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Mar. Drugs 2018, 16(4), 112;

Cloning, Synthesis and Functional Characterization of a Novel α-Conotoxin Lt1.3

Beijing Institute of Biotechnology, Beijing 100071, China
Institute of Physical Science and Information Technology, Anhui University, Hefei 236041, China
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Received: 20 February 2018 / Revised: 16 March 2018 / Accepted: 22 March 2018 / Published: 31 March 2018
(This article belongs to the Special Issue Marine Invertebrate Toxins)
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α-Conotoxins (α-CTxs) are small peptides composed of 11 to 20 amino acid residues with two disulfide bridges. Most of them potently and selectively target nicotinic acetylcholine receptor (nAChR) subtypes, and a few were found to inhibit the GABAB receptor (GABABR)-coupled N-type calcium channels (Cav2.2). However, in all of α-CTxs targeting both receptors, the disulfide connectivity arrangement “C1-C3, C2-C4” is present. In this work, a novel α4/7-CTx named Lt1.3 (GCCSHPACSGNNPYFC-NH2) was cloned from the venom ducts of Conus litteratus (C. litteratus) in the South China Sea. Lt1.3 was then chemically synthesized and two isomers with disulfide bridges “C1-C3, C2-C4” and “C1-C4, C2-C3” were found and functionally characterized. Electrophysiological experiments showed that Lt1.3 containing the common disulfide bridges “C1-C3, C2-C4” potently and selectively inhibited α3β2 nAChRs and not GABABR-coupled Cav2.2. Surprisingly, but the isomer with the disulfide bridges “C1-C4, C2-C3” showed exactly the opposite inhibitory activity, inhibiting only GABABR-coupled Cav2.2 and not α3β2 nAChRs. These findings expand the knowledge of the targets and selectivity of α-CTxs and provide a new structural motif to inhibit the GABABR-coupled Cav2.2. View Full-Text
Keywords: α-conotoxins; Lt1.3; cloning; synthesis; α3β2 nAChRs; GABABR-coupled Cav2.2 α-conotoxins; Lt1.3; cloning; synthesis; α3β2 nAChRs; GABABR-coupled Cav2.2

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Chen, J.; Liang, L.; Ning, H.; Cai, F.; Liu, Z.; Zhang, L.; Zhou, L.; Dai, Q. Cloning, Synthesis and Functional Characterization of a Novel α-Conotoxin Lt1.3. Mar. Drugs 2018, 16, 112.

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