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http://purl.uniprot.org/citations/29614714http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/29614714http://www.w3.org/1999/02/22-rdf-syntax-ns#typehttp://purl.uniprot.org/core/Journal_Citation
http://purl.uniprot.org/citations/29614714http://www.w3.org/2000/01/rdf-schema#comment"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."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.org/dc/terms/identifier"doi:10.3390/md16040112"xsd:string
http://purl.uniprot.org/citations/29614714http://purl.org/dc/terms/identifier"doi:10.3390/md16040112"xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Chen J."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Chen J."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Cai F."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Cai F."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Liu Z."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Liu Z."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Zhou L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Zhou L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Zhang L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Zhang L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Dai Q."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Dai Q."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Liang L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Liang L."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Ning H."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/author"Ning H."xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/date"2018"xsd:gYear
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/date"2018"xsd:gYear
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/name"Mar. Drugs"xsd:string
http://purl.uniprot.org/citations/29614714http://purl.uniprot.org/core/name"Mar. Drugs"xsd:string