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Shk: A peptide isolated from the Caribbean Sea anemone, Stichodactyla heliantus. The 35 amino acid residue peptide is the most potent inhibitor of Kv1.1 and Kv1.3 potassium ion channels discovered to date. The peptide can be produced synthetically and its solution structure has been determined by NMR. Over 380 analogs have been synthesized to gain an understanding of how the peptide interacts with potassium ion channels and to improve its specificity for Kv1.3 potassium channels.
ShK-186, one novel synthetic analog, has a selectivity profile for the Kv1.3 potassium channel that is far greater than that of the naturally derived peptide. ShK -186 is effective in ameliorating disease in animal models of multiple sclerosis, rheumatoid arthritis and delayed type hypersensitivity, and it has an excellent safety profile. ShK-186 and its analogs are being developed as immunomodulators for the therapy of autoimmune diseases. |
