Methionine aminopeptidases (MetAPs) are a critical class of metalloproteases responsible for removing the N-terminal methionine residue from newly synthesized proteins, essential for the maturation and function of proteins. The MetAP family includes two main forms, MetAP1 and MetAP2, localized in the cytoplasm and nucleus, respectively. They are widely distributed across various cells and tissues, participating in multiple biological processes, including cell cycle regulation, signal transduction, and stress response. The activity and expression of MetAPs are tightly regulated, with aberrant expression or functional mutations associated with the development of cancers, infections, and metabolic diseases. Therefore, MetAPs represent an important target in drug development, especially in the fields of anticancer and antimicrobial therapy.