De novo design and synthesis of a mu-conotoxin KIIIA peptidomimetic
Details
Publication Year 2013-09-01, Volume 23, Issue #17, Page 4892-4895
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Publication Type
Journal Article
Abstract
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.
Publisher
PERGAMON-ELSEVIER SCIENCE LTD,
Keywords
Conotoxin; Peptidomimetic; Sodium channel blocker; KIIIA; Pain
WEHI Research Division(s)
Structural Biology
Rights Notice
Copyright © 2013 Elsevier Ltd. All rights reserved.


Creation Date: 2013-09-01 12:00:00
Last Modified: 0001-01-01 12:00:00
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