Given therelevance of dipeptidyl peptidase IV (DPP IV) and carbonic anhydraseisoforms II and V (CAs II and V) roles in the pathology of T2DM aswell as in the weight loss, multitarget ligands able to modulate theseenzymes could represent a promising therapeutic approach for antidiabesitytreatment. The gene discussed is CA2; the disease is type 2 diabetes mellitus.