http://purl.uniprot.org/citations/29925760 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/29925760 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
http://purl.uniprot.org/citations/29925760 | http://www.w3.org/2000/01/rdf-schema#comment | "α-Conotoxin TxID was discovered from Conus textile by gene cloning, which has 4/6 inter-cysteine loop spacing and selectively inhibits α3β4 nicotinic acetylcholine receptor (nAChR) subtype. However, TxID is susceptible to modification due to it containing a methionine (Met) residue that easily forms methionine sulfoxide (MetO) in oxidative environment. In this study, we investigated how Met-11 and its derivatives affect the activity of TxID using a combination of electrophysiological recordings and molecular modelling. The results showed most TxID analogues had substantially decreased activities on α3β4 nAChR with more than 10-fold potency loss and 5 of them demonstrated no inhibition on α3β4 nAChR. However, one mutant, [M11I]TxID, displayed potent inhibition at α3β4 nAChR with an IC50 of 69 nM, which only exhibited 3.8-fold less compared with TxID. Molecular dynamics simulations were performed to expound the decrease in the affinity for α3β4 nAChR. The results indicate replacement of Met with a hydrophobic moderate-sized Ile in TxID is an alternative strategy to reduce the impact of Met oxidation, which may help to redesign conotoxins containing methionine residue."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.org/dc/terms/identifier | "doi:10.3390/md16060215"xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.org/dc/terms/identifier | "doi:10.3390/md16060215"xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Luo S."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Luo S."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Li R."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Li R."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Ren J."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Ren J."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Wu Y."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Wu Y."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Zhu X."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Zhu X."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Zhangsun D."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Zhangsun D."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Ning J."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/author | "Ning J."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/date | "2018"xsd:gYear |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/date | "2018"xsd:gYear |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/name | "Mar. Drugs"xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/name | "Mar. Drugs"xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/title | "Effect of methionine oxidation and substitution of alpha-conotoxin TxID on alpha3beta4 nicotinic acetylcholine receptor."xsd:string |
http://purl.uniprot.org/citations/29925760 | http://purl.uniprot.org/core/title | "Effect of methionine oxidation and substitution of alpha-conotoxin TxID on alpha3beta4 nicotinic acetylcholine receptor."xsd:string |