Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595426 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
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.
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Authors
Ryan M. Brady, Minmin Zhang, Robert Gable, Raymond S. Norton, Jonathan B. Baell,