Assays for histone deacetylase 1/2 selective inhibitors

Details Assays for histone deacetylase 1/2 selective inhibitors Assays for histone deacetylase 1/2 selective inhibitors

C - Chemistry, Metallurgy

12

Q

C12Q 1/34 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2626917

The present invention relates to an assay specific for histone deacetylases HDACl and/or 2 inhibitors which comprises: (i) incubating an HDACl and/or 2 enzyme(s) together with a protein that contains the SANT and ELM2 regions, found in MTA proteins such as MTA-2, MTA-I, MTA-3 and also found in CoREST, CoREST2, CoREST3 and MI-ERl, in a suitable assay buffer (ii) adding the potential HDAC inhibitor and a suitable substrate and incubating (iii) stopping the incubation and determining the effect the putative HDAC inhibitor has had on enzyme activity by comparison with standards.

L'invention porte sur un bio-essai de recherche d'inhibiteurs spécifiques de l'histone déacétylase (HDAC) 1 et/ou 2, consistant: (i) à incuber dans un tampon de bio-essai approprié une enzyme HDAC 1 et/ou 2 avec une protéine comportant les régions SANT et ELM2 des protéines MTA telles que les MTA-2, MTA-I, MTA-3 et des protéines CoREST, CoREST2, CoREST3 et MI-Erl, (ii) à ajouter l'inhibiteur HDAC potentiel, puis procéder à l'incubation, et (iii) à arrêter l'incubation et déterminer les effets que l'inhibiteur HDAC putatif a eu sur l'activité enzymatique par comparaison avec les références.

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