5ug3

Structural highlights

Function

[CA1D_CONGE] Alpha-conotoxins act on postsynaptic membranes, they bind to the nicotinic acetylcholine receptors (nAChR) and thus inhibit them. This toxin reversibly blocks alpha-3-beta-2 (IC(50)=3.1-5.1 nM), alpha-7 (IC(50)=4.5-5.1 nM), and alpha-4-beta-2 (IC(50)=128.6-390 nM) nAChRs.^{[1] [2] [3]}

References

1. ↑ Nicke A, Loughnan ML, Millard EL, Alewood PF, Adams DJ, Daly NL, Craik DJ, Lewis RJ. Isolation, structure, and activity of GID, a novel alpha 4/7-conotoxin with an extended N-terminal sequence. J Biol Chem. 2003 Jan 31;278(5):3137-44. Epub 2002 Nov 4. PMID:12419800 doi:http://dx.doi.org/10.1074/jbc.M210280200
2. ↑ Dutertre S, Nicke A, Lewis RJ. Beta2 subunit contribution to 4/7 alpha-conotoxin binding to the nicotinic acetylcholine receptor. J Biol Chem. 2005 Aug 26;280(34):30460-8. Epub 2005 Jun 1. PMID:15929983 doi:http://dx.doi.org/10.1074/jbc.M504229200
3. ↑ Millard EL, Nevin ST, Loughnan ML, Nicke A, Clark RJ, Alewood PF, Lewis RJ, Adams DJ, Craik DJ, Daly NL. Inhibition of neuronal nicotinic acetylcholine receptor subtypes by alpha-Conotoxin GID and analogues. J Biol Chem. 2009 Feb 20;284(8):4944-51. doi: 10.1074/jbc.M804950200. Epub 2008, Dec 19. PMID:19098004 doi:http://dx.doi.org/10.1074/jbc.M804950200