Single-site labeling of lysine in proteins through a metal-free multicomponent approach†
We report a chemoselective and site-selective approach that distinguishes one Lys from its multiple copies, N-terminus, and other competitors. The phospha-Mannich protocol works with multiple proteins and installs probes without structural and functional perturbations. It delivers an antibody–drug conjugate with selective anti-proliferative activity towards HER2 expressing SKBR3 breast cancer cells.
- This article is part of the themed collection: 20th Anniversary of the CRSI: Celebrating Indian Chemistry in ChemComm