Methods of peptide preparation

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/00 (2006.01) A61P 31/00 (2006.01) A61P 35/00 (2006.01) C07K 14/79 (2006.01)

Patent

CA 2382544

The present invention relates to a method of producing a bioactive peptide, wherein said peptide is 7 to 25 amino acids in length, has at least 3 cationic amino acids and is capable of forming an amphipathic .alpha.-helix, which method comprises identification of a cationic sector and division of the remaining part of the peptide into three further sectors which are substantially equal in size, and incorporation of at least 60 % of the bulk and lipophilicity provided by the amino acid R groups into the sectors flanking the cationic sector; and to uses of the peptides produced thereby in therapy, particularly in the treatment of benign or malignant tumours.

La présente invention concerne un procédé de production d'un peptide biologiquement actif ayant une longueur comprise entre 7 et 25 acides aminés, possédant au moins 3 acides aminés cationiques et pouvant former une hélice .alpha. amphipathique. Ce procédé consiste à identifier un secteur cationique et à diviser la partie restante du peptide en trois secteurs supplémentaires de taille sensiblement égale, et à incorporer au moins 60 % de la masse et de la lipophilie des groupes R d'acides aminés dans les secteurs flanquant le secteur cationique. L'invention concerne également des utilisations des peptides produits à des fins thérapeutiques, et en particulier dans le traitement des tumeurs malignes ou bénignes.

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