Chemical Biology and Chemoproteomics for Drug Discovery

Chemical biology and chemoproteomics have become major drivers in drug discovery. Chemical probes and proteomics allow the identification of potential ligandable sites across the human proteome, including undruggable targets. This enables the discovery of small molecule ligands and novel binding pockets, expanding the possibilities of drug discovery beyond traditional approaches. The field of chemoproteomics is constantly evolving, with advancements in covalent chemoproteomics and reversible small molecule ligand-protein interactions. However, there is still a need for breakthroughs in technology to unlock the full potential of chemoproteomics, particularly in targeting amino acids outside of cysteines and lysines. Additionally, the rational design and development of therapeutic modalities is crucial to convert chemical binders into functional molecules.