Screening methods based on the use of protein kinases

Details Screening methods based on the use of protein kinases Screening methods based on the use of protein kinases

C - Chemistry, Metallurgy

07

K

C07K 14/39 (2006.01) C12N 9/12 (2006.01) C12N 15/81 (2006.01) C12Q 1/02 (2006.01) C12Q 1/48 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2355362

A method of identifying a compound which inhibits to different extents (a) a host yeast cell protein kinase or kinases and (b) a protein kinase derivable from a source other than the said host yeast cell that is equivalent to the said host yeast cell protein kinase or kinases, wherein a compound is exposed to 1) a first host yeast cell wherein the yeast cell is capable of expressing the said host yeast cell protein kinase or kinases and is not capable of expressing the said equivalent protein kinase and 2) a second host yeast cell wherein the yeast cell is (a) not capable of expressing the said yeast cell protein kinase or kinases and (b) is capable of expressing the said equivalent protein kinase derivable from a source other than the host yeast cell and the effect of the compound on the viability of the said yeast cells is measured, and a compound that affects the viability of the first said yeast cell and the said second yeast cell differently, is identified. The method may be useful in a screen for identifying compounds that inhibit a mammalian or fungal protein kinase. The compounds may be useful in medicine.

L'invention concerne une méthode d'identification d'un composé présentant, à divers égards, a) une protéine kinase ou des kinases d'une cellule de levure hôte; et b) une protéine kinase pouvant être obtenue d'une source autre que ladite protéine kinase ou lesdites kinases de la cellule de levure hôte et équivalente à la protéine kinase ou aux kinases. Un composé est exposé à: 1) une première cellule de levure hôte capable d'exprimer la protéine kinase ou les kinases, mais incapable d'exprimer la protéine kinase équivalente; et 2) une deuxième cellule de levure hôte qui est: a) incapable d'exprimer la protéine kinase ou les kinases de la cellule de levure; et b) capable d'exprimer cette protéine kinase équivalente pouvant être obtenue d'une source autre que la cellule de levure hôte. L'effet du composé sur la viabilité des cellules de levure hôtes est mesuré et un composé ayant une incidence différente sur la viabilité de la première cellule de levure et sur celle de la deuxième cellule de levure est identifié. Cette méthode peut être utile dans un criblage destiné à identifier des composés inhibant une protéine kinase mammalienne ou fongique. Ces composés peuvent être utiles dans des applications médicales.

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