GsMTx4

Product Name: GsMTx4

CAS No: 1209500-46-8

Purity: 95%

Molar Mass: 4095.8

Chemical Formula: C185H273N49O45S6

Storage: Store at -20??

Sequence: GCLEFWWKCNPNDDKCCRPKLKCSKLFKLCNFSF-NH2

Target: MSCs

Application: GsMTx4 (Grammostola spatulata Mechanosensitive Toxin 4) is a peptide toxin isolated from the tarantula Grammostola spatulata venom. It acts as a selective inhibitor of stretch-activated ion channels, particularly those involved in mechanotransduction processes in cells. By blocking these channels, GsMTx4 suppresses mechanical stress-induced responses, such as ion flux and cell signaling pathways. This peptide is widely used in biophysical and physiological research to study mechanosensitive channels, cell mechanics, and sensory transduction mechanisms. Its applications extend to exploring roles in cardiovascular physiology, neuronal mechanotransduction, and potential therapeutic strategies for conditions involving abnormal mechanosensitivity.

Current Research:

GsMTx4 is a 35-amino-acid peptide toxin isolated from the venom of the tarantula Grammostola spatulata. It functions as a potent inhibitor of mechanosensitive ion channels (MSCs), including Piezo1 and TRPC6, which are integral to various physiological processes such as touch sensation, vascular tone regulation, and cellular volume control.
Mechanism of Action
Unlike typical inhibitory cystine knot (ICK) peptides that directly bind to ion channel gating structures, GsMTx4 modulates MSC activity through a bilayer-dependent mechanism. It inserts into the lipid bilayer of the cell membrane, altering local membrane tension and thereby reducing the sensitivity of MSCs to mechanical stimuli. This indirect modulation affects the efficiency of force transfer from the lipid bilayer to the channel, leading to inhibition of channel activity. Notably, both L- and D-enantiomers of GsMTx4 exhibit similar inhibitory effects, indicating that its action is not stereospecific.
Applications in Research
Cardiovascular Studies: GsMTx4 has been employed to investigate the role of MSCs in cardiac physiology and pathophysiology. By inhibiting MSCs, it aids in understanding their contribution to conditions such as cardiac arrhythmias and hypertrophy.
Neuroscience Research: The peptide is utilized to study mechanotransduction in neurons, providing insights into sensory processes like touch and pain perception. Its ability to modulate MSCs makes it valuable in exploring neuronal responses to mechanical stimuli.
Muscular Dystrophy Models: GsMTx4 has shown potential in ameliorating symptoms of muscular dystrophy in animal models by inhibiting MSCs, which are implicated in muscle fiber damage due to abnormal mechanical stress responses.
Cancer Research: Emerging studies suggest that MSCs play a role in cancer cell migration and metastasis. GsMTx4 serves as a tool to dissect these mechanisms, offering potential therapeutic insights.
Therapeutic Potential
Due to its specificity and efficacy in inhibiting MSCs, GsMTx4 is being explored for therapeutic applications in conditions where MSC activity is dysregulated. Its favorable pharmacokinetic properties, including stability and non-immunogenicity, make it a promising candidate for drug development targeting mechanosensitive pathways.
Conclusion
GsMTx4 is a critical molecular tool in the study of mechanosensitive ion channels, providing valuable insights into their physiological and pathological roles. Ongoing research continues to explore its applications across various domains, including cardiovascular health, neuroscience, muscular dystrophy, and oncology, highlighting its potential in both basic research and therapeutic development.

Reference: Gnanasambandam, R., Ghatak, C., Yasmann, A., Nishizawa, K., Sachs, F., Ladokhin, A. S., ... & Suchyna, T. M. (2017). GsMTx4: mechanism of inhibiting mechanosensitive ion channels.?Biophysical journal,?112(1), 31-45.