Structure-activity relationships of α-conotoxins targeting neuronal nicotinic acetylcholine receptors

摘要: alpha-Conotoxins that target the neuronal nicotinic acetylcholine receptor have a range of potential therapeutic applications and are valuable probes for examining subtype selectivity. The three-dimensional structures about half known specific alpha-conotoxins now been determined consensus fold containing helical region braced by two conserved disulfide bonds. These bonds define two-loop framework characteristic alpha-conotoxins, CCXmCXnC, where loop 1 comprises four residues (m = 4) 2 between three seven (n 3, 6 or 7). Structural studies, particularly using NMR spectroscopy provided an insight into role spatial location implicated in binding biological activity.