Novel binding site of IKK-beta
AssigneeMacau University of Science and Technology
InventorsLiang LIU, Ting LI, Kam Wai WONG, Zhihong JIANG, Hua ZHOU
Life of this patent
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Abstract
Uses and applications derived from the discovery of a novel binding site of IKK-β, such as method of screening a therapeutic agent as drug candidate for treating cancer, inflammation, or other diseases/disorders, are provided.
Claims32
A method of screening a therapeutic agent as a drug candidate for cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder comprising:
- a) exposing said agent to an assay comprising IKK-β;
- b) detecting whether said agent binds to cysteine-46 residue of IKK-β;
- c) detecting whether said agent inhibits kinase activity of IKK-β upon said binding in step (b);
- and
- d) identifying a drug candidate that performs said binding action of step (b) and said inhibition action of step (c).
A method for diagnosing cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder in a patient comprising:
- a) obtaining a sample from said patient;
- b) contacting said sample with a compound that binds to cysteine-46 residue of IKK-β of said sample;
- c) detecting binding of said compound to IKK-β in said sample;
- d) detecting inhibition action on kinase activity of IKK-β by said compound upon said binding in step (c);
- and
- e) diagnosing said patient as having a likelihood to develop cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder if said compound cannot perform said binding action of step (c) and/or said inhibition action of step (d).
A method of screening a patient to have a likelihood to develop cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder comprising:
- a) obtaining a sample from said patient;
- b) contacting said sample with a compound that binds to cysteine-46 residue of IKK-β of said sample;
- c) detecting binding of said compound to IKK-β in said sample;
- d) detecting inhibition action on kinase activity of IKK-β by said compound upon said binding in step (d);
- and
- e) identifying said patient as having a likelihood to develop cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder if said compound cannot perform said binding action of step (c) and/or said inhibition action of step (d).
A method for treating cancer, inflammation, neurodegenerative disease, immunological disorder, or arthritic disorder comprising administering an effective amount of a therapeutic agent to a patient in need thereof, wherein said patient harbors gene mutations on at least one binding site of IKK-β;
- said mutated binding site is selected from a group consisting of phenylalanine residue, serine-177/181 residue, allosteric binding site of IKK-β, and cysteine residue except cysteine-46 residue.
Dependencies are inferred from the claim text.