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, also known as Grammostola spatulata mechanotoxin 4, is a peptide toxin originally isolated from the venom of the Chilean rose tarantula. Characterized by its unique ability to modulate mechanosensitive ion channels, GsMTx4 has become an invaluable research tool in the field of ion channel physiology. Its structure allows for selective interaction with stretch-activated channels, making it a powerful agent for dissecting the role of these channels in various cellular processes. The peptide's stable conformation and high specificity have driven its adoption in a wide range of experimental settings, from fundamental biophysical studies to advanced cellular investigations. Researchers have leveraged its distinctive properties to unravel complex mechanisms underlying mechanotransduction, providing insights that are difficult to achieve with traditional small molecule inhibitors.
Mechanosensitive Ion Channel Research: One of the primary applications of GsMTx4 is in the study of mechanosensitive ion channels. By selectively inhibiting these channels, the peptide enables scientists to probe the physiological and biophysical roles of stretch-activated currents in excitable and non-excitable cells. Its reversible and targeted action helps delineate the contribution of mechanosensitive channels to cellular homeostasis, signal transduction, and response to mechanical stress. This has proven particularly valuable in uncovering the molecular underpinnings of mechanotransduction pathways and in identifying potential targets for further research into cellular mechanosensitivity.
Electrophysiological Characterization: GsMTx4 serves as an essential tool in electrophysiological studies, where it is used to isolate and characterize mechanosensitive currents. By applying the peptide to patch-clamp preparations or other electrophysiological setups, researchers can selectively block specific ion channel conductances, allowing for precise measurement of channel properties and gating mechanisms. Its utility extends to both in vitro and ex vivo systems, facilitating the identification of mechanosensitive channel subtypes and their distinct functional roles within complex tissues.
Cellular Mechanotransduction Pathways: In the context of cellular signaling, GsMTx4 has enabled significant advances in the understanding of how mechanical forces are transduced into biochemical signals. Its application in cultured cells or tissue slices allows for the dissection of signaling cascades initiated by mechanical stimuli, such as membrane stretch or shear stress. By modulating the activity of mechanosensitive channels, the peptide helps clarify the downstream effects on calcium signaling, cytoskeletal remodeling, and gene expression, providing a clearer picture of the interplay between mechanical and chemical signaling in cells.
Cardiac and Muscle Physiology Research: The study of cardiac and skeletal muscle physiology has greatly benefited from the use of GsMTx4. In experimental models, it is employed to assess the role of mechanosensitive channels in muscle contraction, stretch response, and arrhythmogenesis. Its ability to selectively inhibit stretch-activated currents allows for the exploration of how mechanical forces influence muscle function at both the cellular and tissue levels, offering insights into the biophysical basis of muscle adaptation and maladaptation under various physiological and experimental conditions.
Neurobiological Investigations: GsMTx4 has also found application in neurobiological research, where mechanosensitive channels are implicated in processes such as neuronal excitability, pain perception, and synaptic plasticity. By modulating ion flux through these channels in neuronal preparations, the peptide supports studies aimed at elucidating the mechanistic links between mechanical stimuli and neural activity. This has opened new avenues for exploring the contribution of mechanosensitive channels to sensory transduction, neural development, and adaptive responses in the nervous system.
Biophysical Tool Development: Beyond its direct use in biological experiments, GsMTx4 is instrumental in the development of innovative biophysical tools and assays. Its well-characterized mode of action makes it suitable for validating new mechanosensitive channel probes, biosensors, and screening platforms. By serving as a reference inhibitor, it aids in the benchmarking of novel compounds and methodologies designed to target mechanosensitive ion channels, thereby advancing the field of ion channel pharmacology and facilitating the discovery of new modulators with potential research applications.
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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