Figure 5: α3β4 pharmacophore.
From: Structural mechanisms for α-conotoxin activity at the human α3β4 nicotinic acetylcholine receptor
(a) α3β4 activity was successfully introduced into LsIA through systematic modification of interactions at position 10 and 12. The [R10F][N12L]-LsIA provided a > 250-fold selectivity for α3β4 over α7 nAChR. Data represent the mean ± S.E.M of triplicate data from three independent experiments. (b) The highly conserved aromatic cage involved in ligand recognition at the nAChRs is shown in black. Using α-conotoxin LsIA we have identified residues (boxed) that lie outside this conserved aromatic cage and contribute to ligand recognition at the α3β4.
