C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/00 (2006.01) A61K 38/02 (2006.01) A61K 38/44 (2006.01) A61K 39/00 (2006.01) C12Q 1/26 (2006.01) G01N 33/50 (2006.01) G01N 33/542 (2006.01) G01N 33/573 (2006.01)
Patent
CA 2441291
Light-generating fusion proteins having a ligand binding site and a light- generating polypeptide moiety and their use as diagnostics, in drug screening and discovery, and as therapeutics, are disclosed. The light-generating fusion protein has a feature where the bioluminescence of the polypeptide moiety changes upon binding of a ligand at the ligand binding site. The ligand may be, for example, an enzyme present in an environment only under certain conditions, e.g., ubiquitin ligase in a hypoxic state, such that the light- generating fusion protein is "turned on" only under such conditions.
L'invention concerne des protéines de fusion générant de la lumière, possédant un site de liaison et un fragment polypeptidique générant de la lumière, ainsi que leur utilisation en tant qu'agents de diagnostic, dans le criblage et la découverte de médicaments et en tant qu'agents thérapeutiques. La protéine de fusion générant de la lumière se caractérise en ce que la bioluminescence du fragment polypeptidique change lors de liaison d'un ligand au niveau du site de liaison du ligand. Le ligand peut être, par exemple, une enzyme présente dans un environnement seulement dans certaines conditions, par exemple l'ubiquitine-ligase à l'état hypoxique, de sorte que la protéine de fusion générant de la lumière ne soit <= activée >= que dans certaines conditions.
Ivan Mircea
Kaelin William G.
Dana-Farber Cancer Institute Inc.
Smart & Biggar
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