8.B.41.1.1 Tau-scoloptoxin(04)-Sm1b or RhTx of 69 aas and 1 N-terminal TMS. It is an extremely potent potentiator of TRPV1
(EC(50) = 521.5 nM). It strongly promotes the heat activation process by
downshifting the activation threshold temperature by preferably binding
to the activated channel, promoting its opening. Holding the channel
closed by cooling prevents binding of this toxin, leaving it
ineffective. The toxin binds to the charge-rich outer pore region of the
channel where it directly interacts with the pore helix and turret, two
adjacent structural elements known to be critical for activation gating
of TRPV1. In vivo, it induces pain in mice after intraplantar injection (Lee et al. 2015; Yang et al. 2015). The 3-D structure is known (PD# 2MVA-A). It does not act on mNav1.5/SCN5A, mNav1.7/SCN9A,
tetrodotoxin-sensitive and -resistant Nav, mKv1.1/KCNA1, mKv2.1/KCNB1,
mKv4.1/KCND1, high voltage activated Cav, low voltage activated Cav,
TRPV2, TRPV3 and TRPV4 (Yang et al. 2015).
|
Accession Number: | AKN58847 |
Protein Name: | AKN58847.1 RhTx [Scolopendra subspinipes] |
Length: | 70 |
Molecular Weight: | |
Species: | Scolopendra subspinipes [55038] |
Number of TMSs: | 1 |
Substrate |
|
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1: MMLKSFCILS VFMVLFLAKF PDLCSGEEIS PLKIVVRNSE YLNNPCNGVT CPSGYRCSIV
61: DKQCIKKEK