We observed efficient and selective depletion of Malat1 lncRNA in PSMA+/+ cancer cells with almost no activity in PSMA−/− cells for AS02-md and ASO3-bmd conjugates with PSMA ligand MA-257 at concentrations from 100 nM to 10 μM, which confirms the promise of mesyl and busyl phosphoramidate ASO modifications for the targeted RNA therapy. Here, MALAT1 is linked to cancer.