Rec2 kinase

Details Rec2 kinase Rec2 kinase

C - Chemistry, Metallurgy

12

N

C12N 9/12 (2006.01) A61K 38/51 (2006.01) C12Q 1/48 (2006.01)

Patent

CA 2343936

The invention includes a method of phosphorylating a serine containing substrate by incubating the substrate with ATP and an enzyme that is hsRec2 or muRec2 or a derivative thereof. The natural substrates of the kinase activity of Rec2 are the cell cycle control proteins such as p53 and cyclin E. The over expression of Rec2 is known to cause cell-cycle arrest and apoptosis and the invention discloses that these effects are kinase mediated. Accordingly, the invention provides a method of assessing antagonists and agonists of Rec2, which antagonists and agonists would have pharmacological activity. The invention further discloses that there is specific binding between hsRec2 and at least three cell cycle control proteins: p53, PCNA and cdc2.

L'invention se rapporte à un procédé de phosphorylation d'un substrat contenant la sérine, ce procédé étant réalisé par incubation du substrat au moyen de l'ATP et d'une enzyme hsRec2 ou muRec2, ou d'un dérivé de ladite enzyme. Les substrats naturels de l'activité kinase de Rec2 sont les protéines de régulation du cycle cellulaire, telles que la p53 et la cycline E. La surexpression de Rec2 est réputée provoquer l'interruption et l'apoptose du cycle cellulaire, et selon l'invention, ces effets sont liés à la présence de la kinase. En conséquence, l'invention porte sur un procédé d'évaluation d'antagonistes et d'agonistes de Rec2 pouvant avoir une activité pharmacologique. L'invention porte en outre sur la découverte selon laquelle il existe une liaison spécifique entre hsRec2 et au moins trois protéines de régulation du cycle cellulaire: p53, PCNA et cdc2.

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