Site-selective modification of native proteins

초록

Site-selective modification of native proteins, which eliminates the need for genetic engineering or complex chemical procedures, has become a cornerstone in chemical biology, biotechnology, and medicine. This strategy enables precise functional analysis and therapeutic applications while preserving protein integrity. Advances in ligand-directed (LD) and linchpin methodologies have significantly enhanced selectivity, while ligandand auxiliary-free techniques targeting lysine (Lys), cysteine (Cys), tyrosine (Tyr), and terminal amino acids overcome limitations of traditional chemical modifications. These advancements facilitate the creation of homogeneous protein conjugates, such as antibody-drug conjugates (ADCs), and expand the repertoire of modifiable residues. Furthermore, site-selective modification under native cellular conditions allows for in situ studies of protein function within living cells, offering valuable insights into the biological roles of proteins.

키워드