Protein-protein interaction antagonist screening libraries based upon 1,4-disubstitued napthalenes and related scaffolds
Combinatorial screening libraries with high “hit rates” for challenging protein-protein interaction drug targets are extremely difficult to obtain. This invention describes a novel seed compound (the 1,4-disubstituted naphthalene privileged scaffold ), the process of synthesizing it in stable form and methods to make targeted libraries based on this compound as well as its modifications.
To arrive at this optimal compound, the inventors selected certain compounds that participate in a wide v ariety of naturally occurring reactions. It is known that several of these possess a helix-turn-helix structure and favor analogous affinity approaches to specific kinds of ligands. Rigorous experiments proved that certain kinds of di-substituted nap hthalenes are able to replicate the reactive abilities of naturally occurring ligands and binders. Among these, the seed compound above has been identified as a “best fit” compound for 3 “representative” compounds from the transcription factors famil y.
These new compounds are expected to provide high hit rates against protein-protein interaction targets (especially the helix-turn-helix type of transcription factors). The application scenario spans the vast spectrum of the proteomics, pharmac eutical and biotechnology industries.
Categories: Screening, Materials & Chemicals
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