De novo design and synthesis of a mu-conotoxin KIIIA peptidomimetic
- Author(s)
- Brady, RM; Zhang, MM; Gable, R; Norton, RS; Baell, JB;
- 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
- Research Division(s)
- Structural Biology
- Publisher's Version
- https://doi.org/10.1016/j.bmcl.2013.06.086
- Terms of Use/Rights Notice
- Copyright © 2013 Elsevier Ltd. All rights reserved.
Creation Date: 2013-09-01 12:00:00