Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors

• Published in: Journal of medicinal chemistry Vol. 66; no. 3; pp. 2020 - 2031
• Main Authors: Zhu, Xiaopeng, Wang, Shuai, Kaas, Quentin, Yu, Jinpeng, Wu, Yong, Harvey, Peta J., Zhangsun, Dongting, Craik, David J., Luo, Sulan
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 09.02.2023
• Subjects: Animals; Conotoxins - chemistry; Molecular Docking Simulation; Nicotinic Antagonists - chemistry; Nicotinic Antagonists - pharmacology; Oocytes; Rats; Receptors, Nicotinic - chemistry; Xenopus laevis

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 stru...