Conotoxins

Details Conotoxins Conotoxins

C - Chemistry, Metallurgy

07

K

C07K 14/435 (2006.01) A61K 38/10 (2006.01) A61K 38/17 (2006.01) A61P 25/00 (2006.01) C07K 7/08 (2006.01) G01N 33/566 (2006.01)

Patent

CA 2420184

A substantially pure conotoxin which is highly selective for a specific human receptor, which conotoxin is selected from the group consisting of: Glu-Ser-Glu-Glu-Gly-Gly-Ser-Asn-Ala-Thr-Lys-Lys-Pro- Tyr-Ile-Leu (SEQ ID NO:13) wherein Glu in the 1-position is pGlu and the C-terminus is amidated; Gly-Glu-Xaa-Xaa-Va1-Ala-Lys-Met-Ala-Ala-Xaa-Leu-Ala- Arg-Xaa-Asn-Ile-Ala-Lys-Gly-Cys-Lys-Val-Asn-Cys-Tyr- Pro (SEQ ID NO:12) wherein Xaa is Gla; Ser-Thr-Ser-Cys-Met-Glu-Ala-Gly-Ser-Tyr-Cys-Gly-Ser- Thr-Thr-Arg-Ile-Cys-Cys-Gly-Tyr-Cys-Ala-Tyr-Phe-Gly- Lys-Lys-Cys-Ile-Asp-Tyr-Pro-Ser-Asn (SEQ ID NO:11); Cys-Lys-Thr-Tyr-Ser-Lys-Tyr-Cys-Xaa-Ala-Asp-Ser-Xaa- Cys-Cys-Thr-Xaa-Gln-Cys-Val-Arg-Ser-Tyr-Cys-Thr-Leu- Phe (SEQ ID NO:10) wherein Xaa is Gla and the C-terminus is amidated; His-Xaa-Xaa-Cys-Cys-Leu-Tyr-Gly-Lys-Cys-Arg-Arg-Tyr- Xaa-Gly-Cys-Ser- Ser-Ala-Ser-Cys-Cys-Gln (SEQ ID NO:9) wherein Xaa is 4Hyp; Gly-Cys-Cys-Ser-His-Pro-Ala-Cys-Ser-Gly-Lys-Tyr-Gln- Xaa-Tyr-Cys-Arg- Xaa- Ser (SEQ ID NO:8) wherein Xaa is Gla and the C-terminus is amidated; and Gly-Xaa-Ser-Phe-Cys-Lys-Ala-Asp-Glu-Lys-Xaa-Cys-Glu- Tyr-His-Ala-Asp-Cys-Cys-Asn-Cys-Cys-Leu-Ser-Gly-Ile- Cys-Ala-Xaa-Ser-Thr-Asn-Trp-Ile-Leu-Pro-Gly-Cys-Ser- Thr-Ser-Ser-Phe-Phe-Lys-Ile (SEQ ID NO:7) wherein Xaa is 4Hyp. These conotoxins may be used to prepare medicaments for the treatment of neuromuscular disorders. Some may be used for rapid reversible immobilisation of muscles or for diagnosing myasthenia gravis or Lambert-Eaton myasthenic syndrome.

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