The GABA(B) receptor antagonist CGP55845 (1 microM) antagonized the effect of Vc1.1 and RgIA on the N-type calcium channels in alpha9 KO mice. RT-PCR and western blot analysis confirmed the absen...
Alpha-RgIA: a novel conotoxin that specifically and potently blocks the alpha9alpha10 nAChR. The alpha9 and alpha10 nicotinic acetylcholine receptor (nAChR) subunits assemble to form the alpha9alpha10 nAChR subtype. This receptor is believed to med... M Ellison,C Haberlandt,ME Gomezcasati,.....
Structure-activity data with α-CTx RgIA have indicated that this toxin binds to the ACh binding site on the recep- tor and that toxin residues Asp5, Pro6, Arg7, and Arg9 are important for interaction with α9α10 nAChRs[121]. The recently published three-dimensional structure of α-...
alpha-Conotoxin RgIAalpha-Conotoxin Vc1.1Rat alpha 9 alpha 10 nAChRDockingMolecular dynamics simulationsBinding free energyThe alpha 9 alpha 10 nicotinic acetylcholine receptor (nAChR) is an effective therapeutic target for neuropathic pain. alpha-Conotoxin RgIA and Vc1.1 are two well-known peptides ...
The a9a10 nicotinic receptor antagonist a-conotoxin RgIA prevents neuropathic pain induced by oxaliplatin treatment. Exp Neurol 2016;282:37-48.Pacini A, Micheli L, Maresca M, Branca JJ, McIntosh JM, Ghelardini C, Di Cesare Mannelli L (2016) The α9α10 nicotinic receptor antagonist α-...
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...
In this study, we implement amino-acid substitutions to definitively characterize the chemical properties of RgIA that contribute to its activity against alpha 9 alpha 10 nAChRs. Using this mutational approach, we determined the vital role of biochemical side-chain properties and amino acids in the...
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 ...
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