Although the initial idea of PROTACs is now already more than 20 years old, having emerged in 1999, and being concretized with the publication of the first PROTAC, for which the target was the Methionine aminopeptidase-2 (MetAP-2) in 2001 [17], it is only very recently that there has been an exponential growth in their development [18], presenting a great potential to become the future blockbuster in cancer therapy [19]. Here, METAP2 is linked to cancer.