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Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs

by 1,2, 3,* and 1,2,*
Hainan Provincial Key Laboratory of Carcinogenesis and Intervention, Hainan Medical College, Haikou 571199, Hainan, China
Institution of Tumor, Hainan Medical College, Haikou 570102, Hainan, China
Nebraska Center for Virology, School of Veterinary Medicine and Biological Sciences, University of Nebraska-Lincoln, Lincoln, NE 68583, USA
Authors to whom correspondence should be addressed.
Academic Editors: John B. MacMillan and Tadeusz F. Molinski
Mar. Drugs 2016, 14(10), 173;
Received: 28 July 2016 / Revised: 20 September 2016 / Accepted: 21 September 2016 / Published: 11 October 2016
(This article belongs to the Special Issue Structural Techniques in Natural Products Drug Discovery)
Nicotinic acetylcholine receptors (nAChRs) are targets for developing new drugs to treat severe pain, nicotine addiction, Alzheimer disease, epilepsy, etc. α-Conotoxins are biologically and chemically diverse. With 12–19 residues and two disulfides, they can be specifically selected for different nAChRs. Acetylcholine-binding proteins from Aplysia californica (Ac-AChBP) are homologous to the ligand-binding domains of nAChRs and pharmacologically similar. X-ray structures of the α-conotoxin in complex with Ac-AChBP in addition to computer modeling have helped to determine the binding site of the important residues of α-conotoxin and its affinity for nAChR subtypes. Here, we present the various α-conotoxin residues that are selective for Ac-AChBP or nAChRs by comparing the structures of α-conotoxins in complex with Ac-AChBP and by modeling α-conotoxins in complex with nAChRs. The knowledge of these binding sites will assist in the discovery and design of more potent and selective α-conotoxins as drug leads. View Full-Text
Keywords: α-conotoxins; nAChRs; Ac-AChBP; X-ray structure; model; design α-conotoxins; nAChRs; Ac-AChBP; X-ray structure; model; design
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Lin, B.; Xiang, S.; Li, M. Residues Responsible for the Selectivity of α-Conotoxins for Ac-AChBP or nAChRs. Mar. Drugs 2016, 14, 173.

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