Halogen-stabilized insulin

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/62 (2006.01) A61K 38/28 (2006.01) C12N 15/17 (2006.01)

Patent

CA 2732439

An insulin analogue comprises a B-chain polypeptide incorporating a halogenated phenylalanine at position B24, B25 or B26. The halogenated phenylalanine may be ortho-monofluoro- phenylalanine, ortho-monobromo-phenylalanine or ortho-monochloro-phenylalanine. The analogue may be of a mammalian insulin, such as human insulin. A nucleic acid encodes such an insulin analogue. The halogenated insulin analogues retain significant activity. A method of treating a patient comprises administering a physiologically effective amount of the insulin analogue or a physiologically acceptable salt thereof to a patient. Halogen substitution-based stabilization of insulin may enhance the treatment of diabetes mellitus in regions of the developing world lacking refrigeration.

L'invention concerne un analogue d'insuline comprenant un polypeptide de chaîne B incorporant une phénylalanine halogénée dans la position B24, B25 ou B26. La phénylalanine halogénée peut être de l'ortho-monofluoro-phénylalanine, de l'ortho-monobromo-phénylalanine, ou de l'ortho-monochloro-phénylalanine. L'analogue peut être de l'insuline de mammifère, comme de l'insuline humaine. Un acide nucléique code un tel analogue d'insuline. Les analogues d'insuline halogénée conservent une activité importante. Un procédé de traitement d'un patient comprend l'administration d'une quantité physiologiquement efficace de l'analogue d'insuline, ou d'un sel physiologiquement acceptable de celui-ci, à un patient. Une stabilisation à base de substitution par halogène de l'insuline peut améliorer le traitement du diabète mellitus dans des zones des pays en voie de développement manquant de réfrigération.

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