Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 17, Pages 4892-4895Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.086
Keywords
Conotoxin; Peptidomimetic; Sodium channel blocker; KIIIA; Pain
Categories
Funding
- Australian Research Council Grant [DP1094212]
- Australian Research Council [DP1094212] Funding Source: Australian Research Council
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mu-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 alpha-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. (C) 2013 Elsevier Ltd. All rights reserved.
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