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- W4317702937 startingPage "2020" @default.
- W4317702937 abstract "α6β4 nicotinic acetylcholine receptors (nAChRs) are expressed in the central and peripheral nervous systems, but their functions are not fully understood, largely because of a lack of specific ligands. Here, we characterized a novel α-conotoxin, LvIC, and designed a series of analogues to probe structure-activity relationships at the α6β4 nAChR. The potency and selectivity of these conotoxins were tested using two-electrode voltage-clamp recording on nAChR subtypes expressed in Xenopus laevis oocytes. One of the analogues, [D1G,ΔQ14]LvIC, potently blocked α6/α3β4 nAChRs (α6/α3 is a chimera) with an IC50 of 19 nM, with minimal activity at other nAChR subtypes, including the structurally similar α6/α3β2β3 and α3β4 subtypes. Using NMR, molecular docking, and receptor mutation, structure-activity relationships of [D1G,ΔQ14]LvIC at the α6/α3β4 nAChR were defined. It is a potent and specific antagonist of α6β4 nAChRs that could potentially serve as a novel molecular probe to explore α6β4 nAChR-related neurophysiological and pharmacological functions." @default.
- W4317702937 created "2023-01-22" @default.
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- W4317702937 date "2023-01-22" @default.
- W4317702937 modified "2023-10-14" @default.
- W4317702937 title "Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors" @default.
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- W4317702937 doi "https://doi.org/10.1021/acs.jmedchem.2c01786" @default.
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