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Improved Th17 Selectivity of α‑Galactosylceramide via Noncovalent Interactions with Diether Moiety

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journal contribution
posted on 04.04.2019, 00:00 by Yoon Soo Hwang, Junhyeong Yim, Heebum Song, Seung Bum Park
α-Galactosylceramide (α-GalCer) is a typical antigen for invariant natural killer T cells that are a subset of T cells and play critical roles in regulating immune responses. To selectively induce the secretion of certain cytokines via introducing hydrogen-bonding interaction with polar amino acid residues in the binding pocket of CD1d, a series of α-GalCer analogues with diether moiety in the acyl chain were designed and synthesized. The subsequent in vitro biological evaluation of these analogues revealed the structure–activity relationship for the selective IL-17 secretion. Analogues 5 and 6 induced the significantly increased IL-17 secretion over other cytokines, suggesting protective effects against pathogens. In contrast, analogue 7 showed the highly reduced IL-17 secretion, which may indicate potential anti-inflammatory effects.