C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/44 (2006.01) A61K 31/00 (2006.01) A61K 38/45 (2006.01) C12N 9/16 (2006.01) G01N 33/535 (2006.01)
Patent
CA 2405711
An alternative therapeutic approach for PDE4 inhibition is disclosed. PDE4 dislocators, will remove the PDE4 away from the native location in the cell and thereby increase the concentration of cAMP in this location. By dislocating the PDE4, and thereby not acting directly on the catalytic, among phosphodiesterase inhibitors, well conserved site, the compound will act e.g. at the binding domain of the PDE4, thereby providing isoform-specific 'inhibitors' of PDE4. The dislocation of PDE4s are visualised with fusions to GFP. The native location is induced by treatment with Rolipram.
L'invention concerne une approche thérapeutique alternative pour l'inhibition de PDE4, selon laquelle des dislocateurs de PDE4 retirent les PDE4 de leur emplacement naturel dans la cellule et augmentent ainsi la concentration d'adénosine monophosphate cyclique (AMP cyclique) dans cet emplacement. En disloquant les PDE4, et donc en n'agissant pas directement sur le site catalytique bien conservé, parmi les inhibiteurs de phosphodiestérase, le composé agit par ex. sur le domaine de liaison de PDE4, produisant ainsi des inhibiteurs de PDE4 isoformes spécifiques. La dislocation des PDE4 est visualisée au moyen de fusions avec des protéines GFP. L'emplacement naturel est induit par traitement au Rolipram.
Almholt Dorthe Christensen
Bjorn Sara Petersen
Praestegaard Morten
Scudder Kurt Marshall
Terry Bernard Robert
Bioimage A/s
Sim & Mcburney
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