Department of Chemistry, Pohang University of Science and Technology, Pohang 790-784, Republic of Korea.
Bioorg Med Chem Lett. 2010 Feb 1;20(3):814-8. doi: 10.1016/j.bmcl.2009.12.103. Epub 2010 Jan 4.
KRN7000 is an important ligand identified for CD1d protein of APC, and KRN7000/CD1d complex can stimulate NKT cells to release a broad range of bioactive cytokines. In an effort to understand the structure-activity relationships, we have carried out syntheses of 26 new KRN7000 analogues incorporating aromatic residues in either or both side chains. Structural variations of the phytosphingosine moiety also include varying stereochemistry at C3 and C4, and 4-deoxy and 3,4-dideoxy versions. Their biological activities are described.
KRN7000 是 APC 中 CD1d 蛋白的重要配体，KRN7000/CD1d 复合物可刺激 NKT 细胞释放广泛的生物活性细胞因子。为了了解结构-活性关系，我们进行了 26 种新的 KRN7000 类似物的合成，这些类似物在任一侧链或两侧链中都包含芳族残基。植烷醇部分的结构变化还包括 C3 和 C4 立体化学的变化，以及 4-脱氧和 3,4-二脱氧版本。描述了它们的生物学活性。
