Competitive Advantages:
Chemo diversity, enhanced conformational rigidity, and greater protease resistance, Increased conformational constraint and binding affinity, Proven method of drug discovery.
A one-bead-two-compound combinatorial synthesis techÂnique provides libraries of macrocyclic peptidomimetic compounds and compositions with use as ligands for the Ephrin type-A receptor 2 (EphA2). The one-bead-two-comÂpound technique and libraries of macrocyclic compounds are useful as research tools in drug discovery and/or to treat or prevent a range of diseases or disorders.Combinatorial chemistry serves as a powerful tool for ligand screening against potential protein and peptide targets. However, macrocyclic peptidomimetic combinatorial libraries are virtually nonexistent. Described is a new class of peptidomimetic macrocyclic combinatorial library which provides a novel method of drug discovery. The library is based on the use of peptide mimicking molecules with ?-AApeptide backbones and macrocyclic functional groups for binding specific biological targets. The advantages are the unique structure of its ligands as macrocyclic and peptidomimetic molecules. The ?-AApeptide backbones ensure chemo diversity, enhanced conformational rigidity, and greater protease resistance. This has been used successfully to identify a ligand targeting receptor tyrosine kinase, a protein involved in melanoma, ovarian, breast, and lung cancers, but has unlimited applications.
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