Coiled-coil fusion proteins comprising cell receptor domains

C - Chemistry – Metallurgy – 12 – N

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Details

C12N 15/62 (2006.01) A61K 38/00 (2006.01) C07K 19/00 (2006.01) C12N 15/63 (2006.01)

Patent

CA 2536936

Fusion proteins and coiled-coil induced dimers prepared from both the ectodomains and the kinase domains are disclosed. The receptor domains when presented in the form of a homodimer or heterodimer by virtue of the coiled- coil tag have enhanced ligand binding activity or enhanced kinase activity. The kinetics of binding and the antagonistic potencies of the ectodomain dimers, and their use to alter or inhibit signaling is described. Application of the ectodomain and kinase domain dimers in assays for selecting compounds capable of inhibiting ligand binding and kinase activity, respectively, is described.

L'invention concerne des protéines hybrides et dimères induits bispiralés qui sont préparés à partir des ectodomaines and des domaines kinases. Les domaines de récepteurs présentent une activité améliorée de liaison aux ligands ou de kinase lorsqu'ils se présentent comme un homodimère ou un hétérodimère grâce au fragment bispiralé. Les cinétiques de liaison et efficacité antagoniste des dimères des ectodomaines et leur utilisation pour modifier ou inhiber la signalisation sont mentionnées. L'utilisation des dimères des ectodomaines et des domaines de kinases dans des dosages afin de sélectionner les composés qui peuvent inhiber les activités de liaison aux ligands et de kinase respectivement est mentionnée.

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