ABSTRACT: The one and only fold? Three chemically synthesized μ-conotoxin PIIIA isomers, which contain different disulfide connectivity, block the skeletal muscle voltage-gated sodium channel Na(V) 1.4 with similar, yet distinguishable potency. Hence, bioactivity of this μ-conotoxin is not strictly coupled to its native fold. Future development of conotoxin-derived analgesics may benefit from such a widened structural repertoire.
Angewandte Chemie International Edition 03/2012; 51(17):4058-61. · 13.45 Impact Factor