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There are numerous drug targets that cannot be readily addressed by standard industry ('Lipinski Rule of 5') compounds. In many of these cases, the protein target works by recognizing another protein or peptide substrate through an extended binding motif – by interacting over a large surface area rather than tightly via a small "active site". Disrupting such large surface area motifs is an attractive strategy for drug discovery, and has been observed repeatedly in nature through the activity of large secondary metabolites with a circular backbone, called macrocycles. But creating diverse macrocycles synthetically in the laboratory in large numbers, as is needed for drug discovery, has been extremely difficult.
By using DPC™, Ensemble is able to synthesize and rapidly test collections of macrocyclic Ensemblins against extended binding motif targets, and our portfolio has been selected by choosing mechanistically validated targets that represent a medical need and commercial opportunity. These programs include finding novel molecules such as:
- Disruptors of protein-protein interactions
Ensemble is searching for unprecedented drug-like macrocycles to treat cancer by disrupting certain anti-apoptotic protein complexes.
- Novel protease inhibitors
Ensemble is targeting various proteases involved in neuropathological, infectious and oncologic diseases.
- Novel phosphatase inhibitors
Ensemble is developing inhibitors of the phosphatase PTP1B, a novel class of ‘insulin sensitizer’ drugs useful in the management of type 2 diabetes and metabolic syndrome.
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