Barr Tivon

Introduction Click to copy section linkSection link copied! Chemical probes that form a covalent bond with their target protein can offer many advantages over noncovalent probes, such as improved potency, longer duration of action and enhanced selectivity when targeting a nonconserved protein nucleophile.

Abstract There is a growing demand for covalent tool compounds and chemical probes to investigate and perturb protein function and dysregulation. The combination of a covalent electrophile with a peptide or protein-based scaffold with an extended binding footprint enables the targeting of shallow protein surfaces, not typically addressable using small molecules.