nkt cell

α-Galactosylceramide (KRN7000) 是一种具有抗肿瘤和免疫刺激作用的合成糖脂。它是一种高效的 NKT 细胞激动剂，可与 CD1d 有效结合。它与 CD1d 的复合物可与 NKT 细胞的 T 细胞抗原受体结合。

Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminomethyl)benzamide) is the analogue of BMS-509744, which can potently and selectively inhibit Itk kinase activity. In vitro: BMS-509744 could reduce TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells [1]. In vivo: BMS-509744 suppressed the production of IL-2 induced by anti-TCR antibody administered to mice. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1]. Clinical trial: Up to now, both BMS-509744 and ITK inhibitor is still in the preclinical development stage.

GCS-12 作为一种 Th1 2 平衡的磺酰胺糖脂,主要通过增强与CD1d的相互作用来发挥作用.该化合物能激活自然杀伤 T 细胞 (NKT cell),诱导它们分泌细胞因子IFN-γ和IL-4,进而在小鼠体内展示出显著的免疫调节和抗肿瘤活性.