ABSTRACT

Metal ions are essential for the living process of organisms physiologically and pathologically, interacting with numerous proteins in biological systems. Metal ions have also been incorporated into pharmaceuticals for diagnostic and therapeutic purposes. However, their mechanisms of action remain uncharted due to the difficulty in mapping their interactive proteomes in the complex biological 266system. Recently, the introduction and development of metalloproteomics facilitates the metal-associated proteomes to be tracked, which provides a fundamental basis for further unveiling the modes of action of metallo-drugs. In this chapter, we introduce the development of metalloproteomics, including the methodology, its implementation in biomedical studies such as anticancer and antimicrobial mechanistic studies of metallo-drugs, and pinpoint the potential application of metalloproteomics in other research areas in the future.