Screening method for identifying hsp90 modulators

G - Physics – 01 – N

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G01N 33/68 (2006.01)

Patent

CA 2524072

A screening method for identifying and/or analysing Hsp90 inhibitors and/or Hsp90 agonists comprises the steps of contacting a compound with at least two of yeast strains A - E wherein each yeast strain comprises expression vectors from which a pair of binding partners for a yeast two-hybrid assay are expressed. The binding partner pairs comprise: A: Hsp90-targeting protein; B: Hsp90-Hsp9O; C: Hsp90-p23; D: Hsp90-E3 ligase; E: Hsp90-Client. Inhibition and/or promotion of dimerisation between the binding partners is then measured.

La présente invention concerne un procédé de criblage permettant d'identifier et/ou d'analyser des inhibiteurs de Hsp90 et/ou des agonistes de Hsp90. Ce procédé comprend les étapes consistant à mettre en contact un composé avec au moins deux souches de levure A - E telles que chaque souche de levure comprend des vecteurs d'expression à partir desquels sont exprimés deux partenaires de liaison pour une bioanalyse de levure à deux hybrides. Les paires de partenaires de liaison comprennent: A: Hsp90-protéine de ciblage; B: Hsp90-Hsp90; C: Hsp90-p23; D: Hsp90-ligase E3; E: Hsp90-client. L'inhibition et/ou l'activation de la dimérisation entre les partenaires de liaison est ensuite mesurée.

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