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Methionine aminopeptidase is a metalloenzyme with two structurally distinct forms in humans, MetAP\u20101 and MetAP\u20102. The MetAP2 inhibitor fumagillin, which was used as an amebicide in the 1950s, has been used for the successful treatment of microsporidiosis in humans; however, it is no longer commercially available. Despite significant efforts and investments by many pharmaceutical companies, no new MetAP inhibitors have been approved for the clinic. Several lead compounds have been designed and synthesized by researchers as potential inhibitors of MetAP and evaluated for their potential activity in a wide range of diseases. MetAP inhibitors such as fumagillin, TNP\u2010470, beloranib, and reversible inhibitors and their analogs guide new prospects for MetAP inhibitor development in the ongoing quest for new pharmacological indications. This perspective provides insights into recent advances related to MetAP, as a potential therapeutic target in drug discovery, bioactive small molecule MetAP2 inhibitors, and data on the role of MetAP\u20102 as a therapeutic target for microsporidiosis.<\/jats:p>","DOI":"10.1111\/jeu.13036","type":"journal-article","created":{"date-parts":[[2024,7,22]],"date-time":"2024-07-22T10:21:18Z","timestamp":1721643678000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":13,"title":["Methionine aminopeptidases: Potential therapeutic target for microsporidia and other microbes"],"prefix":"10.1111","volume":"71","author":[{"ORCID":"https:\/\/orcid.org\/0000-0002-5837-027X","authenticated-orcid":false,"given":"Bhaskar C.","family":"Das","sequence":"first","affiliation":[{"name":"Arnold and Marie Schwartz College of Pharmacy and Health Sciences Long Island University  Brooklyn New York USA"},{"name":"Department of Medicine and Pharmacological Sciences Icahn School of Medicine at Mount Sinai  New York New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Parthiban","family":"Chokkalingam","sequence":"additional","affiliation":[{"name":"Arnold and Marie Schwartz College of Pharmacy and Health Sciences Long Island University  Brooklyn New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mohammed Adil","family":"Shareef","sequence":"additional","affiliation":[{"name":"Arnold and Marie Schwartz College of Pharmacy and Health Sciences Long Island University  Brooklyn New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Srushti","family":"Shukla","sequence":"additional","affiliation":[{"name":"Arnold and Marie Schwartz College of Pharmacy and Health Sciences Long Island University  Brooklyn New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Sasmita","family":"Das","sequence":"additional","affiliation":[{"name":"Arnold and Marie Schwartz College of Pharmacy and Health Sciences Long Island University  Brooklyn New York USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mariko","family":"Saito","sequence":"additional","affiliation":[{"name":"Nathan S. 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