| http://purl.uniprot.org/citations/26721415 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26721415 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/26721415 | http://www.w3.org/2000/01/rdf-schema#comment | "Peptide toxins often have divergent pharmacological functions and are powerful tools for a deep review on the current understanding of the structure-function relationships of voltage-gated sodium channels (VGSCs). However, knowing about the interaction of site 3 toxins from tarantula venoms with VGSCs is not sufficient. In the present study, using whole-cell patch clamp technique, we determined the effects of Jingzhaotoxin-I (JZTX-I) on five VGSC subtypes expressed in HEK293 cells. The results showed that JZTX-I could inhibit the inactivation of rNav1.2, rNav1.3, rNav1.4, hNav1.5 and hNav1.7 channels with the IC50 of 870 ± 8 nM, 845 ± 4 nM, 339 ± 5 nM, 335 ± 9 nM, and 348 ± 6 nM, respectively. The affinity of the toxin interaction with subtypes (rNav1.4, hNav1.5, and hNav1.7) was only 2-fold higher than that for subtypes (rNav1.2 and rNav1.3). The toxin delayed the inactivation of VGSCs without affecting the activation and steady-state inactivation kinetics in the physiological range of voltages. Site-directed mutagenesis indicated that the toxin interacted with site 3 located at the extracellular S3-S4 linker of domain IV, and the acidic residue Asp at the position1609 in hNav1.5 was crucial for JZTX-I activity. Our results provide new insights in single key residue that allows toxins to recognize distinct ion channels with similar potency and enhance our understanding of the structure-function relationships of toxin-channel interactions."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.toxicon.2015.12.009"xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.toxicon.2015.12.009"xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Chen X."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Chen X."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Deng M."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Deng M."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Liu Z."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Liu Z."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Lu M."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Lu M."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Liang S."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Liang S."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Wu Y."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Wu Y."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Zeng X."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Zeng X."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Tao H."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/author | "Tao H."xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/date | "2016"xsd:gYear |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/date | "2016"xsd:gYear |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/name | "Toxicon"xsd:string |
| http://purl.uniprot.org/citations/26721415 | http://purl.uniprot.org/core/name | "Toxicon"xsd:string |