beta-Glycosphingolipids have emerged as a family of potential ligands for natural killer T (NKT)-regulatory lymphocytes. This subset of regulatory lymphocytes has been implicated in the regulation of autoimmune processes. The major histocompatibility complex (MHC) Class I-like CD1d glycoprotein is a member of the CD1 family of antigen-presenting molecules and is responsible for selection of NKT cells. beta-Glycolipids have been shown to alter immune responses in the opposing settings of autoimmune diseases or cancer. In this review, we discuss the potential use of beta-glycoshpingolipids for NKT-based immunotherapy.