TY - JOUR
T1 - Interaction of alpha-conotoxin ImII and its analogs with nicotinic receptors and acetylcholine-binding proteins: additional binding sites on Torpedo receptor
AU - Kasheverov, I.E.
AU - Zhmak, M.N.
AU - Fish, A.
AU - Rucktooa, P.
AU - Khruschov, A.Y.
AU - Osipov, A.V.
AU - Ziganshin, R.H.
AU - D'Hoedt, D.
AU - Bertrand, D.
AU - Sixma, T.K.
AU - Smit, A.B.
AU - Tsetlin, V.I.
PY - 2009
Y1 - 2009
N2 - α-Conotoxins interact with nicotinic acetylcholine receptors (nAChRs) and acetylcholine-binding proteins (AChBPs) at the sites for agonists/competitive antagonists. α-Conotoxins blocking muscle-type or α7 nAChRs compete with α-bungarotoxin. However, α-conotoxin ImII, a close homolog of the α7 nAChR-targeting α-conotoxin ImI, blocked α7 and muscle nAChRs without displacing α-bungarotoxin (Ellison et al. 2003, 2004), suggesting binding at a different site. We synthesized α-conotoxin ImII, its ribbon isomer (ImIIiso), 'mutant' ImII(W10Y) and found similar potencies in blocking human α7 and muscle nAChRs in Xenopus oocytes. Both isomers displaced [
AB - α-Conotoxins interact with nicotinic acetylcholine receptors (nAChRs) and acetylcholine-binding proteins (AChBPs) at the sites for agonists/competitive antagonists. α-Conotoxins blocking muscle-type or α7 nAChRs compete with α-bungarotoxin. However, α-conotoxin ImII, a close homolog of the α7 nAChR-targeting α-conotoxin ImI, blocked α7 and muscle nAChRs without displacing α-bungarotoxin (Ellison et al. 2003, 2004), suggesting binding at a different site. We synthesized α-conotoxin ImII, its ribbon isomer (ImIIiso), 'mutant' ImII(W10Y) and found similar potencies in blocking human α7 and muscle nAChRs in Xenopus oocytes. Both isomers displaced [
U2 - 10.1111/j.1471-4159.2009.06359.x
DO - 10.1111/j.1471-4159.2009.06359.x
M3 - Article
SN - 0022-3042
VL - 111
SP - 934
EP - 944
JO - Journal of Neurochemistry
JF - Journal of Neurochemistry
ER -