MetAP-1 inhibitors belong to a class of chemical compounds specifically designed to target and modulate the activity of Methionine Aminopeptidase-1 (MetAP-1), an essential enzyme involved in protein maturation and regulation of protein function. MetAP-1 is a metalloenzyme found in nearly all organisms, from bacteria to humans, and plays a crucial role in post-translational protein processing. Its primary function is to cleave the initiator methionine (Met) from newly synthesized polypeptide chains, which is often the first amino acid in a nascent protein. This enzymatic cleavage is essential for the proper folding, stability, and function of many proteins, as the removal of the initiator Met allows the protein to adopt its correct conformation. Inhibitors designed to target MetAP-1 are primarily employed in molecular and cellular biology research to investigate the functional properties and regulatory mechanisms associated with this enzyme.The development of MetAP-1 inhibitors typically involves a combination of biochemical, biophysical, and structural approaches aimed at identifying or designing molecules that can selectively interact with MetAP-1 and modulate its enzymatic activity. By inhibiting MetAP-1, these compounds can disrupt the removal of initiator Met, leading to aberrant protein maturation and affecting the functionality of specific proteins in cellular processes. Researchers use MetAP-1 inhibitors to explore the intricate roles played by this enzyme in cellular functions, attempting to unravel its contributions to protein quality control, post-translational modifications, and interactions with other cellular pathways. Furthermore, these inhibitors serve as valuable tools for dissecting the broader network of cellular processes involving protein maturation, contributing to our understanding of fundamental cell biology mechanisms and providing insights into avenues for further scientific exploration.