Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 2 Nanwei Rd., Xicheng District, Beijing 100050, PR China.
Bioorg Med Chem Lett. 2011 Jul 15;21(14):4292-5. doi: 10.1016/j.bmcl.2011.05.056. Epub 2011 May 25.
A series of new muramyl dipeptide (MDP) mimics were designed and synthesized via a solid-phase synthetic route. Their adjuvant activities were evaluated ex vivo for investigation of the synergism of the S(28-39) peptide, which is an MHC class I binding epitope of recombinant hepatitis B surface antigen (HBsAg) for both humans and mice. Several compounds without the carbohydrate moiety exerted better adjuvanticity than the MDP-C that has been reported by our laboratory previously. A primary screening test revealed that compounds 6, 14 and 16 exhibited stronger adjuvanticity compared with other MDP mimics.
设计并合成了一系列新型的 muramyl dipeptide (MDP) 类似物,通过固相合成路线。对它们的佐剂活性进行了体外评估,以研究 S(28-39)肽的协同作用,该肽是重组乙型肝炎表面抗原 (HBsAg) 的 MHC 类 I 结合表位,对人和小鼠均有效。一些没有碳水化合物部分的化合物表现出比我们实验室之前报道的 MDP-C 更好的佐剂活性。初步筛选测试表明,与其他 MDP 类似物相比,化合物 6、14 和 16 具有更强的佐剂活性。