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Mapping the molecular surface of the analgesic NaV17-selective peptide Pn3a reveals residues essential for membrane and channel interactions

ACS Pharmacol. Transl. Sci.. 2020; 
Alexander Mueller, Zoltan Dekan, Quentin Kaas, Akello Joanna Agwa, Hana Starobova, Paul F. Alewood, Christina I Schroeder, Mehdi Mobli, Jennifer R. Deuis, and Irina Vetter
Products/Services Used Details Operation
Molecular Biology Reagents The QuikChange II XL kit (Agilent Technologies, Santa Clara, CA, USA) was used for sitedirected mutagenesis on murine Scn9a (encoding mNaV1.7) containing plasmids (GenScript, Piscataway, NJ, USA; Accession number NM_001290674, transcript variant 1) according to the manufacturer’s instructions to introduce a F823G mutation, equivalent to F813 in hNaV1.7. Get A Quote

摘要

Endogenous active substance guanosine diphosphate (GDP) is involved in the physiological process of DNA transfection and expression in the cytoplasm by binding to Ran proteins. To substantially improve the gene delivery efficiency of nanoparticles, phospholipid-coated Ca(P-GDP)/pDNA/NLS hybrid nanoparticles were prepared using GDP as a common biophosphorus source based on the biological process of exogenous gene expression in the cells. This nanoparticle has a relative uniform particle size distribution and in vitro stability. The addition of GDP in nanoparticles significantly enhanced the gene expression efficiency with good biocompatibility. Moreover, an in vivo study further verified that hybrid nanoparticle... More

关键词

Structure-activity relationship, Peptide synthesis, Voltage-gated sodium channel 1.7, Gatingmodifier toxin, Pharmacophore, Pain.