Sakai T, Naidenko O V, Iijima H, Kronenberg M, Koezuka Y
Pharmaceutical Research Laboratory, Kirin Brewery Company, Ltd., 3 Miyahara-cho, Takasaki-shi, Gunma 370-1295, Japan.
J Med Chem. 1999 May 20;42(10):1836-41. doi: 10.1021/jm990054n.
A representative alpha-galactosylceramide (alpha-GalCer), KRN7000, has strong immunostimulatory and antitumor activity. Recent studies demonstrated that KRN7000-pulsed antigen-presenting cells (APC) can activate natural killer T (NKT) cells, a novel T-cell lineage, and CD1d molecules on APC play an important role in the activation of NKT cells. However, it remains unclear whether alpha-GalCers actually bind to CD1d molecules. To address this question, we synthesized three kinds of biotinylated alpha-GalCer and a biotinylated beta-GalCer and found that the biotinylated alpha-GalCers significantly stimulate the proliferation of murine spleen cells, but the biotinylated beta-GalCer does not and that all biotinylated compounds bind to CD1d molecules.
一种具有代表性的α-半乳糖神经酰胺（α-GalCer），即KRN7000，具有很强的免疫刺激和抗肿瘤活性。最近的研究表明，用KRN7000脉冲处理的抗原呈递细胞（APC）可以激活自然杀伤T（NKT）细胞，这是一种新型的T细胞谱系，并且APC上的CD1d分子在NKT细胞的激活中起重要作用。然而，α-GalCers是否真的与CD1d分子结合仍不清楚。为了解决这个问题，我们合成了三种生物素化的α-GalCer和一种生物素化的β-GalCer，发现生物素化的α-GalCers能显著刺激小鼠脾细胞的增殖，但生物素化的β-GalCer不能，并且所有生物素化化合物都能与CD1d分子结合。
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