disorders and could be used as complementary therapies, such as anti-inflammatory drugs and gene replacement strategies.