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De novo design and synthesis of a mu-conotoxin KIIIA peptidomimetic


Brady, RM; Zhang, MM; Gable, R; Norton, RS; Baell, JB
2013-09-01
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Journal Article
23
17
4892-4895
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.
PERGAMON-ELSEVIER SCIENCE LTD,
Conotoxin; Peptidomimetic; Sodium channel blocker; KIIIA; Pain
Structural Biology
10.1016/j.bmcl.2013.06.086
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Creation Date 2013-09-01 12:00:00