Alpha conotoxin peptides with analgesic properties

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 7/08 (2006.01) A61K 38/10 (2006.01) A61P 21/00 (2006.01) A61P 25/00 (2006.01) A61P 25/02 (2006.01) A61P 25/08 (2006.01) A61P 25/16 (2006.01) A61P 25/28 (2006.01) A61P 25/34 (2006.01) A61P 29/00 (2006.01) C07K 14/435 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2442495

This invention relates to novel .alpha.-conotoxin-like peptides comprising the following sequence of amino acids: Xaa1CCSXaa2Xaa3Xaa4CXaa5Xaa6Xaa7Xaa8Xaa9Xaa10Xaa11C-NH2 in which Xaa1 is G or D; Xaa3 is proline, hydroxyproline or glutamine; each of Xaa2 to Xaa8 and Xaa11 is independently any amino acid; Xaa9 is proline, hydroxyproline or glutamine; Xaa10 is aspartate, glutamate or .gamma.-carboxyglutamate; Xaa11 is optionally absent; and the C-terminus is optionally amidated, with the proviso that the peptide is not .alpha.-conotoxin Ep1 or .alpha.-conotoxin Im1. The peptides are useful in the treatment or prevention of pain, in recovery from nerve injury, and in the treatment of painful neurological conditions such as stroke.

L'invention se rapporte à de nouveaux peptides de type .alpha.-conotoxine comprenant la séquence suivante d'acides aminés: Xaa¿1?CCSXaa¿2?Xaa¿3?Xaa¿4?CXaa¿5?Xaa¿6?Xaa¿7?Xaa¿8?Xaa¿9?Xaa¿10?Xaa¿11?C-NH¿2? dans laquelle Xaa¿1? désigne G ou D; Xaa¿3? désigne une proline, une hydroxyproline ou une glutamine; pris indépendamment Xaa¿2? à Xaa¿8? et Xaa¿11? désigne un acide aminé quelconque; Xaa¿9? désigne une proline, une hydroxyproline ou une glutamine; Xaa¿10? désigne un aspartate, un glutamate ou un .gamma.-carboxyglutamate; Xaa¿11? est éventuellement absent; et la terminaison C est éventuellement amidifiée, à condition que le peptide ne soit pas une .alpha.-conotoxine Ep1 ou une .alpha.-conotoxine Im1. Les peptides sont utiles dans le traitement ou la prévention de douleurs, dans la récupération faisant suite à des lésions nerveuses et dans le traitement de pathologies neurologiques douloureuses, notamment les accidents vasculaires cérébraux.

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