Methionine aminopeptidases (MetAP), also designated peptidase M proteins, are members of the M24 family of proteins. Both MetAP-1 and MetAP-2 release N-terminal amino acids, usually methionine, from nascent peptides and arylamines. Eukaryotes contain both MetAP-1 and MetAP-2, whereas prokaryotes possess only the MetAP-1 enzyme. MetAP-1 and MetAP-2 control cell proliferation in mammalian cells. MetAP-2 is highly conserved between human and Saccharomyces cerevisiae. Neurofibromin (NF1) regulates MetAp-2 and increased expression of MetAP-2 correlates with several forms of cancer. Inhibitors of MetAP-2 are potential targets in cancer therapeutics, particularly in NF1-associated tumor proliferation. Chemotherapeutic drugs such as ovalicin and fumagillin bind to the active site of and inhibit MetAp-2.
