STAPLED PEPTIDE THERAPEUTIC FOR NON-DRUGGABLE TARGETS

Existing therapeutic platforms and drug arsenals utilize small molecules and large antibody proteins, addressing only 20 percent of the druggable market. The chemical space required for inhibition of protein-protein interactions is considered “undruggable” and remains underexplored. Undesirable properties of peptides such as instability, lack of cell/ tissue penetration, and immunogenicity of synthetics compound the problem and make it unsuitable for use in humans.

The new method is a proprietary facile and efficient synthetic platform method to generate high yield stapled peptides involving macrocyclization and a two-component thiol-ene based reaction.