Corticotropin-releasing factor-binding-protein inhibitors...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 14/575 (2006.01) A61K 38/00 (2006.01) A61K 38/03 (2006.01) A61K 38/22 (2006.01) A61K 45/00 (2006.01) A61P 25/24 (2006.01) A61P 25/28 (2006.01) A61P 25/30 (2006.01) C07K 4/12 (2006.01) C07K 14/47 (2006.01) G01N 33/53 (2006.01) G01N 33/541 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2195197

Levels of free corticotropin-releasing factor (CRF) in the brain are increased by administration to a patient of a ligand inhibitor of a CRF/CRF-binding protein complex. The ligand inhibitor binds to CRF-binding protein causing the release of CRF. The ligand inhibitor may be a peptide derived from CRF or a related protein or a non-peptide. Administration of the ligand inhibitor may provide improvement in learning and memory, resulting in decreased food intake or provide treatment for diseases associated with low levels of CRF in the brain, notably Alzheimer's disease. A method is also provided for screening compounds to select particularly effective CRF antagonists for in vivo administration to mammals.

On accroît le taux du facteur de libération de la corticotropine (CRF) dans le cerveau en administrant à un patient un inhibiteur de ligand d'un complexe CRF/protéine de liaison du CRF. L'inhibiteur de ligand se lie à la protéine de liaison du CRF, provoquant ainsi la libération du CRF. Ledit inhibiteur de ligand peut être un peptide dérivé du CRF ou une protéine apparentée ou un non peptide. L'administration de l'inhibiteur de ligand peut améliorer l'apprentissage et la mémoire, ce qui entraîne une baisse de la prise d'aliments, ou constituer un traitement pour des maladies associées à des taux faibles de CRF dans le cerveau, notamment la maladie d'Alzheimer. La présente invention concerne également un procédé de sélection de composés destiné à sélectionner des antagonistes de CRF particulièrement efficaces en vue de l'administration in vivo à des mammifères.

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