Ontology highlight
ABSTRACT:
SUBMITTER: Paul George AA
PROVIDER: S-EPMC6669574 | biostudies-literature | 2019 Jul
REPOSITORIES: biostudies-literature
Paul George Ajay Abisheck AA Heimer Pascal P Leipold Enrico E Schmitz Thomas T Kaufmann Desiree D Tietze Daniel D Heinemann Stefan H SH Imhof Diana D
Marine drugs 20190702 7
Cyclic µ-conotoxin PIIIA, a potent blocker of skeletal muscle voltage-gated sodium channel Na<sub>V</sub>1.4, is a 22mer peptide stabilized by three disulfide bonds. Combining electrophysiological measurements with molecular docking and dynamic simulations based on NMR solution structures, we investigated the 15 possible 3-disulfide-bonded isomers of µ-PIIIA to relate their blocking activity at Na<sub>V</sub>1.4 to their disulfide connectivity. In addition, three µ-PIIIA mutants derived from the ...[more]