The design and development of covalent protein-protein interaction inhibitors for cancer treatment.

摘要: Protein-protein interactions (PPIs) are central to a variety of biological processes, and their dysfunction is implicated in the pathogenesis range human diseases, including cancer. Hence, inhibition PPIs has attracted significant attention drug discovery. Covalent inhibitors have been reported achieve high efficiency through forming covalent bonds with cysteine or other nucleophilic residues target protein. Evidence suggests that there reduced risk for development resistance against drugs, which major challenge areas such as oncology infectious diseases. Recent improvements structural biology chemical reactivity enabled design potent selective PPI inhibitors. In this review, we will highlight therapeutic agents targeting cancer therapy.