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Bioorg. Med. Chem. Lett. · Sep 2013
De novo design and synthesis of a μ-conotoxin KIIIA peptidomimetic.
- Ryan M Brady, Minmin Zhang, Robert Gable, Raymond S Norton, and Jonathan B Baell.
- The Walter and Eliza Hall Institute of Medical Research, 1G Royal Parade, Parkville, VIC 3052, Australia.
- Bioorg. Med. Chem. Lett. 2013 Sep 1; 23 (17): 4892-5.
Abstractμ-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. Copyright © 2013 Elsevier Ltd. All rights reserved.
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