A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor
- Author(s)
- Harvey, AJ; Gable, RW; Baell, JB;
- Details
- Publication Year 2005-07-01,Volume 15,Issue #13,Page 3193-3196
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Publication Type
- Journal Article
- Abstract
- The ShK toxin is a polypeptide that blocks the Kv1.3 potassium channel in T-lymphocytes and has been identified as a potential therapeutic for multiple sclerosis. ShK is well characterised in terms of structure and binding, offering an attractive target for the design of structural and functional mirnetics. Building on our previous success in developing rationally designed peptidomimetics of ShK, we report a novel mimetic of the K22 Y23-R24 residues of the peptide. The mimetic was shown to inhibit the Kv1.3 channel with moderate activity. (c) 2005 Elsevier Ltd. All rights reserved.
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- GATED POTASSIUM CHANNEL; SEA-ANEMONE TOXIN; MEMORY T-CELLS; AUTOIMMUNE-DISEASES; NONPEPTIDE MIMETICS; MULTIPLE-SCLEROSIS; CONOTOXIN GVIA; III MIMETICS; K+ CHANNELS; DESIGN
- Publisher's Version
- https://doi.org/10.1016/j.bmcl.2005.05.014
- Terms of Use/Rights Notice
- Refer to copyright notice on published article.
Creation Date: 2005-07-01 12:00:00