A method of modulating cellular activity

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 9/12 (2006.01) A61K 31/145 (2006.01) A61K 31/352 (2006.01) A61K 38/00 (2006.01) A61K 38/19 (2006.01) A61P 29/00 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) A61K 38/45 (2006.01)

Patent

CA 2480661

The present invention relates generally to a method of modulating cellular activity and to agents for use therein. More particularly, the present invention provides a method of modulating cellular activity by modulating phosphorylation of sphingosine kinase and, thereby, its activation. In a related aspect, the present invention provides a method of modulating sphingosine kinase functional activity via modulation of its phosphorylation and agents for use therein. The present invention still further extends to sphingosine kinase variants and to functional derivatives, homologues or analogues, chemical equivalents and mimetics thereof exhibiting reduced and/or ablated capacity to undergo phosphorylation. The method and molecules of the present invention are useful, inter alia, in the treatment and/or prophylaxis of conditions characterised by aberrant, unwanted or otherwise inappropriate cellular and/or sphingosine kinase functional activity. The present invention is further directed to methods for identifying and/or designing agents capable of modulating sphingosine kinase phosphorylation.

L'invention concerne de manière générale une méthode de modulation d'activité cellulaire et les agents utilisés pour ce faire. L'invention concerne, plus particulièrement, une méthode de modulation d'activité cellulaire par modulation de la phosphorylation de la sphingosine kinase et, de ce fait, son activation. Dans un aspect correspondant, l'invention concerne une méthode de modulation de l'activité fonctionnelle de la sphingosine kinase via la modulation de sa phosphorylation et des agents utilisés pour ce faire. L'invention concerne également des variants de la sphingosine kinase et des dérivés fonctionnels, des homologues ou des analogues, des équivalents chimiques et des mimétiques de ceux-ci présentant une aptitude réduite et/ou diminuée à la phosphorylation. Ladite méthode et les molécules de l'invention sont utiles, inter allia, dans le traitement et/ou la prophylaxie d'états caractérisés par une activité fonctionnelle cellulaire et/ou de la sphingosine kinase aberrante, non souhaitée ou autrement inappropriée. L'invention concerne enfin des méthodes permettant d'identifier et/ou de désigner des agents capables de moduler la phosphorylation de la sphingosine kinase.

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