Alpha-RgIA, a novel conotoxin that blocks the alpha9alpha10 nAChR: structure and identification of key receptor-binding residues Alpha-conotoxins are small disulfide-constrained peptides from cone snails that act as antagonists at specific subtypes of nicotinic acetylcholine receptor... M Ellison,ZP...
alpha-Conotoxin RgIA and Vc1.1 are two well-known peptides blocking alpha 9 alpha 10 nAChR potently and selectively, which have been extensively investigated as drug candidates. Several key residues were established in previous experimental research. However, the mechanism of the specific interaction ...
α-Conotoxins PeIA, RgIA and Vc1.1 Three newly dis- covered α-conotoxins have been shown to target the α9α10 nAChR, a subtype with highly unusual pharmacology as compared to other nAChRs[110, 111]. α-CTx PeIA, cloned from the venom of Conus pergrandis, blocks heterologously expressed...
Previously the 13-amino-acid peptide, RgIA, was shown to block alpha 9 alpha 10 nAChRs with high potency and specificity. This peptide, characterized from the venom of the carnivorous marine snail, Conus regius, produced analgesia in several rodent models of chronic pain. Despite promising pre-...
α-RgIA, a Novel Conotoxin That Blocks the α9α10 nAChR: Structure and Identification of Key Receptor-Binding Residues α-Conotoxins are small disulfide-constrained peptides from cone snails that act as antagonists at specific subtypes of nicotinic acetylcholine receptors (... M Ellison,ZP Feng...
Pacini A, Micheli L, Maresca M, Branca JJ, McIntosh JM, Ghelardini C, Di Cesare Mannelli L (2016) The α9α10 nicotinic receptor antagonist α-cono- toxin RgIA prevents neuropathic pain induced by oxaliplatin treatment. Exp Neurol 282:37-48....
FIELD: biochemistry.;SUBSTANCE: present invention relates to a novel peptide compound capable of blocking pain signal transmission. Invention object is an analogue of conotoxin RgIA, in which disulphide bonds are modified to thioester bonds. Novel analogue shows high biological and physiological activity...
Marine snail alpha-conotoxins PnIA, RgIA and ArIB11L16D, blockers of alpha 3 beta 2/alpha 6 beta 2, alpha 9 alpha 10 and alpha 7 nAChR subtypes, respectively, as well as alpha-cobratoxin, a blocker of alpha 7 and muscle subtype nAChRs, exhibit low cytotoxicity, but enhance the ...
Weiss, B.; Ebel, R.; Elbrächter, M.; Kirchner, M.; Proksch, P. Defense Metabolites from the Marine Sponge Verongia Aerophoba. Biochem. Syst. Ecol. 1996, 24, 1–12. [Google Scholar] [CrossRef] Bergeron, Z.L.; Chun, J.B.; Baker, M.R.; Sandall, D.W.; Peigneur, S.; ...
αO-conotoxin GeXIVA[1,2] was isolated in our laboratory from Conus generalis, a snail native to the South China Sea, and is a novel, nonaddictive, intramuscularly administered analgesic targeting the α9α10 nicotinic acetylcholine receptor (nAChR) with