GsMTx4 is a spider venom peptide that selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology. GsMTx4 significantly attenuates bladder hyperactivity.
CAT No: HB00094
CAS No:1209500-46-8
Synonyms/Alias:GsMTx4;1209500-46-8;GsMTx-4;H-Gly-DL-Cys(1)-DL-Leu-DL-Glu-DL-Phe-DL-Trp-DL-Trp-DL-Lys-DL-Cys(2)-DL-Asn-DL-Pro-DL-Asn-DL-Asp-DL-Asp-DL-Lys-DL-Cys(3)-DL-Cys(1)-DL-Arg-DL-Pro-DL-Lys-DL-Leu-DL-Lys-DL-Cys(2)-DL-Ser-DL-Lys-DL-Leu-DL-Phe-DL-Lys-DL-Leu-DL-Cys(3)-DL-Asn-DL-Phe-DL-Ser-DL-Phe-NH2;CHEBI:194078;HB1161;AKOS024458413;C185H273N49O45S6;CID:90488987;
GsMTx4 is a peptide toxin originally isolated from the venom of the tarantula Grammostola spatulata, recognized for its unique ability to modulate mechanosensitive ion channels in biological membranes. As a cyclic peptide composed of 34 amino acids, it exhibits a highly stable structure and demonstrates remarkable selectivity for stretch-activated and mechanosensitive cation channels. GsMTx4 has become an indispensable tool in the study of mechanotransduction processes, offering researchers a precise means to probe the physiological and molecular roles of mechanically gated ion channels across diverse biological systems. Its distinct mechanism of action and well-characterized pharmacological profile make it a valuable resource for both fundamental research and advanced technical applications in electrophysiology and membrane biophysics.
Electrophysiological research: GsMTx4 is widely utilized in patch-clamp studies to dissect the biophysical properties of mechanosensitive ion channels, such as Piezo, TREK, and MscL families. By selectively inhibiting or modulating these channels, the peptide enables researchers to isolate mechanosensitive currents and quantify their contributions to cellular excitability and signal transduction. Its application facilitates the identification of channel subtypes, gating mechanisms, and voltage-dependence, thereby advancing the understanding of how cells perceive and respond to mechanical stimuli at the molecular level.
Mechanotransduction pathway analysis: The peptide serves as a potent tool for elucidating the downstream signaling cascades initiated by mechanical stress in various cell types, including neurons, cardiomyocytes, and endothelial cells. By specifically targeting mechanosensitive channels, it allows for the dissection of the roles these channels play in processes such as cell migration, volume regulation, and cytoskeletal remodeling. Experimental use of GsMTx4 in pathway analysis has contributed significantly to mapping the molecular interactions that underlie mechanotransduction and identifying novel regulatory proteins involved in these pathways.
Drug discovery and screening: Due to its specificity and well-characterized mode of action, GsMTx4 is employed in high-throughput screening assays to identify small molecule modulators of mechanosensitive channels. The peptide acts as a reference inhibitor or positive control in assays designed to evaluate the efficacy and selectivity of new compounds targeting these ion channels. Its use enhances assay reliability and supports the development of new research tools or pharmacological probes that target mechanosensitive pathways.
Membrane biophysics and structural studies: The unique structure and channel-modulating properties of GsMTx4 make it a valuable reagent for investigating the physical interactions between membrane lipids, proteins, and the cytoskeleton. Researchers use the peptide to probe the conformational dynamics of mechanosensitive channels and to assess how changes in membrane tension or lipid composition affect channel function. Insights gained from these studies inform models of membrane mechanics and contribute to the broader understanding of cellular mechanosensitivity.
Peptide engineering and functional analog development: GsMTx4's sequence and structural motifs serve as templates for the rational design of peptide analogs with altered selectivity, potency, or stability. By leveraging its well-characterized scaffold, researchers can generate novel peptides for probing mechanosensitive channel function or for developing new research tools with tailored properties. These efforts support advancements in peptide-based probe development and expand the repertoire of modulators available for mechanotransduction research.
Grammastola spatulata mechanotoxin #4 (GsMTx4) is a 35 amino acid peptide that inhibits the gating of cation selective MSCs with similar affinity in either the l or d enantiomic forms, emphasizing its lack of stereospecificity when interacting with MSCs. Cationic MSCs may belong to the Transient Receptor Potential (TRP) and/or Piezo families known to be expressed in cardiomyocytes and vascular tissue. In vitro measures of MSC activity in cardiac tissue, single cells and patch assays, show GsMTx4 activity in the range of 0.1–5 μM. GsMTx4 is a gating modifier that inhibits MSCs by clamping the membrane tension of the outer monolayer where its penetration depth, and thus its surface area contribution, is tension dependent.
GsMTx4-D is a cardioprotectant against myocardial infarction during ischemia and reperfusion
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