GsMTx4 |
Catalog No.GC38465 |
GsMTx4 inhibe sélectivement les canaux mécanosensibles perméables aux cations (MSC) appartenant aux familles de canaux Piezo et TRP.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1209500-46-8
Sample solution is provided at 25 µL, 10mM.
GsMTx4 is a 34 amino acid spider venom peptide and belongs to the huwentoxin-1 family[1]. GsMTx4 selectively inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo, TRPC1 and TRPC6 channels.
GsMTx4 is similar to many other channel-active peptides isolated from spider venom, which are small (3–5 kD) amphipathic molecules built on a conserved inhibitory cysteine-knot (ICK) backbone[4].GsMTx4 has high potency for inhibiting mechanosensitive channels, and its inhibition is not stereospecific, i.e., both its enantiomers (L- and D-form) inhibiting MSCs[3].
GsMTx4 significantly attenuates bladder hyperactivity[2]. Intraperitoneal injection of GsMTx-4 has been shown to reduce mechanical hyperalgesia induced by carrageenan or sciatic nerve injury[5], although it does not inhibit SAC currents in cultured DRG neurons[6].
GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology[4].
References
[1]. Suchyna TM, et al. Identification of a peptide toxin from Grammostola spatulata spider venom that blocks cation-selective stretch-activated channels. J Gen Physiol. 2000 May;115(5):583-98.
[2]. Liu Q, et al. Increased Piezo1 channel activity in interstitial Cajal-like cells induces bladder hyperactivity by functionally interacting with NCX1 in rats with cyclophosphamide-induced cystitis. Exp Mol Med. 2018 May 7;50(5):60.
[3]. Suchyna T.M., Tape S.E., Gottlieb P.A. Bilayer-dependent inhibition of mechanosensitive channels by neuroactive peptide enantiomers. Nature. 2004;430:235–240.
[4]. Gnanasambandam R, et al. GsMTx4: Mechanism of Inhibiting Mechanosensitive Ion Channels. Biophys J. 2017 Jan 10;112(1):31-45.
[5]. Park SP, et al. A tarantula spider toxin, GsMTx4, reduces mechanical and neuropathic pain. Pain. 2008;137:208–217.
[6]. Drew LJ, , et al.. High-threshold mechanosensitive ion channels blocked by a novel conopeptide mediate pressure-evoked pain. PLoS ONE. 2007;2:e515.
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