A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor.

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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 mimetics. 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.

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Journal

Journal ID (iso-abbrev): Bioorg. Med. Chem. Lett.

Title: Bioorganic & medicinal chemistry letters

Publisher: Elsevier BV

ISSN: 0960-894X

ISSN (Print): 0960-894X

Publication date (Electronic): Jul 01 2005

Volume: 15

Issue: 13

Affiliations

[1 ] The Walter and Eliza Hall, Institute of Medical Research, Biotechnology Centre, 4 Research Avenue, La Trobe R and D Park, Bundoora 3086, Australia.

Article

Publisher Item ID: S0960-894X(05)00557-3

DOI: 10.1016/j.bmcl.2005.05.014

PubMed ID: 15935664

SO-VID: ec21fac3-f598-4faf-93b0-df31841bc3f2

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