Protein-protein interaction antagonist screening libraries...

Combinatorial chemistry technology: method – library – apparatus – Library – per se – Library containing only organic compounds

Reexamination Certificate

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C506S013000, C562S063000

Reexamination Certificate

active

07662750

ABSTRACT:
The present invention relates to 1,4-disubstituted naphthalene scaffold compounds and other closely related scaffold compounds. The present invention also relates to combinatorial libraries of such compounds. In addition, the present invention relates to a method of identifying a protein-protein interaction antagonist. The method first involves providing a compound as described herein. Next, the compound is contacted with interacting proteins of a protein-protein interaction target complex, whereby the compound is allowed to compete with the interacting proteins. Then, the activity of the compound for inhibiting formation of the protein-protein interaction target complex is measured. Finally, the compound that inhibits formation of the protein-protein interaction target complex is identified as a protein-protein interaction antagonist. Also disclosed is a method for modulating a protein-protein interaction. The method involves contacting interacting proteins of a protein-protein interaction target with a compound as described herein, whereby the protein-protein interaction between the interacting proteins is modulated.

REFERENCES:
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Dixon et al., “Preparation of a Series of Substituted Fluoromethylnaphthalenes,” Canadian J. of Chemistry, 59:2629-41 (1981).
Ji et al., “Privileged Scaffolds for Blocking Protein-Protein Interactions: 1,4-Disubstitued Naphthalene Antagonists of Transcription Factor Complex HOX-PBX/DNA,”Bioorganic&Medicinal Chemistry Letters14:3875-3879 (2004).
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