This study delineated potential benefits and drawbacks of designing pharmacological hybrid peptides targeting hNaV1.7. (bvsalud.org)
Toxin4
In the present study we investigated the possible molecular mechanism of the antinociceptive efficacy of HWTX-I, a spider peptide toxin blocking Ca2+ channels, on the rat rheumatoid arthritis model. (smartox-biotech.com)
To do this, we created an array of heterodimeric toxins designed to target human NaV1.7 by ligating a conotoxin to a spider toxin and assessed the potency and selectivity of the resulting bivalent toxins. (bvsalud.org)
At hNaV1.4, a synergistic effect between the pore blocker and gating modifier toxin moieties was observed, resulting in altered sodium channel subtype selectivity compared to the parent peptides. (bvsalud.org)
Excelsatoxin A (ExTxA), a pain-causing knottin peptide from the Australian stinging tree Dendrocnide excelsa, is the first reported plant-derived NaV channel modulating peptide toxin. (bvsalud.org)
Inhibitor2
Intrathecal applications of BC-1215 (a Fbxo3 activity inhibitor), Fbxl2 mRNA-targeting small-interfering RNA, and ω-conotoxin GVIA (a Ca V 2.2 blocker) attenuated RIM1α upregulation, enhanced RIM1α expression, and exhibited no effect on RIM1α expression, respectively. (jneurosci.org)
This conformational exchange is especially peculiar for peptides containing an inhibitor cystine knot motif, which confers excellent structural stability under conditions that are not conducive to disulfide shuffling. (bvsalud.org)
Calcium channels2
The selectivity of Huwentoxin-I for calcium channels appears to be higher than ω-conotoxin MVIIA and equivalent to ω-conotoxin GVIA . (smartox-biotech.com)
Huwentoxin-I (HWTX-I) is a 33-residue peptide isolated from the venom of Ornithoctonus huwena and could inhibit TTX-sensitive voltage-gated sodium channels and N-type calcium channels in mammalian dorsal root ganglion (DRG) neurons. (smartox-biotech.com)
Calcium1
OMEGA-CONOTOXINS inhibit voltage-activated entry of calcium into the presynaptic membrane and therefore the release of ACETYLCHOLINE. (bvsalud.org)
Venom1
A neurotoxic peptide, which is a cleavage product (VIa) of the omega-Conotoxin precursor protein contained in venom from the marine snail, CONUS geographus. (nih.gov)
Inhibit1
Omega toxins inhibit the actions of these channels by altering their voltage dependence. (lookformedical.com)
Marine1
Peptide neurotoxins from the marine fish-hunting snails of the genus CONUS. (bvsalud.org)