title: De novo design and synthesis of a μ-conotoxin KIIIA peptidomimetic.
abstract: μ-Conotoxin KIIIA blocks voltage-gated sodium channels and displays potent analgesic activity in mice models for pain. Structure-activity studies with KIIIA have shown that residues important for sodium channel activity are presented on an α-helix. Herein, we report the de novo design and synthesis of a three-residue (Lys7, Trp8, His12) peptidomimetic based on a novel diketopiperazine (DKP) carboxamide scaffold.
authors.affiliation: The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.
authors.forename: Ryan M
authors.initials: RM
authors.lastname: Brady
authors.forename: Minmin
authors.initials: M
authors.lastname: Zhang
authors.forename: Robert
authors.initials: R
authors.lastname: Gable
authors.forename: Raymond S
authors.initials: RS
authors.lastname: Norton
authors.forename: Jonathan B
authors.initials: JB
authors.lastname: Baell
mesh_terms: D000818:Animals; D020916:Conotoxins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D052078:Conus Snail / Q000737:chemistry; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D010146:Pain / Q000188:drug therapy; D057786:Peptidomimetics / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D026941:Sodium Channel Blockers / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D020916:Conotoxins; D057786:Peptidomimetics; D026941:Sodium Channel Blockers
keywords: Conotoxin; KIIIA; Pain; Peptidomimetic; Sodium channel blocker