Given the relevance of the DPP IV/CA (II andV) roles in both T2DM and obesity, multitarget ligands able to modulatethese enzymes could represent a novel and promising therapeutic approach.Repositioning of WB-4101 and morphing its structure have been thestrategies applied to obtain potent and selective multitarget ligandsagainst DPP IV and CAs (isoforms II and V). This evidence concerns the gene DPP4 and obesity due to melanocortin 4 receptor deficiency.